Day: July 2, 2021

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.69034-12-4, name is 2-Chloro-5-(trifluoromethyl)pyrimidine, molecular formula is C5H2ClF3N2, molecular weight is 182.531, as common compound, the synthetic route is as follows.Recommanded Product: 2-Chloro-5-(trifluoromethyl)pyrimidine

A mixture of l-((lr,4r)-4-((2-fluoro-4- (methylsulfonyl)phenoxy)methyl)cyclohexyl)piperazine dihydrochloride (29 mg, 0.065 mmol), 2-chloro-5-(trifluoromethyl)pyrimidine (16 mg, 0.085 mmol) and triethylamine (34 mu, 0.262 mmol) in IPA (1.5 mL) was heated at 130 C for 40 min under microwave irradiation. The mixture was cooled down. The solid precipitate was collected, washed with IPA and dried to give the title compound (30 mg, 89.2%). Exact mass calculated for C23H28F4N4O3S: 516.2, found: LCMS m/z = 517.2 [M+H]+; lU NMR (400 MHz, CDC13) delta ppm 1.10-1.20 (m, 2H),1.35-1.45 (m, 2H), 1.78-1.90 (m, 1H), 1.98-2.10 (m, 4H), 2.40-2.50 (m, 1H), 2.65-2.75 (m, 4H), 3.03 (s, 3H), 3.85-4.05 (m, 4H), 3.90 (d, J = 6.2 Hz, 2H), 7.05 (t, J = 8.0 Hz, 1H), 7.62-7.69 (m, 2H), 8.49 (s, 2H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,69034-12-4, 2-Chloro-5-(trifluoromethyl)pyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; ARENA PHARMACEUTICALS, INC.; JONES, Robert M.; BUZARD, Daniel J.; HAN, Sangdon; KIM, Sun Hee; LEHMANN, Juerg; YUE, Dawei; ZHU, Xiuwen; WO2012/145361; (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. 3993-78-0, name is 2-Amino-4-chloropyrimidine, the common compound, a new synthetic route is introduced below. Product Details of 3993-78-0

NaH (1.15 g, 60% in mineral oil, 28.7 mmol) was added the mixture of 4-chloropyrimidin-2-amine (1.0 g, 7.75 mmol) and solketal (3.07 g, 23.25 mmol) in dioxane (12 mL) solution at 0 C. The temperature was elevated to 120 C for 15 h. After cooling to room temp, the solids were filtered, filtrate was concentrated and residue purified by column chromatography to give 4-((2,2-dimethyl-1,3-dioxolan-4-yl)methoxy)pyrimidin-2- amine (1.2 g, 69 %). MS (ESI) calcd for C10H15N3O3: 225.11

The synthetic route of 3993-78-0 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; SIRTRIS PHARMACEUTICALS, INC.; CASAUBON, Rebecca, L.; NARAYAN, Radha; OALMANN, Christopher; VU, Chi, B.; WO2013/59587; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 932-52-5 ,Some common heterocyclic compound, 932-52-5, molecular formula is C4H5N3O2, 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.

7 g of caustic soda (0.175 mol) diluted in 350 ml of water were added to 21.5 g of 5-aminouracil (0.17 mol). The mixture was heated at a boiling water bath until 5-aminouracil was fully dissolved. Then 32 g of 3,5-dichlorosalicylic aldehyde (0.17 mol) dissolved in 150 ml of hot ethanol were added in portions to the reaction mass at the temperature of the boiling water bath while stirring. For the purpose of quantitative transfer of aldehyde into the reaction flask, the vessel in which it was dissolved was washed with 50 ml of ethanol. A sediment of orange-red color precipitated in the flask. Then the reaction mass was stirred for 30 more minutes at the water bath and was gradually cooled down to room temperature. The obtained residue was filtered, washed with 300 ml of ethanol and dried. 600 ml of aqueous ethanol were distilled off the filtrate by means of rotary evaporator. The remaining mixture was filtered by means of glass filter to obtain 75.5 g of the target compound.

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. 932-52-5, 5-Aminopyrimidine-2,4(1H,3H)-dione, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Tets, Viktor Veniaminovich; Tets, Georgy Viktorovich; Krutikov, Viktor Iosifovich; US2013/261301; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 36315-01-2, 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. 36315-01-2, name is 2-Amino-4,6-dimethoxypyrimidine. A new synthetic method of this compound is introduced below.

In a 1 OOO mL reaction flask, 100 g of 2-sulfonyl chloride-N, N-dimethylnicotinamide (0.40 mol) 40 g of sodium cyanate (0.62 mol), 101 g of triethylamine (1.00 mol) and 125 g of acetonitrile were charged and the mixture was stirred at 25 ± 5 C for isocyanating. After 5 h, 75 g of 2-amino-4,6-dimethoxypyrimidine (0.48 mol) was added to the reaction flask and stirred for 1 h at ambient temperature (0 to 40 C). After the completion of the condensation reaction, 500 g of deionized water (about 1.5 h) was added dropwise to the reaction bottle. After dropping, the pH was adjusted to 1.0 with hydrochloric acid, After drying, 157.8 g of nicosulfuron were obtained in a yield of 92.1% and a purity of 95.7%.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,36315-01-2, 2-Amino-4,6-dimethoxypyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; Jiangsu agricultural hormone Engineering Technology Research Center Co., Ltd.; Jiangsu Hormone Research Institute Co., Ltd; Sun, Yong Hui; kong, Fan Lei; Shi, yueping; Gao, Jian Hong; Zhang, Yuan yuan; Cao, Wei; (5 pag.)CN103524493; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 153435-63-3, 2-(Tributylstannyl)pyrimidine, 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, 153435-63-3, blongs to pyrimidines compound. SDS of cas: 153435-63-3

General procedure 8Intermediates 46-50 (1 eq) was dissolved dry DMF (20ml/mmol), then CsF (2 eq), CuI (0.2 eq), [Ph3P]4Pd (0.1 eq) and the corresponding Ar2-tributylstannane (1.5 eq; prepared according to Eur. J. Org. Chem. 2003, 171 1 -1721 ) were added. The mixture was warmed at 130 C for 10 minutes (microwave), then poured in aqueous saturated solution of NH4CI and extracted with AcOEt . The organic layers were combined, dried (Na2SO4) and concentrated under vacuum; crude product was purified by silica gel column chromatography (DCM to DCM/MeOH 9/1 ). The enantiomeric purity was calculated as enantiomeric eccess (ee%) by chiral HPLC methods.According to general procedure 8 the following compounds were prepared:

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,153435-63-3, its application will become more common.

Reference:
Patent; ROTTAPHARM S.P.A.; STASI, Luigi, Piero; ROVATI, Lucio; WO2011/6960; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 7461-50-9, 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. 7461-50-9, name is 2-Chloropyrimidin-4-amine. A new synthetic method of this compound is introduced below.

To a reaction vessel was added 2-chloropyrimidin-4-amine (1.0 g, 8.0 mmol, 1.1 equiv), 3,3- dimethylpiperidin-4-ol (1.0 g, 9.0 mmol, 1.0 equiv), triethylamine (3.0 g, 30 mmol, 4.0 equiv), and 2-propanol (5 mL). The sealed reaction vessel was heated under microwave irradiation at 150 C for 45 min. The reaction mixture was cooled to room temperature, diluted with saturated aqueous sodium bicarbonate and extracted with dichloromethane. The organic layer was dried over magnesium sulfate, filtered and concentrated in vacuo to afford l-(4-aminopyrimidin-2-yl)-3,3- dimethyl-piperdin-4-ol (1.24 g, 70%). LCMS (ESI): [M+H]+ = 223.2; lH NMR (300 MHz, DMSO-d6) delta 7.69 (d, J= 5.6 Hz, 1H), 6.28 (s, 2H), 5.64 (d, J= 5.6 Hz, 1H), 4.55 (d, J= 4.7 Hz, 1H), 4.33 – 4.22 (m, 1H), 4.02 (dd, J= 12.8, 1.7 Hz, 1H), 3.25 (dd, J= 9.4, 4.6 Hz, 1H), 3.08 – 2.96 (m, 1H), 2.75 (d, J= 13.0 Hz, 1H), 1.66 – 1.54 (m, 1H), 1.47 – 1.35 (m, 1H), 0.87 (s, 3H), 0.74 (s, 3 H).

At the same time, in my other blogs, there are other synthetic methods of this type of compound,7461-50-9, 2-Chloropyrimidin-4-amine, and friends who are interested can also refer to it.

Reference:
Patent; GENENTECH, INC.; BRYAN, Marian C.; CHAN, Bryan; DIEDERICH, Francois; DOTSON, Jennafer; HANAN, Emily; HEFFRON, Timothy; LAINCHBURY, Michael; HEALD, Robert; SEWARD, Eileen M.; WO2014/210354; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 126728-20-9, 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. 126728-20-9, name is 2,4-Dichloropyrido[2,3-d]pyrimidine, molecular formula is C7H3Cl2N3, 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.

General procedure: A mixture of 5 (5.0 mmol), the respective amine (12 mmol), equimolecular amounts of triethylamine, and ethanol (15 mL) was heated at 70 C for 5 h with stirring. The solvent was removed under vacuum and the residue was dissolved in water (30 mL); the mixture was extracted with chloroform (3 × 25 mL) and the organic extracts were dried over anhydrous sodium sulfate and the solvent was removed in vacuum. For compounds 6t-y the resulting solid was purified by recrystallization as indicated in Table 1. For compounds 6z-ai the residual material isolated after removal of the solvent was washed with 5% HCl (25 mL) and the resulting solid was isolated and purified as indicated in Table 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 126728-20-9, 2,4-Dichloropyrido[2,3-d]pyrimidine.

Reference:
Article; Font, Maria; Gonzalez, Alvaro; Palop, Juan Antonio; Sanmartin, Carmen; European Journal of Medicinal Chemistry; vol. 46; 9; (2011); p. 3887 – 3899;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 93416-51-4, 2,4,6-Trichloropyrimidine-5-carboxylic acid, 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, Recommanded Product: 2,4,6-Trichloropyrimidine-5-carboxylic acid, blongs to pyrimidines compound. Recommanded Product: 2,4,6-Trichloropyrimidine-5-carboxylic acid

(1) A N,N-dimethylformamide solution 6 ml of 3-chloro-4-methoxybenzylamine 1.51 g and triethylamine 2.46 g is dropped over a period of 25 minutes under ice cooling a solution of 5-carboxy-2,4,6-trichloropyrimidine (prepared in Example 318(1)) 2.00 g in N,N-dimethylformamide 12 ml, and the mixture is further stirred for 90 minutes. The reaction mixture is diluted with a 10% aqueous citric acid solution and extracted with ethyl acetate. The combined extract is washed with water and an aqueous sodium chloride solution, dried over anhydrous sodium sulfate and concentrated in vacuo to give 4-(3-chloro-4-methoxybenzylamino)-2,6-dichloropyrimidine-5-carboxylic acid as a pale brown crystalline powder 2.92 g. mp 144-151 C.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,93416-51-4, 2,4,6-Trichloropyrimidine-5-carboxylic acid, and friends who are interested can also refer to it.

Reference:
Patent; Yamada, Koichiro; Matsuki, Kenji; Omori, Kenji; Kikkawa, Kohei; US2004/142930; (2004); 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.56844-12-3, name is 6-Bromo-4-chlorothieno[2,3-d]pyrimidine, molecular formula is C6H2BrClN2S, molecular weight is 249.52, as common compound, the synthetic route is as follows.category: pyrimidines

General procedure: Compound 1 (1.00 g, 4.01 mmol) was mixed with the benzylamine (2-3 eq.) and i-PrOH (2-10 mL) and agitated at 80 C for 1-50 h, under nitrogen atmosphere. Then the mixture was cooled to rt, concentrated in vacuo, diluted with water (50 mL) and diethyl ether (100 mL) or EtOAc (100 mL). After phase separation, the water phase was extracted with more diethyl ether (2×50 mL) or EtOAc (2×50 mL). The combined organic phases were washed with saturated aq NaCl solution (25-50 mL), dried over anhydrous Na2SO4, filtered and concentrated in vacuo. The crude oil was purified by drying under reduced pressure to constant weight, by silica-gel column chromatography or crystallized as specified for each individual compound.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,56844-12-3, 6-Bromo-4-chlorothieno[2,3-d]pyrimidine, and friends who are interested can also refer to it.

Reference:
Article; Bugge, Steffen; Moen, Ingri Ullestad; Kragseth Sylte, Kent-Ove; Sundby, Eirik; Hoff, Bard Helge; European Journal of Medicinal Chemistry; vol. 94; (2015); p. 175 – 194;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 10070-92-5 ,Some common heterocyclic compound, 10070-92-5, molecular formula is C5H4N2O, 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.

To a solution of pyrimidine-5-carbaldehyde (0.300 g, 2.77 mmol) in methanol (6 mL), sodium borohydride (0.158g, 4.16 mmol) was added at 0 C over 10 minutes and the reaction mixture was stirred at the same temperature for 30 min. After completion of the reaction, the solvent was removed under vacuum. The residue obtained was poured into water (30 mL), extracted with ethyl acetate (150 mL), The organic layer was dried over sodium sulfate and concentrated to provide the title compound (0.160 g, 52.4%), 1H NMR (400 MHz, DMSO-d6) delta ppm 9.18-9.20 (s, 1H), 8.74 (s, 2H), 5.49-5.67 (b, 1H), 4.60 (s, 2H).

These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,10070-92-5, its application will become more common.

Reference:
Patent; TEMPERO PHARMACEUTICALS, INC.; BALOGLU, Erkan; GHOSH, Shomir; LOBERA, Mercedes; SCHMIDT, Darby, R.; WO2013/19621; (2013); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia