Day: March 18, 2021

Electric Literature of 130049-82-0, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 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, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

Example-6 Preparation of Paliperidone (One Pot Process) To the solution of 6-fluoro-3-(piperidin-4-yl)benzo[d]isoxazole (formula-8) (10.0 grams) in methanol (50 ml), 3-(2-chloroethyl)-9-hydroxy-2-methyl-6,7,8,9-tetrahydro-4H-pyrido[1,2-a]pyrimidin-4-one (formula-7) (11 grams) and diisopropyl ethyl amine (9 grams) were added. The reaction mixture heated to 65-70 C. and stirred for 24 hrs at the same temperature. The reaction mixture was cooled. Dichloromethane (100 ml) and sodium borohydride (0.086 grams) were added to it and stirred for 60 minutes at the same temperature. The solvent was distilled off under reduced temperature. Methanol was added to the residue and heated to reflux for 30 min. The reaction mixture was cooled to 20 C. and stirred for 1 hour. Filtered the solid precipitated. Washed the solid with chilled methanol and dried the compound. Yield: 12.5 grams.

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; MSN LABORATORIES LIMITED; US2011/293889; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 94741-69-2, name is 4-Amino-2-chloro-5-pyrimidinecarbonitrile, molecular formula is C5H3ClN4, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. Product Details of 94741-69-2

EXAMPLE 94; A mixture of 2-chloro-5-cyano-6-amino pyrimdine (0,1 g), 3,4,5-trimethoxy aniline (0.71 mmol), palladium(II) acetate (1 mol%), 9.9-dimethyI-4,5- bis(diphenylphosphino)xanthene (1.5 mol%) and cesium carbonate (L29 mmol) in dioxane (2 mL) was heated in a microwave at 1500C for 20 minutes, cooled, filtered through diatomaceous earth (Celite) and concentrated.. The concentrate was purified by HPLC on a C18 column with acetonitrile/water/0.1% trifluoroacetic acid, 1H NMR (DMSOd6) delta 9 35 (br s, IH), 8.15 (s, IH), 6.45 (s, 2H), 5,5 (s, 2H), 3.73 (s, 6H), 3.70 (s, 3H).

With the rapid development of chemical substances, we look forward to future research findings about 94741-69-2.

Reference:
Patent; ABBOTT LABORATORIES; WO2007/140233; (2007); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 26452-81-3, 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 26452-81-3 as follows.

To a RBF equipped with a reflux condenser containing DME (42.9 mL), EtOH(5.36 mL) was added 4-chloro-6-methoxypyrimidine (1.55 g, 10.72 mmol), 4-methyl-2-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline (2.5 g, 10.72 mmol) and 2 M aqNa2CO3 (5.36 mL, 10.72 mmol). The mixture was purged with Ar for 10 mm thenPdC12(dppf)-CH2Cl2Adduct (0.876 g, 1.072 mmol) was added and the reaction mixtureheated at 90 ¡ãC. After 2 h, the reaction was diluted with water and extracted with EtOAc. The organic layer washed with brine and concentrated to give a brown oil. The crude product was purified by normal phase chromatography using heptane and EtOAc as eluents to give 2-(6-methoxypyrimidin-4-yl)-4-methylaniline (670 mg, 29percent) as a solid.MS(ESI)m/z: 216.1 (M+H). ?HNMR(500MHz, CDC13-d) oe 8.79 (d, J1.1 Hz, 1H),7.33 (d, J1.4 Hz, 1H), 7.08 – 7.01 (m, 2H), 6.67 (d, J8.3 Hz, 1H), 5.68 (br. s., 2H), 4.03 (s, 3H), 2.29 (s, 3H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,26452-81-3, its application will become more common.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; CORTE, James R.; DE LUCCA, Indawati; FANG, Tianan; YANG, Wu; WANG, Yufeng; DILGER, Andrew K.; PABBISETTY, Kumar Balashanmuga; EWING, William R.; ZHU, Yeheng; WEXLER, Ruth R.; PINTO, Donald J. P.; ORWAT, Michael J.; SMITH, Leon M. II; WO2015/116886; (2015); 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.13162-26-0, name is 2,4-Dichloro-6-methyl-5-nitropyrimidine, molecular formula is C5H3Cl2N3O2, molecular weight is 208, as common compound, the synthetic route is as follows.Recommanded Product: 13162-26-0

To a solution of 2,4-dichloro-6-methyl-5-nitropyrimidine (7 g, 34 mmol) and CH3COOK (9.8 g, 100 mmol) in MeOH (150 mL) was added Pd C (3 g). The mixture was stirred at H2 atmosphere for overnight. The reaction mixture was filtered, and the solvent was concentrated under reduced pressure to give the product 4-methylpyrimidin-5 -amine (1.5 g, 43%), which was used to next step without furthermore purification. ‘HNMR: MeOD 400MHz ? 8.28(s, 1H), 8.04(s, 1H), 2.3 l(s, 3H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,13162-26-0, 2,4-Dichloro-6-methyl-5-nitropyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; ARRAY BIOPHARMA INC.; GENENTECH, INC.; SKELTON, Nicholas; GRADL, Stefan; BLAKE, James F.; GRAHAM, James M.; GUNAWARDANA, Indrani W.; HENTEMANN, Martin; MARLOW, Allison L.; TANG, Tony P.; WO2013/78254; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 955368-90-8, 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. 955368-90-8, name is 2-Allyl-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidin-3(2H)-one. A new synthetic method of this compound is introduced below.

Cuprous iodide (42.82 mg, 224.85 mumol), N,N’-dimethyllethylenediamine (22.20 mg, 251.83 mumol, 27.07 muL) and potassium carbonate (42.88 mg, 310.29 mumol) were added separately into the compound I1 (49.98 mg, 224.85 mumol) and 72-1 (56.00 mg, 224.85 mumol) in dioxane (3 mL) solution, the reaction mixture was stirred at 95C for 1 hour under nitrogen atmosphere, then concentrated and added 20 mL ammonia, extracted by EA 150 mL (50 mLx3) and washed by saturated brine 30 mL, dried over anhydrous sodium sulfate, then filtered to give the crude compound. The crude product was purified by silica gel column chromatography (PE/EA=3/1) 72-1. MS m/z: 391.0 [M+H]+

At the same time, in my other blogs, there are other synthetic methods of this type of compound,955368-90-8, 2-Allyl-6-(methylthio)-1H-pyrazolo[3,4-d]pyrimidin-3(2H)-one, and friends who are interested can also refer to it.

Reference:
Patent; Shijiazhuang Sagacity New Drug Development Co., Ltd.; QIAN, Wenyuan; YANG, Chundao; LI, Zhengwei; LI, Jie; LI, Jian; CHEN, Shuhui; (137 pag.)EP3572413; (2019); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 4316-93-2, name is 4,6-Dichloro-5-nitropyrimidine, molecular formula is C4HCl2N3O2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below. COA of Formula: C4HCl2N3O2

To a 500 ml three neck round bottomed flask, 4,6-dichloro-5-nitropyrimidine (25 g, 129 mmole) was dissolved in CH2Cl2 (300 ml) and cooled to 0 C. To this, dibenzylamine (49.6 ml, 257.7 mmole) was added dropwise by maintaining temperature at 0 C. and stirred for 1.5 h at same temperature. The reaction mixture was diluted with CH2Cl2 and washed with water. The combined organic layer was dried over sodium sulphate and concentrated to give the crude product which was purified by trituration with n-pentane to yield 38 g of N,N-dibenzyl-6-chloro-5-nitropyrimidin-4-amine (83.06% yield).

With the rapid development of chemical substances, we look forward to future research findings about 4316-93-2.

Reference:
Patent; Principia Biopharma Inc.; Owens, Timothy D.; US2014/142099; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 183438-24-6 ,Some common heterocyclic compound, 183438-24-6, molecular formula is C4H2BrIN2, 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.

Example 29A 3-[(5-bromopyrimidin-2-yl)oxy]quinuclidine 3-Hydroxy quinuclidine (Aldrich, 254 mg, 2 mmol) in tetrahydrofuran (10 ml) was treated with potassium tert-butoxide (Aldrich, 224 mg, 2 mmol) at ambient temperature for 1 hour. The mixture was treated with 2-iodo-5-bromo-pyrimidine (TCl, 568 mg, 2 mmol), stirred at room temperature for 1 hour, treated with water (5 mL), and extracted with chloroform:isopropyl alcohol (10:1) (3*20 mL). The extracts were combined and concentrated. The title compound was purified by chromatography (SiO2, CH2Cl2: MeOH: NH3H2O, 90:10:2, Rf. 0.20) as oil (210 mg, yield, 71%). 1H NMR (MeOH-d4, 300 MHz) delta 1.56-1.68 (m, 1H), 1.70-1.90 (m, 2H), 2.05-2.30 (m, 2H), 2.79-3.06 (m, 5H), 3.40-3.48 (m, 1H), 5.11 (m, 1H), 8.64 (s, 2H) ppm. MS (DCl/NH3) m/z 284 (M+H)+, 286 (M+H)+.

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,183438-24-6, its application will become more common.

Reference:
Patent; Abbott Laboratories; US2005/137226; (2005); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 871254-61-4, Adding some certain compound to certain chemical reactions, such as: 871254-61-4, name is 2,4-Dichloropyrimidine-5-carbaldehyde,molecular formula is C5H2Cl2N2O, 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 871254-61-4.

To a flask containing MeOH (24.0 mL), was added 2,4- dichloropyrimidine-5-carbaldehyde (1.5159 g, 1.0 equiv.), PPTS (215.0 mg, 0.1 equiv.) and trimethyl orthoformate (6.0 mL). The reaction mixture was stirred at 65 C for 14 h, cooled to rt and concentrated. The resulting residue was purified via column chromatography to yield the title compound as an oil (1.4361 g, 75% yield). NMR (400 MHz, Chloroform-^ d 8.73 (s, 1H), 5.54 (s, 1H), 3.38 (s, 7H). LC-MS: m/z 223, 225 [M+H]+.

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. 871254-61-4, 2,4-Dichloropyrimidine-5-carbaldehyde, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; AGIOS PHARMACEUTICALS, INC.; KONTEATIS, Zenon D.; LI, Mingzong; LIU, Peng; MEDEIROS, Matthew; REZNIK, Samuel K.; SUI, Zhihua; TRAVINS, Jeremy M.; POPOVICI-MULLER, Janeta; ZHOU, Shubao; MA, Guangning; (298 pag.)WO2019/191470; (2019); 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. 4359-87-9, name is 2,4,6-Trichloro-5-nitropyrimidine, the common compound, a new synthetic route is introduced below. SDS of cas: 4359-87-9

PREPARATION 112 2-Chloro-6-morpholin-4-yl-9-(tetrahydro-2W-pyran-4-yl)-7,9-dihydro-8H-purin-8- o a) 4-(2,6-Dichloro-5-nitropyrimidin-4-yl)morpholine A solution of morpholine (362 mg, 4.16 mmol) and triethylamine (0.58 mL, 4.16 mmol) in methylene chloride (11 mL) was added dropwise to a cooled (0 C) solution of 2,4,6- trichloro-5-nitropyrimidine (950 mg, 4.16 mmol) in methylene chloride (25 mL) and the resulting mixture was stirred overnight at ambient temperature. Solvent was then evaporated and the crude was purified by flash cromatography (3:1 hexanes/ethyl acetate) to yield the title compound (780 mg, 67%) as a yellow solid. LRMS (m/z): 279 (M+1)+ 1H NMR (300 MHz, CDCI3) delta ppm 3.77 (m, 4H), 3.50 – 3.67 (m, 4H).

The synthetic route of 4359-87-9 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ALMIRALL, S.A.; EASTWOOD, Paul Robert; GONZALEZ RODRIGUEZ, Jacob; GOMEZ CASTILLO, Elena; BACH TANA, Jordi; WO2011/157397; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 374930-88-8, As we all know, there are many different methods for the synthesis of a compound, and people can choose the synthesis method that suits their own laboratory according to the actual situation. 374930-88-8, name is tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate, molecular formula is C13H19BrN4O2, The compound is widely used in many fields, so it is necessary to find a new synthetic route. The downstream synthesis method of this compound is introduced below.

A mixture of tert-butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate (684 mg, 2.0 mmol), 4-fluorophenol (1.1 g, 5.0 mmol), copper (650 mg, 10.0 mmol) and Cs2CO3 (6.5 g, 20.0 mmol) in pyridine (15 mL) was heated at 120 C. for 12 h. The mixture was cooled to RT, diluted with ethyl acetate (200 mL) and filtered. The filtrate was concentrated under reduced pressure, and the residue was purified by silica gel column chromatography (petroleum ether/ethyl acetate=20/1) to afford the title compound (200 mg, 27%) as a brown solid. MS (ES+) C19H23FN4O3 requires: 374. found: 319 [M-56+1]+.

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 374930-88-8, tert-Butyl 4-(5-bromopyrimidin-2-yl)piperazine-1-carboxylate.

Reference:
Patent; Hodous, Brian L.; Kim, Joseph L.; Wilson, Kevin J.; Wilson, Douglas; Zhang, Yulian; US2015/111887; (2015); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia