Tag: M.W=400-500

Reference of 147118-40-9, With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.147118-40-9, name is Rosuvastatin methyl ester, molecular formula is C23H30FN3O6S, molecular weight is 495.56, as common compound, the synthetic route is as follows.

The fraction obtained in preparative HPLC is evaporated under reduced pressure (ca 200 mbar) to 50 ml and coled in freezer (ca -20°C) for 3 days. The suspension is filtered. The obtained crystals are dried under vacuum at 40 °C for 5 hours yielding 0,57 g of dry product, containing ca 11 percent of enantiomer; The fraction obtained in preparative HPLC is evaporated under reduced pressure (ca 200 mbar) to 50 ml and coled in freezer (ca -20°C) for 3 days. The suspension is filtered. The obtained crystals are dried under vacuum at 40 °C for 5 hours yielding 0,57 g of dry product, containing ca 11 percent of enantiomer; The filtrate of previous step is evaporated under reduced pressure and dried under vacuum at 40 °C for 5 hours yielding 0,43 g of dry product, containing less than 0,1percent of 3S, 5R enantiomer. The product is enantimerically pure MER having 99,9 percent enantiomeric purity, , as shown on Fig.4

The chemical industry reduces the impact on the environment during synthesis 147118-40-9, I believe this compound will play a more active role in future production and life.

Reference:
Patent; LEK Pharmaceuticals d.d.; EP2022784; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 147118-40-9 ,Some common heterocyclic compound, 147118-40-9, molecular formula is C23H30FN3O6S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

Previous to give 62 g (0.125 mol) of crystalline product was added 860 ml of ethanol, 140 ml 1N-NaOH was stirred at 25 degrees for 1 hour. At 35-40 ° ethanol was removed by vacuum distillation, by 1 l methyl t-butyl ether and extracted twice. With an appropriate amount of the aqueous layer was filtered through Celite and activated carbon, with a small amount of water dissolved calcium acetate was added to the filtrate, stirred for 2 hours at 25 °, filtered washed with water, and dried to give 52.9 g (84.5percent theoretical yield) rosuvastatin statin calcium.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,147118-40-9, its application will become more common.

Reference:
Patent; Anhui Menovo Pharmaceuticals Co., Ltd; Fan, qijiao; Wang, bangfeng; Shi, jianxiang; (9 pag.)CN105461636; (2016); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.1421372-67-9, name is N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine, molecular formula is C25H29N7O3, molecular weight is 475.5429, as common compound, the synthetic route is as follows.COA of Formula: C25H29N7O3

A 125 ml autoclave was taken, and after replacing nitrogen three times, a compound F (1.50 g, 3.15 mmol) and a Raney nickel catalyst (0.70 g) were added and dissolved in ethyl acetate (30 ml), and the hydrogen was replaced twice and then charged with 2.0 MPa of hydrogen.The temperature was raised to 40 C to stir the reaction.Filter off and wash the filter cake twice with ethyl acetate (10 ml x 2).The filtrate was concentrated under reduced pressure at 40 C to give a dark green solid: 1.36 g.The molar yield was 96.90%.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,1421372-67-9, N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine, and friends who are interested can also refer to it.

Reference:
Patent; Zhejiang Jiuzhou Pharmaceutical Technology Co., Ltd.; Zhang Xianyi; Jiang Youyu; Wang Chong; Gao Hongjun; Che Daqing; (10 pag.)CN108129342; (2018); A;,
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. 799842-07-2, name is N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide. A new synthetic method of this compound is introduced below., category: pyrimidines

General procedure: Aq 1 M NaOH (9 mL, 1.5 equiv) was added to a stirred MeOH (20mL) solution of the appropriate aromatic thiol (7.2 mmol, 1.2equiv). The solution was stirred at r.t. for 15 min and then the heterocyclicalkyl bromide 2 or 3 (6 mmol, 1 equiv) was added. When rosuvastatin moiety bromides 2 were used, THF (10 mL) was also added to the mixture to improve solubility. After 18 h, the solvent was evaporated, the residue was dissolved in CH2Cl2 (50 mL), and washed with H2O (100 mL). The aqueous phase was additionally extracted with CH2Cl2 (2 × 25 mL). The combined organic phases were dried (MgSO4) and the solvent was evaporated. The residuewas recrystallized and the isolated product was dried in vacuumovernight at 60 C below 50 mbar to give the pure sulfide heterocyclic precursor 4 or 5 in 75-97% yield.

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, 799842-07-2, N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide.

Reference:
Article; Fabris, Jan; ?asar, Zdenko; Smilovi?, Ivana Gazi?; ?rnugelj, Martin; Synthesis; vol. 46; 17; (2014); p. 2333 – 2346;,
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Pyrimidine – Wikipedia

Related Products of 1421372-67-9, 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 1421372-67-9 as follows.

Compound 7 from the previous step, iron (12.8 g), and ammonium chloride (1.42 g) were heated in ethanol (100 mL) and water (30 mL) at reflux for 1.5 h. The mixture was cooled and filtered. The solids were rinsed with DCM. The filtrate was concentrated to approximately 20 mL and NaOH (1 N, 50 mL) was added. The gray precipitates were filtered off and rinsed with DCM. The mixture was partitioned and the organic layer was washed with NH4OH (50 mL), brine (100 mL) and concentrated to a brown foam (compound 8, 12 g).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,1421372-67-9, its application will become more common.

Reference:
Patent; NEUFORM PHARMACEUTICALS, INC.; CHAORAN, Huang; CHANGFU, Cheng; (85 pag.)WO2017/117070; (2017); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

With the rapid development and complex challenges of chemical substances, the synthesis of new drugs is usually one of the most effective ways to increase yield.799842-07-2, name is N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, molecular formula is C16H19BrFN3O2S, molecular weight is 416.31, as common compound, the synthetic route is as follows.Product Details of 799842-07-2

b) from PMDBR (Kornblum oxidation): NaHC03 (220 mg, 2.6 mmol, 1.1 equiv.) and Nal (10 mol %) were dissolved in DMSO (5 mL) and cooled to 20 C. Then, PMDBR (1.0 g, 2,4 mmol, 1 equiv.) in DMSO (5 mL) was slowly added via a syringe pump during 1 h and reaction was left to stir for 24 h. Reaction mixture was then warmed to 70 C and Ac20 (5 equiv.) was added dropwise. Reaction was left to stir for additional 3 hours. After cooling on an ice bath, water (20 mL) was slowly added and precipitate was filtered off to afford 0.78 g (93 %) of PMDCHO.1H NMR (CDCI3): delta 1.30 (6H, d, J = 6.7 Hz), 3.53 (3H, s), 3.62 (3H, s), 3.99 (1 H, sep, J = 6.7 Hz), 7.21 (2H, m), 7.61 (2H, m), 9.95 (1 H, s) ppm. 13C NMR (CDCI3): 521.6, 31.9, 33.0, 42.4, 115.8, 116.0, 119.5, 132.5, 132.6, 158.7, 163.1 , 165.6, 169.7, 178.9, 190.4 ppm.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,799842-07-2, N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, and friends who are interested can also refer to it.

Reference:
Patent; LEK PHARMACEUTICALS D.D.; CASAR, Zdenko; STERK, Damjan; JUKIC, Marko; WO2012/13325; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 1421372-67-9, 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. 1421372-67-9, name is N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine. A new synthetic method of this compound is introduced below.

Under nitrogen protection,928 ml of methanol was added to a 2 L four-necked flask,Then, 92.8 g of the compound represented by the formula (III)Stirring,18.6g was added Raney nickel (water-wet product)8 at atmospheric pressure under hydrogenation,Reaction temperature 25 ,The reaction was carried out for 6 hours.Filtered by rotary evaporation to yield 82.6 g of gray solid, yield: 95.0%

At the same time, in my other blogs, there are other synthetic methods of this type of compound,1421372-67-9, N1-(2-(Dimethylamino)ethyl)-5-methoxy-N1-methyl-N4-(4-(1-methyl-1H-indol-3-yl)pyrimidin-2-yl)-2-nitrobenzene-1,4-diamine, and friends who are interested can also refer to it.

Reference:
Patent; Luoxin Bio-technology (Shanghai) Co., Ltd.; Shandong Luoxin Pharmaceutical Group Co., Ltd.; Pan Longgang; Cai Zhengyuan; Li Guoliang; Yang Wenqian; Wang Tielin; (10 pag.)CN107188888; (2017); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 799842-07-2 , The common heterocyclic compound, 799842-07-2, name is N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide, molecular formula is C16H19BrFN3O2S, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc., below Introduce a new synthetic route.

General procedure: Aq 1 M NaOH (9 mL, 1.5 equiv) was added to a stirred MeOH (20mL) solution of the appropriate aromatic thiol (7.2 mmol, 1.2equiv). The solution was stirred at r.t. for 15 min and then the heterocyclicalkyl bromide 2 or 3 (6 mmol, 1 equiv) was added. When rosuvastatin moiety bromides 2 were used, THF (10 mL) was also added to the mixture to improve solubility. After 18 h, the solvent was evaporated, the residue was dissolved in CH2Cl2 (50 mL), and washed with H2O (100 mL). The aqueous phase was additionally extracted with CH2Cl2 (2 × 25 mL). The combined organic phases were dried (MgSO4) and the solvent was evaporated. The residuewas recrystallized and the isolated product was dried in vacuumovernight at 60 C below 50 mbar to give the pure sulfide heterocyclic precursor 4 or 5 in 75-97% yield.

The synthetic route of 799842-07-2 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Fabris, Jan; ?asar, Zdenko; Smilovi?, Ivana Gazi?; ?rnugelj, Martin; Synthesis; vol. 46; 17; (2014); p. 2333 – 2346;,
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. 1152107-25-9, name is Gsk-1322322. A new synthetic method of this compound is introduced below., Recommanded Product: Gsk-1322322

Example 8 [(2R)-2-(Cyclopentylmethyl)-3-(2-{5-fluoro-6-[(9aS)-hexahydropyrazino [2,1 -c] [1 ,4] oxazin- 8(1 H)-yl]-2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl] hydroxyl formamide dimethanesulphonate. Crystalline [(2R)-2-(Cyclopentylmethyl)-3-(2-{5-fluoro-6-[(9aS)- hexahydropyrazino[2, 1 -c][1 ,4]oxazin-8(1 H)-yl]-2-methyl-4-pyrimidinyl}hydrazino)-3- oxopropyl]hydroxyformamide (100 mg) was dissolved in ethyl acetate (10 ml_). Methanesulphonic acid (40.1 mg) in ethyl acetate (ca. 10 ml.) was prepared. The methanesulphonic acid solution was added dropwise to the solution of freebase in ethyl acetate. A precipitate was formed. The slurry was stirred and aged overnight. The precipitate’s crystallinity was verified by polarized light microscopy. The precipitate and supernatant were separated by filtration. The solids were then vacuum dried. The resulting solid was analytically characterized and found to be Form 1 of the dimethanesulphonate salt of [(2R)-2-(Cyclopentylmethyl)-3-(2-{5-fluoro-6-[(9aS)- hexahydropyrazino[2, 1 -c][1 ,4]oxazin-8(1 H)-yl]-2-methyl-4-pyrimidinyl}hydrazino)-3- oxopropyl]hydroxyformamide by XRPD (see Figure 7). X-Rav Powder Diffraction of r(2R)-2-(Cvclopentylmethyl)-3-(2-f5-fluoro-6-r(9aS)- hexahvdropyrazinor2,1-ciri,41oxazin-8(1 H)-vn-2-methyl-4-pyrimidinyl>hvdrazino)-3- oxopropyUhydroxyformamide dimethanesulphonate The XRPD pattern for polymorphic Form 1 of [(2R)-2-(Cyclopentylmethyl)-3-(2-{5- fluoro-6-[(9aS)-hexahydropyrazino[2, 1 -c][1 ,4]oxazin-8(1 H)-yl]-2-methyl-4- pyrimidinyl}hydrazino)-3-oxopropyl]hydroxyformamide dimethanesulphonate is presented in Figure 7. The X-ray powder diffractogram was collected with a diffraction system utilizing copper Ka radiation, automated divergent slits, nickel Kappabeta filter, and multiple strip detector. Sample presentation consisted of a thin powder layer mounted on a silicon zero background wafer. Thermal Analysis Based on differential scanning calorimetry (DSC) seen in Figure 8 and thermogravimetric analysis (TGA) seen in Figure 9, polymorphic Form 1 of [(2R)-2- (cyclopentylmethyl)-3-(2-{5-fluoro-6-[(9aS)-hexahydropyrazino[2,1 -c][1 ,4]oxazin-8(1 h)-yl]- 2-methyl-4-pyrimidinyl}hydrazino)-3-oxopropyl]hydroxyformamide dimethanesulphonate decomposes at ca. 180 to 185 C under nitrogen.

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, 1152107-25-9, Gsk-1322322.

Reference:
Patent; GLAXOSMITHKLINE INTELLECTUAL PROPERTY (NO. 2) LIMITED; AUBART, Kelly, Marshall; GILLIAN, Jason, Michael; QIN, Donghui; MCKEOWN, Robert, Rahn; WILLIAMS, Glenn, R.; WO2013/82388; (2013); A1;,
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. 799842-07-2, name is N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide. A new synthetic method of this compound is introduced below., Recommanded Product: 799842-07-2

General procedure: Aq 1 M NaOH (9 mL, 1.5 equiv) was added to a stirred MeOH (20mL) solution of the appropriate aromatic thiol (7.2 mmol, 1.2equiv). The solution was stirred at r.t. for 15 min and then the heterocyclicalkyl bromide 2 or 3 (6 mmol, 1 equiv) was added. When rosuvastatin moiety bromides 2 were used, THF (10 mL) was also added to the mixture to improve solubility. After 18 h, the solvent was evaporated, the residue was dissolved in CH2Cl2 (50 mL), and washed with H2O (100 mL). The aqueous phase was additionally extracted with CH2Cl2 (2 × 25 mL). The combined organic phases were dried (MgSO4) and the solvent was evaporated. The residuewas recrystallized and the isolated product was dried in vacuumovernight at 60 C below 50 mbar to give the pure sulfide heterocyclic precursor 4 or 5 in 75-97% yield.

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, 799842-07-2, N-[5-Bromomethyl-4-(4-fluorophenyl)-6-isopropylpyrimidine-2-yl]-N-methylmethane sulfonamide.

Reference:
Article; Fabris, Jan; ?asar, Zdenko; Smilovi?, Ivana Gazi?; ?rnugelj, Martin; Synthesis; vol. 46; 17; (2014); p. 2333 – 2346;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia