Day: June 23, 2021

Electric Literature of 739364-95-5, 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.739364-95-5, name is 2-Methylpyrazolo[1,5-a]pyrimidine-6-carboxylic acid, molecular formula is C8H7N3O2, molecular weight is 177.16, as common compound, the synthetic route is as follows.

Compound of formula (1) (30 g) and N-hydroxysuccinimide (19.5 g)It was suspended in 200 mL of dichloromethane and a mixture of EDCI (36 g) in dichloromethane was added portionwise on an ice bath.The mixture was stirred at room temperature for 8 hours. Filtered to obtain 40 g of O-2,5-dicarbonylpyrrolyl-2-methylpyrazolo[1,5-a]pyrimidine-6-carboxylate (I-1) as a white solid.Yield 86%.

The chemical industry reduces the impact on the environment during synthesis 739364-95-5, I believe this compound will play a more active role in future production and life.

Reference:
Patent; Chenxin Pharmaceutical Co., Ltd.; Shanghai Pharmaceutical Industry Institute; Li Jianqi; Ni Feng; Zhang Yi; Zhang Shuxin; Zhang Jin; Wu Xiabing; Du Zhenxin; Lu Xiulian; (9 pag.)CN104974160; (2017); 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. 696-82-2, name is 2,4,6-Trifluoropyrimidine, the common compound, a new synthetic route is introduced below. Safety of 2,4,6-Trifluoropyrimidine

(Preparation by the process of the older German Patent Application P 39 00 471.6) 335.8 g (1.865 mol) of 30% strength sodium methylate (in methanol) were added to a mixture of 250 g (1.865 mol) of 2,4,6-trifluoropyrimidine and 1.4 1 of methanol at -20 C. over the course of 45 minutes, and the mixture was stirred at this temperature for a further 30 minutes. It was then allowed to warm to 25 C. and concentrated to about 1/5 of its volume. The resulting mixture was partitioned between diethyl ether and water, and then the organic phase was dried over magnesium sulfate and concentrated. Distillation (1.1 m column, 3 mm V-shaped packing) resulted in 141.6 g (52% of theory) of the title compound of boiling point 144-145 C. Distillation of the residue with a Normag head resulted in 114.4 g (42% of theory) of 4,6-difluoro-2-methoxypyrimidine of boiling point 157-161 C.

The synthetic route of 696-82-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Hamprecht; Gerhard; US5283332; (1994); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 3435-28-7, 6-Methylpyrimidin-4-amine, 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, 3435-28-7, blongs to pyrimidines compound. Computed Properties of C5H7N3

A mixure of ferf-butyl N-[3-chloro-4-(4-chlorothiazolo[5,4-c]pyridin-2-yl)-5-fluoro- phenyljcarbamate (56 mg, 0.135 mmol), 6-methylpyrimidin-4-amine (44 mg, 0.40 mmo), Pd2(dba)3 (6.2 mg, 0.00676 mmol), XantPhos (7.8 mg, 0.0135 mmol) and Cs2C03 (88 mg, 0.27 mmol) in 1,4-Dioxane (2 mL) was heated at 150 C in a microwave reactor for 20 min, The mixture was filtered through Celite, washed with EtOAc, concentrated. The crude product was purified by reverse phase HPLC to give the title compound (5.4 mg, 10% yield) as a yellow solid. ¾ NMR (400 MHz, DMSO-i/6) delta 10.48 (s,1H), 8.61 (s, 1H), 8.39 (d, J= 5.6 Hz, 1H), 7.75 (d, J= 5.6 Hz, 1H), 7.58 (s, 1H), 6.66 (s, 1H), 6.49 (dd, J = 12.7, 2.0 Hz, 1H), 6.34 (s, 2H), 2.38 (s, 3H). LCMS (Method B): RT = 3.43 min, m/z 387.0 [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,3435-28-7, its application will become more common.

Reference:
Patent; F. HOFFMANN-LA ROCHE AG; BLENCH, Toby; ELLWOOD, Charles; GOODACRE, Simon; LAI, Yingjie; LIANG, Jun; MACLEOD, Calum; MAGNUSON, Steven; TSUI, Vickie; WILLIAMS, Karen; ZHANG, Birong; WO2012/35039; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 10070-92-5, Pyrimidine-5-carbaldehyde, 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, 10070-92-5, blongs to pyrimidines compound. COA of Formula: C5H4N2O

General procedure: To a solution of amine (1.0 equiv) in 1,2-dichloroethane (0.1 M) were added aldehyde (1.2 equiv) and acetic acid (0.5 mL), the reaction mixture stirred at rt for 10 min, followed the addition of sodium triacetoxyborohydride (2.0 equiv). The reaction was stirred at rt under nitrogen for 18 h and concentrated. Sat. NaHCO3 (30 mL) was added and extracted with dichloromethane (20 mL x 3) and the combined organic layers were dried over anhydrous Na2SO4, filtered and evaporated under reduced pressure. The crude residue was purified by flash chromatography on silica gel eluting with 0-10% methanol/dichloromethane to give the desired product.

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:
Article; Wang, Mingliang; Fang, Yanjia; Gu, Shoulai; Chen, Fangfang; Zhu, Zhengjiang; Sun, Xun; Zhu, Jidong; European Journal of Medicinal Chemistry; vol. 132; (2017); p. 157 – 172;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 959070-42-9, name is Ethyl 4,6-dichloro-2-(methylthio)pyrimidine-5-carboxylate. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: Ethyl 4,6-dichloro-2-(methylthio)pyrimidine-5-carboxylate

To an ice cold solution of the ethyl ester of 4,6-dicholoro-2-methylthiopyrimidine-5-carboxylic acid (5 g, 18.72 mmol) in tetrahydrofuran (60 ml) was added methyl 3-benzylaminopropanoate (3.61 g, 18.72 mmol) followed by Et3N (2.86 ml, 20.59 mmol). The reaction mixture was stirred at room temperature for 6 hours. It was then diluted with ethyl acetate and washed with water. The organic layer was separated, dried, filtered and concentrated to give the crude product. The crude product was then purified by silica gel flash column chromatography (15% ethyl acetate in hexane) to afford the desired product as a pale yellow solid (6 g, 75% yield). 1H NMR (CDCl3 400 MHz) delta 7.36-7.28 (m, 4H), 7.19 (d, J=6.8 Hz), 4.76 (s, 2H), 4.13-4.08 (q, 2H), 3.74 (t, J=7.2 Hz, 2H), 3.66 (s, 3H), 2.67 (t, J=7.2 Hz), 2.44 (s, 3H), 1.20 (7.2 Hz, 3H).

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, 959070-42-9, Ethyl 4,6-dichloro-2-(methylthio)pyrimidine-5-carboxylate.

Reference:
Patent; ArQule, Inc.; US2010/249110; (2010); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 69034-12-4, Adding some certain compound to certain chemical reactions, such as: 69034-12-4, name is 2-Chloro-5-(trifluoromethyl)pyrimidine,molecular formula is C5H2ClF3N2, 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 69034-12-4.

Step A: (2S,3R)-tert-butyl 2-methyl-3-((5-(trifluoromethyl)pyrimidin-2-yl)amino)piperidine-1-carboxylate. A solution of intermediate B-4 (1 g), 2-chloro-5-(trifluoromethyl)pyrimidine (850 mg) and DIPEA (1.6 mL) in n-BuOH (15 mL) was heated to 100 C. for 1 h. The mixture was diluted with H2O and extracted with EtOAc. The combined organics were dried (MgSO4). Purification via silica gel chromatography (0-30% EtOAc in heptane) gave the title compound (1.5 g, 89%). MS (ESI) mass calcd. for C16H23F3N4O2, 360.4; m/z found 305.1 [M-55]+.

According to the analysis of related databases, 69034-12-4, the application of this compound in the production field has become more and more popular.

Reference:
Patent; JANSSEN PHARMACEUTICA NV; Dvorak, Curt A.; Shireman, Brock T.; US2014/275095; (2014); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 147118-37-4, 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 147118-37-4, name is N-(4-(4-Fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide. This compound has unique chemical properties. The synthetic route is as follows.

The present embodiment of rosuvastatin calcium intermediate preparation,which is 6 – [(1E) -2- [4- (4- fluorophenyl) -6-isopropyl- 2- [methyl (methylsulfonyl) amino] -5-pyrimidinyl] ethenyl] -dimethyl-l, 3-dioxane-4-acetic acid tert-butyl ester comprises the following steps: (1) under the protection of N2,To a 1000 mL reaction flask was added 36 g of compound of formula 3,21 g of compound of formula 2 and 620 mL of tetrahydrofuran,Heated to 42 C and stirred until clear,Then cooled to -15 C, added 1.8mL of water, 20g of potassium tert-butoxide, the reaction was incubated for 60 minutes after the addition; (2) The reaction was quenched with 105mL saturated ammonium chloride, quenched after the addition of 600mL water, and then 600mL ethyl acetate extraction, washed with brine, dried and concentrated to give a pale yellow solid,Add 288mL of methanol and 48mL water recrystallization,Filtration and drying gave 31 g of a white solid, which was the target product.

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 147118-37-4, N-(4-(4-Fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide.

Reference:
Patent; Zhejiang Mei Nuohua Pharmaceutical Chemical Co., Ltd.; Yu Kui; Huang Xiangliang; Xing Yulong; Shen Qi; Yu Shenggang; Chen Weiren; Yao Chengzhi; (7 pag.)CN107298675; (2017); 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.696-82-2, name is 2,4,6-Trifluoropyrimidine, molecular formula is C4HF3N2, molecular weight is 134.06, as common compound, the synthetic route is as follows.Quality Control of 2,4,6-Trifluoropyrimidine

EXAMPLE 12 Preparation of 2-benzylamino-4,6-difluoropyrimidine (Variant A) STR20 23.5 g (0.22 mol) of benzylamine were added at -20 C. to a stirred mixture of 13.4 9 (0.1 mol) of 2,4,6-trifluoropyrimidine in 150 ml of diethyl ether within 15 min, and the mixture was stirred at this temperature for 1 hour. After a further hour at 25 C., working up was carried out as in Example 10. 21.4 g (98% of theory) of the title compound of melting point 70-73 C. were obtained in this way.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,696-82-2, 2,4,6-Trifluoropyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; BASF Aktiengesellschaft; US5011927; (1991); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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 55583-59-0, name is 2,5-Diamino-4,6-dichloropyrimidine. This compound has unique chemical properties. The synthetic route is as follows. Recommanded Product: 2,5-Diamino-4,6-dichloropyrimidine

Scheme 4. Synthesis of 7-substituted-2-amino-4-chloro-8-((4-methoxy-3,5-dimethylpyridin- 2-yl)methyl)-7,8-dihydropteridin-6(5H)-one: (a) NaBH(OAc)3, TEA, CH2Cl2, room temperature, 2 hr; 57 – 76% yield (b) 4,6-dichloropyrimidine-2,5-diamine, H2SO4, MeOH, reflux, overnight; 2.1% yield c) DIEA, nBuOH, 150C in sealed tube, 48 h; 5 – 10% yield (d) NaH, DMF, RX., room temperature, overnight.

With the rapid development of chemical substances, we look forward to future research findings about 55583-59-0.

Reference:
Patent; PONIARD PHARMACEUTICALS, INC.; WO2009/139834; (2009); 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