Day: November 16, 2020

1193-24-4, 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. 1193-24-4, name is 4,6-Dihydroxypyrimidine. This compound has unique chemical properties. The synthetic route is as follows.

b. 4,6-Dichloro-pyrimidine-5-carbaldehyde A mixture of DMF (3.2 mL) and POCl3 (10 mL) at 0 C. was stirred for 1 h, treated with 4,6-dihydroxypyrimidine (2.5 g, 22.3 mmol), and stirred for 0.5 h at ambient temperature. The heterogeneous mixture was heated at reflux for 3 h and the volatiles were removed at reduced pressure. The residue was poured into ice water and extracted six times with ethyl ether. The organic phase was washed with aqueous NaHCO3, dried over Na2SO4 and concentrated to afford a yellow solid (3.7 g, 95%). 1H NMR (CDCl3) delta 10.46 (s, 1H), 8.90 (s, 1H).

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 1193-24-4, 4,6-Dihydroxypyrimidine.

Reference:
Patent; Gaul, Michael David; Xu, Guozhang; Baumann, Christian Andrew; US2006/281764; (2006); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

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 147118-37-4 as follows., 147118-37-4

Example 13 Preparation of 2-((4/?,6S)-6-((E)-2-(4-(4-fluorophenyl)-6-isopropyl-2-(N- methylmethylsulfonamido)pyrimidin-5-yl)vinyl)-2,2-dimethyl-1 ,3-dioxan yl)acetate, methyl ester (O) from N-(4-(4-fluorophenyl)-5-formyl-6- isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (J) and 2-((4 ?,6S)-6- ((benzo[d]thiazol-2-ylsulfonyl)methyl)-2,2-dimethyl-1 ,3-dioxan-4-yl)acetate methyl ester (N)(N) (J) (O) N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide (0.35 g, I .O mmol) and 2-((4 ,6S)-6-((benzo[d]thiazol-2-ylsulfonyl)methyl)-2,2-dimethyl- 1 ,3-dioxan-4-yl)acetate methyl ester (0.45 g, 1.1 mmol) were added to 12 mL of dry THF After stirring for 10 min at 20C, the reaction mixture was cooled to -70C. At this temperature 1.5 mL of NaHMDS solution (1 M in THF, total 1.5 mmol) was added in 1 h keeping the temperature between -70 and -75C. When dosing was completed, the reaction mixture was stirred for 2h at -75C, then quenched with 10% aqueous NaHC03 (10 mL). The phases were separated. The aqueous layer was extracted with 2 x 25 mL of ethyl acetate. The combined organic phases were washed with 5% aqueous Na2C03 and concentrated under vacuum. The residue was crystallized from isopropanol to give 2-((4 ,6S)-6-((E)-2-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido) pyrimidin-5-yl)vinyl)-2,2-dimethyl-1 ,3-dioxan-4-yl)acetate, methyl ester as a solid (Compound O, 0.34 g, 0.63 mmol, 63% yield).

The chemical industry reduces the impact on the environment during synthesis 147118-37-4, I believe this compound will play a more active role in future production and life.

Reference:
Patent; DSM SINOCHEM PHARMACEUTICALS NETHERLANDS B.V.; DE LANGE, Ben; RIEBEL, Peter, Hans; WOLBERG, Michael; HEEMSKERK, Dennis; MINK, Daniel; WO2012/98048; (2012); A1;,
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 90213-66-4, name is 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine. This compound has unique chemical properties. The synthetic route is as follows. 90213-66-4

A solution of 2,4-dichloro-7H-pyrrolo[2,3-d]pyrimidine (1.00 g, 5.32 mmol) in THF (8 mL) was stirred at 0 C for 5 mm. Then sodium hydride (255 mg, 6.38 mmol) was added. The resulting mixture was stirred for 15 mm, then iodomethane (8.50 g, 53.20 mmol) was added. The reaction mixture was warmed to rt and stirred overnight. H20 (100 mL) was added to quench the reaction, and the resulting mixture was extracted with EtOAc (50 mL x 3). The combined organic phases were washed with brine (80 mL), dried over anhydrous Na2504, filtered, and the filtrate was concentrated in vacuo. The residue was purified by silica gel chromatograph (PE/EtOAc (v/v) = 10/1) to give the tilte compound as a white solid (1.00 g, 93 %).MS (ESI, pos. ion) m/z: 203.0 [M+H]t

Statistics shows that 90213-66-4 is playing an increasingly important role. we look forward to future research findings about 2,4-Dichloro-7H-pyrrolo[2,3-d]pyrimidine.

Reference:
Patent; SUNSHINE LAKE PHARMA CO., LTD.; REN, Qingyun; TANG, Changhua; YIN, Junjun; YI, Kai; LEI, Yibo; WANG, Yejun; ZHANG, Yingjun; (215 pag.)WO2018/127096; (2018); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

2380-63-4, 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. 2380-63-4, name is 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, molecular formula is C5H5N5, 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 1 (15 g, 111 mmol), NIS (30 g, 133.2 mmol) and DMF (150 ml) was stirred at 90 C for 4 h and then cooled to room temperature.Add 150 ml of water and filter with solids.Wash with 100 ml of water and 100 ml of ethanol in sequence.Dry at 70 C to obtain 23 g of solid,Yield: 79.4%.

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. 2380-63-4, 1H-Pyrazolo[3,4-d]pyrimidin-4-amine, other downstream synthetic routes, hurry up and to see.

Reference:
Patent; Shanghai Pharmaceutical Industry Institute; China Pharmaceutical Industry Zongyuan; Zheng Nan; Hao Qun; Zhou Weicheng; Song Chengen; Zhang Peng; He Bo; Cao Yuanchao; Bi Siju; (56 pag.)CN109776544; (2019); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

137281-39-1 , The common heterocyclic compound, 137281-39-1, name is 4-(2-(2-Amino-4-oxo-4,7-dihydro-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl)benzoic acid, molecular formula is C15H14N4O3, 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 4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]-pyrimidin-5-yl)ethyl]benzoic acid (38.4 mg, 0.129 mmol) in 5 mL of DMF was added N-methylmorpholine (40.4 mg, 0.399 mmol), followed by the addition of 2-chloro-4,6-dimethoxy-1,3,5-triazine (22.64 mg, 0.129 mmol). The resulting mixture was stirred for 1.5 hours at 25 !C, at which time HPLC showed that the reaction was complete. L-glutamic acid gamma-benzyl ester (30.6 mg, 0.129 mmol) was added, and stirring was continued at 25 !C until complete conversion of precursor was determined by HPLC (around two hours). To the reaction mixture was added 10 mL of methylene chloride and 10 ml of deionized water, and the mixture was stirred for 15 minutes. The layers were separated. The aqueous layer was extracted with DCM (10 ml*2). The organic phases were combined. The solution was concentrated on rotary-evaporator under reduced pressure. The resulting residue was subjected to flash chromatography on a Biotage system. Yield: 55 mg, 82%. 1HNMR in d6-DMSO, delta ppm: 10.61 (1H, s), 10.20 (1H, s), 8.72 (1H, d, J=10 Hz), 7.78 (2H, d, J=5 Hz), 7.35 (5H, m), 7.30 (2H, m), 6.30 (1H, s), 6.07 (2H, s), 5.14 (2H, s), 3.86 (1H, m), 2.97 (2H, t), 2.84 (2H, t), 2.20 (2H, s), 2.02 (1H, m), 1.95 (1H, m). ESI-MS: 518 [M+H]+.

The synthetic route of 137281-39-1 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; UNIVERSITY OF UTAH RESEARCH FOUNDATION; US2011/269713; (2011); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

611-08-5, 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. 611-08-5, name is 5-Nitrouracil, molecular formula is C4H3N3O4, 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: 2′,3′,5′-tri-O-Benzoyl-5-fluorouridine (3a)S1 (Table 2, entry 1). A mixture of5-fluorouracil (51.1 mg, 0.39 mmol), pyridine (0.6 mL), and hexamethyldisilazane(HMDS) (1.2 mL) was refluxed for ca. 40 min to give a clear solution of 2a. All thevolatiles were then removed under reduced pressure (ca. 1 mmHg) to give a clear syrup,which was dissolved in acetone (3.0 mL). To this were added1-O-acetyl-2,3,5-tri-O-benzoyl–D-ribofuranose (1) (151.8 mg, 0.30 mmol) and 7b (4.5mg, 0.015 mmol, 5 mol%) and the mixture was stirred under reflux for 6 h. After themixture was cooled to rt, it was diluted with EtOAc (2 mL), followed by the addition ofa saturated NaHCO3 aq (2 mL) at 0 C. After the mixture was stirred at 0 oC for 15min, EtOAc (30 mL) and a saturated NaHCO3 aq (20 mL) were added. The organicphase was separated and the aqueous phase was back-extracted with EtOAc (30 mL x 3).The combined organic layers were dried with Na2SO4 and evaporated to afford a crudematerial, which was purified by recrystallization from EtOAc (5 mL) and hexane (7mL) to afford 2′,3′,5′-tri-O-benzoyl-5-fluorouridine (3a) (152 mg, 88%) as a whitepowder.

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. 611-08-5, 5-Nitrouracil, other downstream synthetic routes, hurry up and to see.

Reference:
Article; Shirouzu, Hiroshi; Morita, Hiroki; Tsukamoto, Masaki; Tetrahedron; vol. 70; 22; (2014); p. 3635 – 3639;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

696-45-7, 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 696-45-7, name is 4-Amino-6-methoxypyrimidine. This compound has unique chemical properties. The synthetic route is as follows.

42.0 g of 4-amino-6-methoxypyrimidine (abbreviated as 4-MP, prepared according to Chinese patent CN 102516182) was added to 126 ml of pyridine at 0 to 5¡ãC, and 4-p-acetyl aminobenzenesulfonyl chloride (abbreviation SCL) 87.5 g. After the addition was complete, the reaction mixture was stirred at 20-30 ¡ã C until the 4-MP remained After completion of the reaction, 450 ml of ultrapure water was added and the supernatant was removed from the reaction mixture.

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 696-45-7, 4-Amino-6-methoxypyrimidine.

Reference:
Patent; YWK CHEMICALS (TAICANG) CO., LTD; HAMADA, Shinichi; HAMADA, Tomoko; WANG, YINING; GUO, XIAOYE; CHANG, YONGKAI; CHEN, YAN; WEI, WENJUN; (6 pag.)CN105294576; (2016); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

49845-33-2, A common compound: 49845-33-2, name is 2,4-Dichloro-5-nitropyrimidine,molecular formula is C4HCl2N3O2, it can change the direction of chemical reaction, and react with certain compounds to generate new functional products. A new synthetic method of this compound is introduced below.

General procedure: The reaction of 2,4-dichloro-5-nitropyrimidine withisopropylamine produced intermediate 2-chloro-N-isopropyl-5-nitropyrimidin-4-amine. 4-Fluoronitrobenzene reacted with1-methylpiperazine in DMSO yielded the intermediate 1-methyl-4-(4-nitrophenyl)piperazine in the presence of K2CO3. The catalytichydrogenation of 1-methyl-4-(4-nitrophenyl)piperazine with palladiumon carbon (Pd/C, 5%) quantificationally provided thedesired 4-(4-methylpiperazin-1-yl) aniline. Refluxing of the 2-chloro-N-isopropyl-5-nitropyrimidin-4-amine with 4-(4-methylpiperazin-1-yl)aniline in n-butanol yielded N4-isopropyl-N2-(4-(4-methylpiperazin-1-yl)phenyl)-5-nitropyrimidine-2,4-diamine,which was reduced to intermediate A1 with a good yield by catalytichydrogenation using Pd/C as a catalyst. Intermediates A wereprepared as these steps and used for the next step without furtherpurification. These processes were carried out as reported.

With the rapid development of chemical substances, we look forward to future research findings about 49845-33-2.

Reference:
Article; Hei, Yuan-Yuan; Shen, Ying; Wang, Jin; Zhang, Hao; Zhao, Hong-Yi; Xin, Minhang; Cao, Yong-Xiao; Li, Yan; Zhang, San-Qi; Bioorganic and Medicinal Chemistry; vol. 26; 8; (2018); p. 2173 – 2185;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

130049-82-0, 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.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, molecular weight is 242.7, as common compound, the synthetic route is as follows.

Example 28.0L of methanol, 1.04 Kg (4.28 moles) of 3-(2-chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-4H- pyrido[l,2-a]pyrimidin-4-one, 1.10 kg (10.89 moles) of triethyl amine and 1.0 kg (3.89 moles) of 6-fluoro-3(4-piperidinyl)-l,2-benzisoxazole hydrochloride were charged. The reaction mass was heated to reflux. The completion of reaction was monitored by HPLC. The reaction mass was cooled to 25-30C and further chilled to 0-5C, stirred for 30 min. and centrifuged. The cake obtained was washed with 0.5 L of chilled methanol. Weight of wet product containing paliperidone and inorganic salts was 1.0 kg, HPLC purity of paliperidone: 98.88%, keto- paliperidone impurity: 0.05%. The wet product obtained was further used for purification process.

Statistics shows that 130049-82-0 is playing an increasingly important role. we look forward to future research findings about 3-(2-Chloroethyl)-6,7,8,9-tetrahydro-9-hydroxy-2-methyl-4H-pyrido[1,2-a]pyrimidine-4-one.

Reference:
Patent; MEGAFINE PHARMA (P) LTD.; MATHAD, Vijayavitthal Thippannachar; SOLANKI, Pavankumar Vrajlal; SEKHAR, Babu Uppelli; PANDIT, Bhushan Sudhakar; WO2012/35554; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

3740-92-9 , The common heterocyclic compound, 3740-92-9, name is 4,6-Dichloro-2-phenylpyrimidine, molecular formula is C10H6Cl2N2, 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.

Under a nitrogen atmosphere, (10 g, 50 mmol) of compound 7-24-5 and (6.1 g, 50 mmol) of compound 9-12-6,(3.5 g, 3 mmol) tetrakis (triphenylphosphine) palladium, (3.2 g, 10 mmol) tetrabutylammonium bromide, (2 g, 50 mmol) sodium hydroxide,(15mL) water and (100mL) toluene were added to a 250mL three-necked flask, and the reaction was heated at 80 C with stirring for 12 hours.Most of the solvent was removed by rotary evaporation of the reaction solution, washed three times with dichloromethane and washed with water. The organic liquid was collected and mixed with silica gel.The yield is 80%

According to the analysis of related databases, 3740-92-9, the application of this compound in the production field has become more and more popular.

Reference:
Patent; Guangzhou Huarui Optoelectric Materials Co., Ltd.; He Ruifeng; Lin Weijie; Wu Canjie; Pan Junyou; (40 pag.)CN109970660; (2019); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia