Category: 130049-82-0

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one. A new synthetic method of this compound is introduced below., COA of Formula: C11H15ClN2O2

(II) hydrochloride (48.77 g, 0.195 mol), (III) (48.54 g, 0.2 mol)(50.4 g, 0.6 mol), potassium iodide (3.3 g, 0.02 mol), 400 mL of acetonitrile and 100 mL of water were heated to 65 G in a 1000 mL three-necked flask and stopped for 16 h reaction. Cooling to 25 G, slowly add lOOmL of water to the system, a large number of solid material precipitation, stirring 30 min, the filter to get crude, filter cake with acetonitrile and water were washed solid, dryingOf crude 72.0 g.The crude product of 72.0 g of (I) was placed in 720 mL of water at a temperature of 20-25 C, 16.8 mL of concentrated hydrochloric acid was added, stirred to form (I) hydrochloride, and the aqueous solution of (I) was washed with 500 mL of dichloromethane 2 times, take the aqueous solution layer, add 7.2g activated carbon decolorization, heating to 50 e, stirring 30min, the filter (I) hydrochloric acid solution.The aqueous solution of (I) salt was cooled to 0-10 C and 500 mL of isopropyl alcohol was added to the system at a temperature of 0-10 C,A solution of 20% sodium hydroxide was slowly added with stirring to adjust the pH of the system to 8-9 to give (I) as a white solid. After the dropwise addition, the mixture was stirred at this temperature for 1 hour and filtered to obtain a solid material. Isopropyl alcohol and water (100 mL + 100 mL), and the resulting solid was (I), about 55.0 g.The above-obtained (I) was added to a mixed solvent of 1100 mL of ethanol and 333 mL of water and heated to reflux to a solid materialDissolved in the lh, slowly cooled to 0-5 e, stirring at this temperature for 16h, to obtain a white solid crystalline material, filtration, to obtain high purity (I), drying to get the product 49.2g, yield 60 %.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one.

Reference:
Patent; JIANGSU CHIATAI QINGJIANG PHARMACEUTICAL CO LTD (CTQJ); WANG, WUWEI; CHEN, JIE; WU, TINGZHAO; GU, HAICHENG; HE, JIA; (7 pag.)CN103214485; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Researchers who often do experiments know that organic synthesis is a process of preparing more complex target molecules from simple raw materials through one or more chemical reactions. Generally, it requires fewer steps,and cheap raw materials. 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one. A new synthetic method of this compound is introduced below., COA of Formula: C11H15ClN2O2

(II) hydrochloride (48.77 g, 0.195 mol), (III) (48.54 g, 0.2 mol)(50.4 g, 0.6 mol), potassium iodide (3.3 g, 0.02 mol), 400 mL of acetonitrile and 100 mL of water were heated to 65 G in a 1000 mL three-necked flask and stopped for 16 h reaction. Cooling to 25 G, slowly add lOOmL of water to the system, a large number of solid material precipitation, stirring 30 min, the filter to get crude, filter cake with acetonitrile and water were washed solid, dryingOf crude 72.0 g.The crude product of 72.0 g of (I) was placed in 720 mL of water at a temperature of 20-25 C, 16.8 mL of concentrated hydrochloric acid was added, stirred to form (I) hydrochloride, and the aqueous solution of (I) was washed with 500 mL of dichloromethane 2 times, take the aqueous solution layer, add 7.2g activated carbon decolorization, heating to 50 e, stirring 30min, the filter (I) hydrochloric acid solution.The aqueous solution of (I) salt was cooled to 0-10 C and 500 mL of isopropyl alcohol was added to the system at a temperature of 0-10 C,A solution of 20% sodium hydroxide was slowly added with stirring to adjust the pH of the system to 8-9 to give (I) as a white solid. After the dropwise addition, the mixture was stirred at this temperature for 1 hour and filtered to obtain a solid material. Isopropyl alcohol and water (100 mL + 100 mL), and the resulting solid was (I), about 55.0 g.The above-obtained (I) was added to a mixed solvent of 1100 mL of ethanol and 333 mL of water and heated to reflux to a solid materialDissolved in the lh, slowly cooled to 0-5 e, stirring at this temperature for 16h, to obtain a white solid crystalline material, filtration, to obtain high purity (I), drying to get the product 49.2g, yield 60 %.

If you are interested in these compounds, you can also browse my other articles.Thank you for taking the time to read this article. I hope you enjoyed it, 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one.

Reference:
Patent; JIANGSU CHIATAI QINGJIANG PHARMACEUTICAL CO LTD (CTQJ); WANG, WUWEI; CHEN, JIE; WU, TINGZHAO; GU, HAICHENG; HE, JIA; (7 pag.)CN103214485; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, the common compound, a new synthetic route is introduced below. Recommanded Product: 130049-82-0

EXAMPLE 8 Preparation of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]ethyl]-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (Formula I), Using Microwave Radiation 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (5 g), 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole monohydrochloride (5.2 g), methanol (200 mL) and N-(1-methylethyl)-2-propanamine (4.16 g) were charged into a microwave reactor vessel. Microwave radiation was applied for 7 minutes (temperature raised to 70 C.). After completion of the reaction, solvent was distilled completely under vacuum. To the residue, water (25 mL) was added and the mixture was extracted with dichloromethane (3*25 mL). Combined organic layer was distilled under vacuum at 40 C. to afford a residue. To the residue, acetone (100 mL) was added and heated to reflux for 10 minutes. The mass cooled to 30 C., maintained for about 10-15 minutes, filtered and washed with acetone (5 mL). The solid was dried at 58 C. to afford 4.5 g of the title compound.

The synthetic route of 130049-82-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Padi, Pratap Reddy; Bollikonda, Satyanarayana; Akundi, Surya Prabhakar; Cherukupally, Praveen; Suthrapu, Sashikanth; Mohanarangam, Saravanan; Kandirelli, Venkat Kiran; Chellu, Malleswara Rao; Pagadala, Narasimha Rao; US2009/48272; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound, 130049-82-0, blongs to pyrimidines compound. Application In Synthesis of 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one

Example 1 – Synthesis of 3-[2-[4-(6-fluoro-1,2-benzoisoxazol-3-yl)-1-piperidinyl]ethyl-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]-pyrimidin-4-one hydrochloride (Paliperidone hydrochloride) 6-Fluoro-3-(4-piperidinyl)-1,2-benzoisoxazole hydrochloride (300 g, 1.17 mols), 3-(chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidin-4-one (343 g, 1.40 mols) and triethylamine (272 g, 2.69 mols) are suspended in methanol (1.5 1) in a 3000 ml reactor under nitrogen atmosphere, and the reaction mixture is heated at reflux temperature for 18-20 h. Conversion to the product is checked by HPLC titre, obtaining a yield of 96.5% in solution. The mixture is concentrated to a residue. The so obtained product has an XRPD spectrum as shown in Figure 5, and a DSC thermogram as shown in Figure 6, which are characteristic of paliperidone crystalline Form I. The mixture is taken up with demineralised water (1.5 1) and 36.5% hydrochloric acid (113 g, 1.13 mols), obtaining a solution with a pH of 3-4. A solid then reprecipitates, and the mixture is cooled to 0C and filtered. The solid is washed with demineralised water cooled to 0-5C (2 x 150 ml), and then with acetone cooled to 0-5C (3 x 200 ml). The solid is dried in oven under reduced pressure at a temperature of 50C for 16-18h. 451 g of paliperidone hydrochloride is obtained, with a potentiometric titre of 99.9%, an argentimetric titre of 7.8%, 99.2% HPLC purity, and a total yield of 90%. The product has an XRPD spectrum as shown in Figure 1, and a DSC thermogram as shown in Figure 2.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,130049-82-0, its application will become more common.

Reference:
Patent; Dipharma Francis S.r.l.; EP2243780; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 130049-82-0, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 130049-82-0 as follows.

To a methanol (500 mL) solution, nitrogen was purged for 30 minutes to remove the nascent oxygen. 6-Fluoro-3-piperidin-4-yl-benzo[d]isoxazole Hydrochloride (50 g), 9-Hydroxy-3-(2-chloroethyl)-2-methyl-6,7,8,9-tetrahydro-4H-pyrido (1,2-a) pyrimidine-4-one (52 g) and triethylamine (55) were added and stirred at reflux for 30-32 hours. The reaction mixture was cooled to 25-35 C, and filtered off to yield paliperidone base. Yield: 75 g.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,130049-82-0, its application will become more common.

Reference:
Patent; ORCHID CHEMICALS & PHARMACEUTICALS LIMITED; US2010/298566; (2010); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, the common compound, a new synthetic route is introduced below. Recommanded Product: 130049-82-0

300 ml of acetonitrile was charged followed by 20.0 g of 3-(2-chloroethyl)-9-hydroxy-2- methyl-6,7,8,9-tetrahydro-4H-pyrido-[1 ,2-a]-pyrimidin-4-one and 21.0 g of 6-fluoro-3-(4- piperidinyl)-1 ,2-benzisoxazole hydrochloride at room temperature. The reaction mass was stirred at room temperature for 5 minutes and 20.0 g of potassium carbonate and 0.7 g of potassium iodide were charged. Further, 0.2 g of sodium borohydride was charged and the temperature was raised to 65+/-2C. The reaction mass was maintained at 65+/-2C for 25 hours. After reaction completion, the reaction mass was slowly cooled to room temperature. The solids were filtered, washed with 50 ml of acetonitirle and then dissolved in 800 ml of methylene chloride at room temperature. The contents were heated to 30-35C, maintained for 10 minutes, filtered and washed with 20 ml of methylene chloride. The clear filtrate was distilled completely under vacuum below 35C and replaced with 50 ml of acetone. Further, 300 ml of acetone was charged, heated to 45C and stirred for 30 minutes. The reaction mass was cooled to room temperature and stirred for 1 hour. The product was filtered, washed with 20 ml of acetone and dried under vacuum at 50-55C to yield paliperidone (30 g, yield : 150% w/w, efficiency : 85. 1 %, keto impurity by HPLC : 0.01%, total impurity level by HPLC: 1.0 %)

The synthetic route of 130049-82-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; CIPLA LIMITED; PUPPALA, Ravikumar; PATHI, Srinivas, Laxminarayan; KANKAN, Rajendra, Narayanrao; COTTRILL, Emily, Elizabeth, Helen; WO2012/164242; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, the common compound, a new synthetic route is introduced below. Recommanded Product: 130049-82-0

300 ml of acetonitrile was charged followed by 20.0 g of 3-(2-chloroethyl)-9-hydroxy-2- methyl-6,7,8,9-tetrahydro-4H-pyrido-[1 ,2-a]-pyrimidin-4-one and 21.0 g of 6-fluoro-3-(4- piperidinyl)-1 ,2-benzisoxazole hydrochloride at room temperature. The reaction mass was stirred at room temperature for 5 minutes and 20.0 g of potassium carbonate and 0.7 g of potassium iodide were charged. Further, 0.2 g of sodium borohydride was charged and the temperature was raised to 65+/-2C. The reaction mass was maintained at 65+/-2C for 25 hours. After reaction completion, the reaction mass was slowly cooled to room temperature. The solids were filtered, washed with 50 ml of acetonitirle and then dissolved in 800 ml of methylene chloride at room temperature. The contents were heated to 30-35C, maintained for 10 minutes, filtered and washed with 20 ml of methylene chloride. The clear filtrate was distilled completely under vacuum below 35C and replaced with 50 ml of acetone. Further, 300 ml of acetone was charged, heated to 45C and stirred for 30 minutes. The reaction mass was cooled to room temperature and stirred for 1 hour. The product was filtered, washed with 20 ml of acetone and dried under vacuum at 50-55C to yield paliperidone (30 g, yield : 150% w/w, efficiency : 85. 1 %, keto impurity by HPLC : 0.01%, total impurity level by HPLC: 1.0 %)

The synthetic route of 130049-82-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; CIPLA LIMITED; PUPPALA, Ravikumar; PATHI, Srinivas, Laxminarayan; KANKAN, Rajendra, Narayanrao; COTTRILL, Emily, Elizabeth, Helen; WO2012/164242; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 130049-82-0, Adding some certain compound to certain chemical reactions, such as: 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one,molecular formula is C11H15ClN2O2, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 130049-82-0.

Into a clean 2L, three-necked RB flask equipped with shaft, condenser, and thermo socket was charged 600 ml of DMF, lOOg (0.404 moles) of 3-(2-Chloroethyl)-6,7,8,9- tetrahydro-9-hydroxy-4H-pyrido[l52-a]pyrimidin-4-one of formula- VI obtained from Example 5, 67.19g (0.404 moles) of potassium iodide, 111.91g (0.808moles) of potassium, carbonate and 103.68g (0.404 moles) of 6- fluoro-3-(4- piperidinyl)-l,2- benzisoxazole HCl (formula-VII). The reaction mass was heated to 60-650C and maintained for 18h. Reaction mass was cooled to 25-300C, stirred for Ih and filtered under vacuum. The wet cake was washed with 200ml of DMF. The wet cake was leached with 2 x 500ml of water and 1 x 500ml of methanol. The wet material was dried in the oven at 70-750C for Ih to yield 114g of technical grade paliperidone. Above technical grade paliperidone was recrystallized from methanol via charcoal treatment to get 6Og (34.74% yield) of pure paliperidone. Purity by HPLC is > 99.8%.S Alternatively technical grade paliperidone was purified by the following chemical method.Above technical grade paliperidone (114g) was dissolved in 6.84L of methanol at 65- 7O0C. Charcoal (20 g) was added to the resultant solution and filtered under vacuum using a filter aid. The solvent was distilled of from the filtrate at 60-650C using0 rotavapor under vacuum to get a cream colored solid. Methanol (575 ml) was added to the solid and stirred for 45min at 25-300C. The reaction mass was filtered and dried in an oven at 70-750C to get 90 g of paliperidone.Into a clean and dry IL, three-necked RB flask equipped with shaft, thermo socket,5 addition funnel and stopper was charged 57.0 ml of cone. HCl and 570 ml of water.The reaction mass was stirred for 5min and charged the above solid (9Og). The reaction mass was stirred for 5-10min at 25-300C to get yellow colored clear liquid. pH of the reaction mass was adjusted to 6.0 to 6.5 by dropwise addition of dilute(concentrated aq ammonia solution was diluted with equal volume of water) aq.0 ammonia solution. The reaction mass was stirred for 30min and filtered under vacuum. The wet solid was dried in the oven at 70-750C to get 88g of paliperidoneHCl.Above solid was transferred taken into a IL RB flask containing 570 ml of methanol.5 The suspension was stirred for 30min at 25-3O0C, filtered under vacuum and dried in the oven at 70-750C for Ih to get 85 g pure paliperidone HCl. HPLC purity is > 99.80%.Above paliperidone HCl salt (85.0 g) and 2280 ml of water were suspended in a RB0 flask at 25-300C. pH was adjusted to 8.5 to 9.0 by adding aq. potassium carbonate solution (prepared from 57 g of potassium carbonate and 570 ml of water). The resultant cream-colored suspension was stirred for 30 min at 25-300C and filtered under vacuum. The wet cake was washed with 1500ml of water followed by 300ml of methanol. The wet cake was triturated with 450 ml of methanol for 30 min and filtered. Paliperidone was dried in vacuum oven at 65-70C for 4h to afford 59 g (34.33%) of pure paliperidone. Purity by HPLC is > 99.8%. 1H-NMR (CDCl3): 1.75 (m, 2H, aliphatic-H), 1.95 (m, IH, aliphatic-H), 2.15 (m, 5H, aliphatic-H), 2.24 -2.40 (m, 5H, aliphatic-H), 2.56 (t, 2H, -CH2-, J = 6.84 Hz), 2.76 (t, 2H, -CH2-, J = 7.82 Hz), 3.09 (m, IH, aliphatic-H), 3.18 (d, 2H, aliphatic-H, J =11.72 Hz), 3.92 (m, 2H, aliphatic-H), 4.15 (s, IH, -OH, D2O exchangeable), 4.50 (dd, IH, aliphatic-H J = 3.91 Hz), 7.07 (m, IH, aromatic-H), 7.23 (m, IH aromatic-H), 7.70 (dd, IH, aromatic-H, J= 2.93 Hz).

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; NATCO PHARMA LIMITED; WO2009/10988; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 130049-82-0, Adding some certain compound to certain chemical reactions, such as: 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one,molecular formula is C11H15ClN2O2, can increase the reaction rate and produce products with better performance than those obtained under traditional synthetic methods. Here is a downstream synthesis route of the compound 130049-82-0.

Into a clean 2L, three-necked RB flask equipped with shaft, condenser, and thermo socket was charged 600 ml of DMF, lOOg (0.404 moles) of 3-(2-Chloroethyl)-6,7,8,9- tetrahydro-9-hydroxy-4H-pyrido[l52-a]pyrimidin-4-one of formula- VI obtained from Example 5, 67.19g (0.404 moles) of potassium iodide, 111.91g (0.808moles) of potassium, carbonate and 103.68g (0.404 moles) of 6- fluoro-3-(4- piperidinyl)-l,2- benzisoxazole HCl (formula-VII). The reaction mass was heated to 60-650C and maintained for 18h. Reaction mass was cooled to 25-300C, stirred for Ih and filtered under vacuum. The wet cake was washed with 200ml of DMF. The wet cake was leached with 2 x 500ml of water and 1 x 500ml of methanol. The wet material was dried in the oven at 70-750C for Ih to yield 114g of technical grade paliperidone. Above technical grade paliperidone was recrystallized from methanol via charcoal treatment to get 6Og (34.74% yield) of pure paliperidone. Purity by HPLC is > 99.8%.S Alternatively technical grade paliperidone was purified by the following chemical method.Above technical grade paliperidone (114g) was dissolved in 6.84L of methanol at 65- 7O0C. Charcoal (20 g) was added to the resultant solution and filtered under vacuum using a filter aid. The solvent was distilled of from the filtrate at 60-650C using0 rotavapor under vacuum to get a cream colored solid. Methanol (575 ml) was added to the solid and stirred for 45min at 25-300C. The reaction mass was filtered and dried in an oven at 70-750C to get 90 g of paliperidone.Into a clean and dry IL, three-necked RB flask equipped with shaft, thermo socket,5 addition funnel and stopper was charged 57.0 ml of cone. HCl and 570 ml of water.The reaction mass was stirred for 5min and charged the above solid (9Og). The reaction mass was stirred for 5-10min at 25-300C to get yellow colored clear liquid. pH of the reaction mass was adjusted to 6.0 to 6.5 by dropwise addition of dilute(concentrated aq ammonia solution was diluted with equal volume of water) aq.0 ammonia solution. The reaction mass was stirred for 30min and filtered under vacuum. The wet solid was dried in the oven at 70-750C to get 88g of paliperidoneHCl.Above solid was transferred taken into a IL RB flask containing 570 ml of methanol.5 The suspension was stirred for 30min at 25-3O0C, filtered under vacuum and dried in the oven at 70-750C for Ih to get 85 g pure paliperidone HCl. HPLC purity is > 99.80%.Above paliperidone HCl salt (85.0 g) and 2280 ml of water were suspended in a RB0 flask at 25-300C. pH was adjusted to 8.5 to 9.0 by adding aq. potassium carbonate solution (prepared from 57 g of potassium carbonate and 570 ml of water). The resultant cream-colored suspension was stirred for 30 min at 25-300C and filtered under vacuum. The wet cake was washed with 1500ml of water followed by 300ml of methanol. The wet cake was triturated with 450 ml of methanol for 30 min and filtered. Paliperidone was dried in vacuum oven at 65-70C for 4h to afford 59 g (34.33%) of pure paliperidone. Purity by HPLC is > 99.8%. 1H-NMR (CDCl3): 1.75 (m, 2H, aliphatic-H), 1.95 (m, IH, aliphatic-H), 2.15 (m, 5H, aliphatic-H), 2.24 -2.40 (m, 5H, aliphatic-H), 2.56 (t, 2H, -CH2-, J = 6.84 Hz), 2.76 (t, 2H, -CH2-, J = 7.82 Hz), 3.09 (m, IH, aliphatic-H), 3.18 (d, 2H, aliphatic-H, J =11.72 Hz), 3.92 (m, 2H, aliphatic-H), 4.15 (s, IH, -OH, D2O exchangeable), 4.50 (dd, IH, aliphatic-H J = 3.91 Hz), 7.07 (m, IH, aromatic-H), 7.23 (m, IH aromatic-H), 7.70 (dd, IH, aromatic-H, J= 2.93 Hz).

In the field of chemistry, the synthetic routes of compounds are constantly being developed and updated. I will also mention this compound in other articles. 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; NATCO PHARMA LIMITED; WO2009/10988; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 130049-82-0, The major producers of chemicals have been the Europe, Japan and China. Due to the growing call for a cleaner, greener environment, people will have to find innovative ways to maintain their relevance. Here is a compound 130049-82-0, name is 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one. This compound has unique chemical properties. The synthetic route is as follows.

To a 250 ml three-necked flask, ethanol (100 mL), HW03603-4 (24.2 g, 46 mmol) and 6N HCl or trifluoroacetic acid (50 mL) were sequentially added at room temperature. Then, the reaction system was stirred at room temperature overnight. Depressurization to give a white solid HW03603-5 (about 20g,Yield 100%). Used directly in the next step. Preparation of target compound HW03603: Steps 1-4 of Reference Example 1 Preparation of target compound HW03603: Steps 1-4 of Reference Example 1Add to the 100 ml three-necked bottle at room temperature:Methanol (50 mL), HW03603-5 (4.6 g, 10.8 mmol),HW036-6 (2.62g, 10.8mmol)And N,N-diisopropylethylamine (4.2 g, 32.4 mmol).Then, the reaction system was heated to reflux and stirred overnight.The solvent was evaporated to dryness The organic phase was combined, washed with saturated brine, dried over anhydrous sodium sulfate and filtered.Depressurization to obtain a solid,Recrystallization from methanol gave a white solid HW03603 (3.35 g, yield 49%).

While traditionally a conservative industry, chemical producers will need to modernize their PR strategies to stay relevant.we look forward to future research findings about 130049-82-0, 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one.

Reference:
Patent; Shanghai Kezhen Pharmaceutical Technology Co., Ltd.; Dong Huanwen; Zhang Lurong; (55 pag.)CN109748914; (2019); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia