945016-63-7

945016-63-7 - Names and Identifiers

Name	3-(2-chloropyriMidin-4-yl)-1H-indole
Synonyms	3-(2-Chloro-4-pyrimidyl)indole 3-(2-Chloro-4-pyrimidinyl)-1H-indole 3-(2-chloropyriMidin-4-yl)-1H-indole 1H-Indole, 3-(2-chloro-4-pyrimidinyl)-
CAS	945016-63-7

945016-63-7 - Physico-chemical Properties

Molecular Formula	C12H8ClN3
Molar Mass	229.66
Storage Condition	under inert gas (nitrogen or Argon) at 2-8°C

945016-63-7 - Upstream Downstream Industry

Raw Materials	3-(2-chloropyrimidin-4-yl)-1-(phenylsulfonyl)-1H-indole 1-(PHENYLSULFONYL)-1H-INDOL-3-YLBORONIC ACID Pyrimidine, 2-chloro-4-ethynyl- (9CI) Nitrosobenzene 2,4-Dichloropyrimidine Indole
Downstream Products	N-(4-fluoro-2-Methoxy-5-nitrophenyl)-4-(1-Methylindol-3-yl)pyriMidin-2-aMine AZ 7550

945016-63-7 - Reference Information

application

3-(2-chloro-pyrimidine-4-yl)-1H-indole can be used as an organic synthesis intermediate and a pharmaceutical intermediate, mainly used in laboratory research and development processes and chemical and pharmaceutical synthesis processes.
2,3, 4-trimethoxybenzaldehyde is an important pharmaceutical intermediate, which can be used for the synthesis of new drugs Ca2 channel blockers. The drug can be selectively used in cerebral arteries to reduce the incidence of headache, and there is a certain demand in the European and American markets. It can also be used as trimetazidine impurity C, which can be used in the standard formulation of trimetazidine in the research and development process. The research of impurities is an important content of drug research and development.

preparation

using gallic acid derivative 2,3, 4-trihydroxybenzaldehyde as main raw material, dimethyl sulfate as alkylating agent, methylation reaction is carried out by O-alkylation method in the presence of quaternary amine salt and sodium hydroxide as phase transfer catalyst. the chemical reaction formula is as follows: control the reaction temperature to 50~70 ℃, after the reaction, the material is left to stand and layered, the upper oil is washed to neutral with water, distilled under reduced pressure, and refined to obtain white crystalline powder, which is the product trimetazidine impurity C. The alkylating agent dimethyl sulfate, the catalyst quaternary amine salt and sodium hydroxide are fed in stages to complete the methylation reaction in multiple stages; the weight of each material is fed as follows: 2,3, 4-trihydroxybenzaldehyde: dimethyl sulfate: PTC catalyst = 1: 3~4: 0.08~0.1. The feeding scheme makes the yield of 2,3, 4-trimethoxybenzaldehyde product reach 88%; the new phase transfer catalyst is adopted, the reaction conditions are mild, and the purity is above 99%. The high-purity product can ensure the reliability of this product as an intermediate in pharmaceutical production.

Last Update：2024-04-09 20:52:54

945016-63-7 - Uses and synthesis methods

application

2,3, 4-trimethoxybenzaldehyde is an important pharmaceutical intermediate, which can be used for the synthesis of new drugs Ca2 channel blockers. The drug can be selectively used in cerebral arteries to reduce the incidence of headache, and there is a certain demand in the European and American markets. It can also be used as trimetazidine impurity C, which can be used in the standard formulation of trimetazidine in the research and development process. The research of impurities is an important content of drug research and development.

Preparation

Using gallic acid derivative 2,3, 4-trihydroxybenzaldehyde as the main raw material, dimethyl sulfate as alkylating agent, in the presence of phase transfer catalyst quaternary amine salt and sodium hydroxide, through O-Alkylation method for methylation reaction,

control the reaction temperature of 50~70 ℃, after the reaction, the material is left to stand and stratified, the upper oil is washed to neutral with water, distilled under reduced pressure, and refined to obtain white crystalline powder as trimetazidine impurity c of the product. The alkylating agent dimethyl sulfate, the catalyst quaternary amine salt and sodium hydroxide are fed in stages to complete the methylation reaction in multiple stages; the weight of each material is fed as follows: 2,3, 4-trihydroxybenzaldehyde: dimethyl sulfate: PTC catalyst = 1: 3~4: 0.08~0.1. The feeding scheme makes the yield of 2,3, 4-trimethoxybenzaldehyde product reach 88%; the new phase transfer catalyst is adopted, the reaction conditions are mild, and the purity is above 99%. The high-purity product can ensure the reliability of this product as an intermediate in pharmaceutical production.

Last Update：2024-04-09 01:59:50