Day: February 19, 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.39551-54-7, name is 2,4-Dichloropyrido[3,2-d]pyrimidine, molecular formula is C7H3Cl2N3, molecular weight is 200.0248, as common compound, the synthetic route is as follows.Safety of 2,4-Dichloropyrido[3,2-d]pyrimidine

2,4,-dichloropyrido[3,2-d]pyrimidine (1068 mg, 5.34 mmol, 1 equiv.) was treated with dioxane (10 ml) followed by N,N-diisopropylethylamine (5.7 mL, 32.0 mmol, 6 equiv.), and then 2-amino-2-ethyl-hexanoic acid ethyl ester 85A (1000 mg, 5.34 mmol, 1 equiv., supplied by J&W Pharmlab, LLC). The mixture was stirred at 80 C. overnight. The reaction mixture partitioned between EtOAc (50 mL) and H2O (50 mL). The organics were separated, dried over MgSO4, and concentrated in vacuo to afford 85B that was then used directly. LCMS (m/z): 351.23 [M+H]+; tR=1.43 min. on LC/MS Method A

At the same time, in my other blogs, there are other synthetic methods of this type of compound,39551-54-7, 2,4-Dichloropyrido[3,2-d]pyrimidine, and friends who are interested can also refer to it.

Reference:
Patent; Gilead Sciences, Inc.; Aktoudianakis, Evangelos; Chin, Gregory; Mackman, Richard L.; Metobo, Samuel E.; Mish, Michael R.; Pyun, Hyung-jung; Zablocki, Jeff; (175 pag.)US2016/289229; (2016); 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. 936643-80-0, name is 2-(Chloromethyl)pyrimidine hydrochloride, molecular formula is C5H6Cl2N2, 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 936643-80-0

A solution of 1 -(5-(4,4,5, 5-tetramethyl- 1,3,2-dioxaborolan-2-yl)pyridin-2-yl)piperazine (1 .0 g, 3.5 mmol), 2-(chloromethyl)pyrimidine hydrochloride (0.68 g, 4.1 mmol), and Cs2CO3 (2.8 g, 8.6 mmol) in DMF (6 mL) was stirred overnight at ambient temperature, and then at 50 C until LCMS indicated reaction completion. After cooling to ambient temperature, the reaction mixture was diluted with MTBE (20 mL), and extracted sequentially with 1:1 water: saturated NaHCO3(aq) (5 mL) and brine (3 x 5 mL). The organic extracts were dried over anhydrous Mg504, filtered, and concentrated in vacuo. The residue obtained was purified by silica chromatography (1-25% DCM-MeOH as the gradient eluent) to afford the title compound (500 mg, 38% yield). ?H NMR (400 IVIFIz, CDC13) 8.76-8.75 (d, 2H), 8.54-8.53 (d, 1H), 7.82-7.79 (dd, 1H), 7.22-7.20 (t, 1H), 6.59-6.57 (d, 1H), 3.88 (s, 2H), 3.71-3.68 (m, 4H), 2.70-2.68 (m, 4H), 1.31 (s, 12H).

With the rapid development of chemical substances, we look forward to future research findings about 936643-80-0.

Reference:
Patent; ARRAY BIOPHARMA, INC.; ANDREWS, Steven W.; BLAKE, James F.; CHICARELLI, Mark J.; GOLOS, Adam; HAAS, Julia; JIANG, Yutong; KOLAKOWSKI, Gabrielle R.; (594 pag.)WO2017/11776; (2017); 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. 42965-55-9, name is 5,6-Diaminopyrimidine-2,4(1H,3H)-dione sulfate. A new synthetic method of this compound is introduced below., HPLC of Formula: C4H8N4O6S

General procedure: 5,6-Diaminouracil sulphate (1.31 mmol, 1 eq.) was suspended in water (35 mL). The mixture wasmade alkaline using a methanolic solution of NaOH (0.65M, 3 eq.) and heated to 90 C for 15 min.A solution of diketone (1.96 mmol, 1.5 eq.) in a mixture of THF (40 mL) and water (15 mL) was addedand the mixture was stirred at 90 C for 45 min. The reaction mixture was acidified glacial acetic acid(15 mL) and heated at 90 C for another 20 h. The reaction mixture was subsequently concentrated toapproximately 1/3 of the volume, cooled in the freezer and the as-obtained suspension was filteredand the solid fraction was washed with cold water (30 mL) and cold ethanol (20 mL) to yield the crudeflavin derivative. The crude product was purified by digestion in boiling methanol. The digestedflavin derivative was further subjected to vacuum sublimation to yield the final target compound.

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, 42965-55-9, 5,6-Diaminopyrimidine-2,4(1H,3H)-dione sulfate.

Reference:
Article; Richtar, Jan; Heinrichova, Patricie; Apaydin, Dogukan Hazar; Schmiedova, Veronika; Yumusak, Cigdem; Kovalenko, Alexander; Weiter, Martin; Sariciftci, Niyazi Serdar; Krajcovic, Jozef; Molecules; vol. 23; 9; (2018);,
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. 32779-36-5, name is 5-Bromo-2-chloropyrimidine, the common compound, a new synthetic route is introduced below. Formula: C4H2BrClN2

To a solution of 5-bromo-2-chloropyrimidine (1) (0.01 mol) in methanol (100 mL), added hydrazine hydrate (80%, 0.03 mol) drop wise with external cooling. The reaction mixture was stirred at room temperature. Completion of the reaction was confirmed by thin layer chromatography (TLC). The solid separated was filtered, washed well with water, dried and recrystallized from ethyl acetate [35].

The synthetic route of 32779-36-5 has been constantly updated, and we look forward to future research findings.

Reference:
Article; Adhikari, Adithya; Kalluraya, Balakrishna; Sujith, Kizhakke Veedu; Gouthamchandra, Kuluvar; Jairam, Ravikumar; Mahmood, Riaz; Sankolli, Ravish; European Journal of Medicinal Chemistry; vol. 55; (2012); p. 467 – 474;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 6299-87-2, 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 6299-87-2, name is 6-Hydroxypyrimidine-4-carboxylic acid. This compound has unique chemical properties. The synthetic route is as follows.

Step 2: 6-chloropyrimidine-4-carboxylic acid chloride 50.0 g (0.35 mol) 6-hydroxypyrimidine-4-carboxylic acid were taken and 500 mL phosphorus oxychloride were added. Then 150 g (0.72 mol) phosphorus pentachloride were added batchwise with stirring. The reaction mixture was refluxed for 5 h. The phosphorus oxychloride was distilled off and the residue was purified by vacuum distillation through a column. Yield: 51.9 g (83% of th.) MS: m/z=176/178/180 (M)+

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 6299-87-2, 6-Hydroxypyrimidine-4-carboxylic acid.

Reference:
Patent; BOEHRINGER INGELHEIM INTERNATIONAL GMBH; US2011/21500; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 56181-39-6, 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. 56181-39-6, name is 5-Bromo-4-chloropyrimidine, molecular formula is C4H2BrClN2, 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.

Compound (III-11) (120 mg, 0.620 mmol) and compound (IIb-2) (150 mg, 0.931 mmol) were dissolved in NMP(2.0 mL), p-toluenesulfonic acid monohydrate (118 mg, 0.620 mmol) was added and the mixture was stirred at 60C for2 hr. The reaction mixture was allowed to cool, water was added, and the mixture was extracted with ethyl acetate. Theorganic layer was dried over anhydrous sodium sulfate, and filtered. The solvent was evaporated under reduced pressure,and the residue was purified by silica gel column chromatography (n-hexane:ethyl acetate) to give compound (IV-122)(yield 100 mg, 51%)

According to the analysis of related databases, 56181-39-6, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Kaken Pharmaceutical Co., Ltd.; WATANABE, Atsushi; SATO, Yuuki; OGURA, Keiji; TATSUMI, Yoshiyuki; (331 pag.)EP3351533; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 1142188-60-0, 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. 1142188-60-0, name is tert-Butyl 4-hydroxy-5,6-dihydropyrido[3,4-d]pyrimidine-7(8H)-carboxylate, molecular formula is C12H17N3O3, 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.

31-B. 4-Chloro-5,8-dihydro-6H-pyrido[3,4-Patent; NOVARTIS AG; ARTMAN III, Gerald David; ELLIOTT, Jason Matthew; JI, Nan; LIU, Donglei; MA, Fupeng; MAINOLFI, Nello; MEREDITH, Erik; MIRANDA, Karl; POWERS, James J.; RAO, Chang; WO2010/66684; (2010); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 3680-69-1, Adding some certain compound to certain chemical reactions, such as: 3680-69-1, name is 4-Chloro-7H-pyrrolo[2,3-d]pyrimidine,molecular formula is C6H4ClN3, 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 3680-69-1.

4-chloro-7H-pyrrolo[2,3-d]pyrimidine (8.0 g, 52.32 mmol, 1.0 eq) was dissolved in DMF (40 mL), NIS (15.7 g, 57.55 mmol, 1.1 eq) was added at 0C, stirred overnight at room temperature, 200 mL of saturated Na2S2O3 solution was added, filtered, washed with water three times, and dried in vacuum to obtain 14.6 g (100%) of products. 1H NMR (400 MHz, d6-DMSO): delta 12.94 (s, 1H), 8.59 (s, 1H), 7.93 (d, J = 2.4 Hz, 1H).

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. 3680-69-1, 4-Chloro-7H-pyrrolo[2,3-d]pyrimidine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Jinan University; Shanghai Institute of Materia Medica, Chinese Academy of Sciences; DING, Ke; GENG, Meiyu; TAN, Li; DING, Jian; ZHANG, Zhang; AI, Jing; REN, Xiaomei; GAO, Donglin; TU, Zhengchao; LU, Xiaoyun; ZHANG, Dongmei; (88 pag.)EP3339294; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Application of 14394-56-0, Adding some certain compound to certain chemical reactions, such as: 14394-56-0, name is 4-Amino-6-chloro-5-methylpyrimidine,molecular formula is C5H6ClN3, 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 14394-56-0.

The compound 6-chloro-5-methylpyrimidin-4-amine 48a (100 mg, 0.700 mmol), cyclopropylcarbonyl chloride (87 mg,0.839 mmol), pyridine (3 mL) and tetrahydrofuran (3 mL) were combined.The mixture was heated to 60 C and stirred for 16 hours.This mixture was diluted with 20 ml of water and extracted with ethyl acetate (20 mL¡Á2).The combined organic phases were washed with brine (20 mL¡Á2).The organic phase is dried over anhydrous sodium sulfate, and the desiccant is removed by filtration.Decompressing under reduced pressure to obtain a crude product,The residue was purified by preparative silica gel ( petroleum ether / ethyl acetate = 4:1).The target product N-(6-chloro-5-methylpyrimidin-4-yl)cyclopropanecarboxamide 48b (40 mg,0.190 mmol, white solid). Yield: 27%.

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. 14394-56-0, 4-Amino-6-chloro-5-methylpyrimidine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Nanjing Tianyinjianhua Pharmaceutical Technology Co., Ltd.; Kong Xianglong; Zhou Chao; Zheng Zhixiang; (105 pag.)CN109020957; (2018); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 6693-08-9, 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 6693-08-9 as follows.

Intermediate 17(4,6-Dichloro-5-fluoro-pyrimidin-2-yl)-(5-methoxy-lH-pyrazol-3-yl)-amine To the solution of 2,4,6-trichloro-5-fluoro-pyrimidine (PCT Pub. No. WO200549033, 1.66 g, 8.26 mmol) in EtOH (3OmL) at -300C was added 5-methoxy-lH-pyrazol-3-amine (Intermediate 8, 1.Og, 9.08 mmol). DIPEA (4.3 mL, 25 mmol) was added to the solution and the reaction mixture was naturally warmed to 00C for 3 hours and then at room temperature overnight. Evaporation of the solvents under reduced pressure, a white precipitate was removed by filtration. The mother liquid was evaporated to dryness and purified by silica gel chromatography (ISCO, DCM/MeOeta/Neta4Oeta: 100/0/0-100/3/0.3) to give the title compound (221mg, 10%). LCMS: 279 [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,6693-08-9, its application will become more common.

Reference:
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2008/132502; (2008); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia