Tag: M.W=500-600

Related Products of 274693-26-4, 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.274693-26-4, name is 2-(((3aR,4S,6R,6aS)-6-(7-(((1R,2S)-2-(3,4-Difluorophenyl)cyclopropyl)amino)-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl)-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl)oxy)ethanol, molecular formula is C26H32F2N6O4S, molecular weight is 562.63, as common compound, the synthetic route is as follows.

2 g of compound h, 50 mL of methanol, 3 mol/L of HCl 48 mL were added to the reaction flask at room temperature, and magnetically stirred until dissolved.Solution, the ice bath was cooled to below 20 C, and the reaction was stirred for 15 h. After the reaction of co is completed, 20 mL of a 1 mol/L NaOH aqueous solution is added thereto. The pH was adjusted to about 7.2, methanol was distilled off, and 50 mL of ethyl acetate was added. The aqueous layer was separated and the organic layer was washed with brine. Evaporate 20 mL of ethyl acetate, replenish 30 mL of ethyl acetate, repeat the operation twice, combine the filtrates, and distill off part of the acetic acid.Ethyl ester, 200 mL of isooctane was added thereto, and the temperature was slowly raised to 50 C by an oil bath, stirred at a constant temperature for 30 min, and cooled to 20 C.The product j was precipitated, and dried by filtration to obtain 1.2 g of a pale yellow powder. The yield was 90%, and the HPLC purity was 97.88%. Compound j Chemical name: (1S, 2S, 3R, 5S)-3-[7-{[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino}-5-( Propylthio)-3H-[1,2,3]-triazole[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-dialcohol.

The chemical industry reduces the impact on the environment during synthesis 274693-26-4, I believe this compound will play a more active role in future production and life.

Reference:
Patent; Beijing Kanglisheng Pharmaceutical Development Co., Ltd.; Cheng Gang; (14 pag.)CN104059069; (2016); B;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 355806-00-7, (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, 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, Quality Control of (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, blongs to pyrimidines compound. Quality Control of (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester

Example 3; Hydrolysis of terf-butyl ester of rosuvastatin in a solution of strong organic nitrogen bases; The solution of terf-butyl ester of rosuvastatin in a mixture of a base, tetrahydrofuran and water in the ratio of 1:6:15 by volume is stirred at 50C for few hours. The reaction mixture is sampled and analysed by HPLC to find out the completion of reaction. Results are shown in Table 2. EPO

The synthetic route of 355806-00-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; LEK PHARMACEUTICALS D.D.; WO2006/136407; (2006); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 289042-12-2, tert-Butyl 2-((4R,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, 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, HPLC of Formula: C29H40FN3O6S, blongs to pyrimidines compound. HPLC of Formula: C29H40FN3O6S

The method for synthesizing the rosuvastatin calcium chiral isomer impurity of the present embodiment comprises the following steps:(1) 20g compound I was added to 500mL three reaction flask, stirred and dissolved in 220mL of acetonitrile was added dropwise 60mL 0.05M hydrochloric acid, the reaction was incubated dropwise at 35 ~ 40 C for 3 hours until the starting material disappeared (TLC: Ester: petroleum ether = 6: 1),The pH was adjusted to neutral with 5% sodium bicarbonate solution, the acetonitrile was removed by distillation under reduced pressure, extracted twice with methylene chloride (100 mL * 2), dried over anhydrous sodium sulfate, filtered,The filtrate was transferred to 500mL three reaction flask, 60g of manganese dioxide was added, the reaction was refluxed for 20 hours, the reaction was over, filtered, the filtrate was evaporated under reduced pressure and concentrated to dryness to give 17.6g light yellow oil, namely compound III, directly into the next reaction; The yield of compound III was 95.2%

The synthetic route of 289042-12-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Zhejiang Mei Nuohua Pharmaceutical Chemical Co., Ltd.; Yu Kui; Huang Xiangliang; Jia Jiangnan; Liu Tao; Yu Shenggang; Lin Zufeng; Chen Weiren; Yao Chengzhi; (12 pag.)CN107382875; (2017); A;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Adding a certain compound to certain chemical reactions, such as: 1195768-23-0, N-(3-(2-(tert-Butyl)-5-(2-chloropyrimidin-4-yl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide, 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: N-(3-(2-(tert-Butyl)-5-(2-chloropyrimidin-4-yl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide, blongs to pyrimidines compound. Recommanded Product: N-(3-(2-(tert-Butyl)-5-(2-chloropyrimidin-4-yl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide

Preparation Example 1 The preparation of the Known Crystal Form 1: Refer to the preparation method described in example 58a of patent document WO2009/137391A2 or U.S. Pat. No. 7,994,185B2, with the details as follows: Add N-{3-[5-(2-chloro-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide (196 mg, 0.364 mmol) and 7M methanol solution of ammonia (8 ml, 56 mmol) into a 25 mL autoclave, heat to 90 C. and react for 24 h; when the TLC shows the raw material is completely reacted, cool the above reaction system to room temperature, filter to get N-{3-[5-(2-amino-4-pyrimidinyl)-2-(1,1-dimethylethyl)-1,3-thiazol-4-yl]-2-fluorophenyl}-2,6-difluorobenzenesulfonamide (i.e. Dabrafenib). 1H-NMR (400 MHz, DMSO-d6) delta ppm 10.83 (s, 1H), 7.93 (d, J=5.2 Hz, 1H), 7.55-7.70 (m, 1H), 7.35-7.43 (m, 1H), 7.31 (t, J=6.3 Hz, 1H), 7.14-7.27 (m, 3H), 6.70 (s, 2H), 5.79 (d, J=5.13 Hz, 1H), 1.35 (s, 9H). The XPRD pattern is as shown in FIG. 25 and is substantially the same as that of the Known Crystal Form 1 of Dabrafenib prepared in example 58a of patent document U.S. Pat. No. 7,994,185B2. The PLM plot is as shown in FIG. 26. It shows small block-shaped crystals. PSD shows: D10, D50 and D90 are 40 mum, 104 mum and 151 mum, respectively. The dynamic vapor sorption isothermal is as shown in FIG. 27. It shows: the weight change is 1.9% between 20% RH80% RH.

At the same time, in my other blogs, there are other synthetic methods of this type of compound,1195768-23-0, N-(3-(2-(tert-Butyl)-5-(2-chloropyrimidin-4-yl)thiazol-4-yl)-2-fluorophenyl)-2,6-difluorobenzenesulfonamide, and friends who are interested can also refer to it.

Reference:
Patent; Hangzhou Pushai Pharmaceutical Technology Co., LTD.; LAO, Haiping; SHENG, Xiaoxia; Sheng, Xiaohong; US2015/307484; (2015); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Related Products of 289042-12-2, 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.289042-12-2, name is tert-Butyl 2-((4R,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, molecular formula is C29H40FN3O6S, molecular weight is 577.71, as common compound, the synthetic route is as follows.

To a solution of acetonide protected tert-butyl ester of rosuvastatin (II) (25 g) a dilute solution of TFA in water (2.5 g in 25 mL water) was added at 30-40 C. The reaction was stirred for 30 minutes to 1 hour and then water (25 mL) was added to it. The reaction mixture was again stirred for 3-4 hours at the same temperature. Then an aqueous solution of sodium hydroxide (3.46 g in 100 mL water) was added and the reaction mixture was stirred for 1 hour. The reaction mixture was further diluted with water (200 mL) and washed with toluene (2 x 250 mL) and MTBE (125 mL). MTBE (250 mL) was further added to the aqueous layer. Then sodium chloride (6.25 g) was added to the reaction mixture. An aqueous solution of sodium bisulphate (15 g in 100 mL of water) was added to the reaction mass and the pH was adjusted to 2.4. The organic layer was separated. The aqueous layer was again extracted with MTBE (200 mL) and the combined organic layer was washed with sodium chloride solution (125 mL). A solution of tert-butyl amine (7.91 g) in MTBE (250 mL) was added to the reaction mixture and stirred for 2-6 hours. The reaction mixture was cooled to 15-20 C and stirred at this temperature for 1 hour. The precipitated solid was isolated and dried. The solid was suspended in a mixture of acetonitrile (62.5 mL) and IPA (62.5 mL) and heated to a temperature of 50-55 C for 1-3 hours. The reaction mixture was then cooled to 25-35 C and stirred at this temperature for 2-6 hours. The reaction mixture was further cooled to 10-15 C and stirred for 1 hour. The precipitated solid was filtered, washed with a mixture of acetonitrile and IPA and dried to provide the title compound.Yield: 20.5 g (86 %)Purity by HPLC: 99.82 %

The chemical industry reduces the impact on the environment during synthesis 289042-12-2, I believe this compound will play a more active role in future production and life.

Reference:
Patent; DR. REDDY’S LABORATORIES LIMITED; DAHANUKAR, Vilas Hareshwar; AMBHAIKAR, Narendra Bhalchandra; VADALI, Ravi kumar; MERUVA, Suresh babu; MANIKONDA, Swapna; KAMARAJU, Raghavendra Rao; TIMMANNA, Upadhya; MOHAMMED, Aaseef; PULIPATI, Ranga Prasad; MOHAMMED, Yakub Iqbal; WO2012/172564; (2012); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 355806-00-7, 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. 355806-00-7, name is (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, molecular formula is C26H36FN3O6S, 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 1; Hydrolysis of terf-butyl ester of rosuvastatin in aqueous solution of amines; 7.5 g of terf-butyl ester of rosuvastatin 38 ml of demineralized water 2 to 5 equivalents of amineThe reactants and water as the solvent are stirred in the autoclave from 98 to 1000C for 1 to 4 hours. The reaction mixture is sampled and analyzed by HPLC (“High Pressure Liquid Chromatography”) to find out the completion of reaction. Results are shown in Table 1. EPO

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 355806-00-7, (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester.

Reference:
Patent; LEK PHARMACEUTICALS D.D.; WO2006/136407; (2006); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Reference of 355806-00-7, 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.355806-00-7, name is (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, molecular formula is C26H36FN3O6S, molecular weight is 537.64, as common compound, the synthetic route is as follows.

A solution of the compound of formula (41) (4.2 g, 7.8 MMOL) in ethanol (100 ML) IS added dropwise, at 0C, to a solution of sodium hydroxide (0. 1 M in water, 76 ml). The ice bath is removed and the reaction mixture is stirred at room temperature for 1 hour. The solvent is then drawn off using a rotary evaporator and the crude product is made to crystallise by adding ether. In that manner, 3.6 G (92 %) of the sodium salt (42) can be obtained in the form of a slightly yellowish powder. 1H NMR (300 MHz, D20): 1.14 (d, J = 6.7 Hz, 6H); 1.39-1. 42 (m, 1H) ; 1.50-1. 61 (m, 1H) ; 2.10-2. 24 (m, 2H); 3.21-3. 38 (m, 1H) ; 3.36 (s, 3H); 3.46 (s, 3H); 3.61-3. 72 (m, 1H) ; 4. 18-4. 24 (m, 1 H) ; 5.39 (dd, J = 8.5, 8.5 Hz, 2H); 7.40-7. 49 (m, 2H).

Statistics shows that 355806-00-7 is playing an increasingly important role. we look forward to future research findings about (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester.

Reference:
Patent; CIBA SPECIALTY CHEMICALS HOLDING INC.; WO2004/103977; (2004); A2;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Synthetic Route of 355806-00-7, 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.355806-00-7, name is (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, molecular formula is C26H36FN3O6S, molecular weight is 537.64, as common compound, the synthetic route is as follows.

B . 7- [4-(4-fluorophenyl)-6-isopropyl-2-(memanesulfonyl-methyl- amino)-pyrimidin-5-yl]- (S^SSydihydroxy-hept-delta-enoic acid zinc salt (2:1)7.54 g (13.96 mmol) of 7-[4-(4-fluorophenyl)-6-isopropyl-2- (methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3i?,55)-dihydroxy- hept-6-enoic acid tert-butylester [compound of the general Formula (III), wherein the meaning of T is hydroxy, R is hydrogen, Q is t-butyl group] obtained in the previous stage are dissolved in 80 ml of ethanol and into this solution 6.98 ml of 2.5 M (17.44 mmol) of sodium hydroxide solution are added dropwise in 20 minutes. Subsequently the reaction mixture is stirred at the temperature of 60 C for 60 minutes. Subsequently the reaction mixture is cooled by using an ice- water mixture to a temperature between 0 and 10 C and at the same temperature, 5.80 ml (17.44 mmol) of 3.0 M hydrochloric acid solution are added thereto dropwise and the stirring is continued for a further 10 minutes. The reaction mixture is evaporated and the residue is extracted with 80 ml of water and 80 ml of ethylacetate.

Statistics shows that 355806-00-7 is playing an increasingly important role. we look forward to future research findings about (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester.

Reference:
Patent; EGIS GYOGYSZERGYAR NYILVANOSAN MUeKOeDOe RESZVENYTARSASAG; WO2009/47577; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 289042-12-2, Adding some certain compound to certain chemical reactions, such as: 289042-12-2, name is tert-Butyl 2-((4R,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,molecular formula is C29H40FN3O6S, 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 289042-12-2.

3 g of the compound prepared in Example 1 is dissolved in 30 ml of ACN at room temperature, and then 9 ml of 1N HCl is added. The reaction is completed by stirring at room temperature for 8 hours.The reaction was cooled and maintained at 0 C,Add 0.9 g 10% aqueous NaOH solution.The reaction is allowed to warm to room temperature and then stirred for 4 hours to complete the reaction. Water is added to quench the reaction and then 3 mL of 1N HCl is slowly added dropwise to bring the pH to 8.0. The aqueous layer was washed with methylene chloride to separate the aqueous layerdo. 2.7 g of CaCl2 was added thereto, followed by stirring at room temperature for about 30 minutes. The reaction solution is kept below 15 C to produce a solid and then filtered.After washing with water, suvastatin was dried under reduced pressure to obtain 2.6 g of a calcium salt of a white solid.

According to the analysis of related databases, 289042-12-2, the application of this compound in the production field has become more and more popular.

Reference:
Patent; WELL ENC CO., LTD; GO, SUNG HWAN; KIM, GYUNG IR; GO, YOUNG LI; PARK, YONG MUK; JUNG, HUN HWEE; (18 pag.)KR101566536; (2015); B1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia

Electric Literature of 355806-00-7, 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. 355806-00-7, name is (3R,5S,6E)-7-[4-(4-Fluorophenyl)-6-isopropyl-2-[(methanesulfonyl) methylamino]pyrimidin-5-yl]-3,5-dihydroxyhept-6-enoic acid tert-butyl ester, molecular formula is C26H36FN3O6S, 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.

B . 7- [4-(4-fluorophenyl)-6-isopropyl-2-(methanesulfonyl-methyl- amino)-pyrimidin-5-yl]- (3i?,5S)-dihydroxy-hept-6-enoic acid zinc salt (2:1)7.81 g (14.5 mmol) of 7-[4-(4-fluorophenyl)-6-isopropyl-2- (methanesulfonyl-methyl-amino)-pyrimidin-5-yl]-(3i?,5S)-dihydroxy- hept-6-enoic acid fert-butylester are dissolved in 200 ml of ethanol at room temperature and 58 ml of 0.25 M sodium hydroxide solution (14.5 mmol) are added dropwise in 30 minutes. The reaction mixture is kept at the temperature of 60 C for 4 hours. Subsequently the solution is filtered on a G4 sintered glass filter and the ethanol is evaporated at 20 Hgmm pressure. The residue is mixed with 40 ml of water and extracted three times with 15 ml of ethylacetate each and the aqueous layer is evaporated. From the residue, 10 ml of ethanol is evaporated twice and the remaining solids are stirred in 40 ml of diisopropylether and filtered. Yield, 6.65 g (91 %)The quality of the product is identical in all respects with those of the product obtained in Example 5.

According to the analysis of related databases, 355806-00-7, the application of this compound in the production field has become more and more popular.

Reference:
Patent; EGIS GYOGYSZERGYAR NYILVANOSAN MUeKOeDOe RESZVENYTARSASAG; WO2009/47577; (2009); A1;,
Pyrimidine | C4H4N2 – PubChem,
Pyrimidine – Wikipedia