Improved process of preparing quinazoline compound used for preparing chlordiazepoxide active pharmaceutical ingredient, involves reacting 2-chloroacetamido-5-chlorobenzophenone oxime compound with p-toluene sulfonic acid in presence of non-polar solvents to obtain quinazoline compound
	TRIPATHI A P; RAIKWAR D K; PAWAR M P; NAIK A M; SAWANT S D
	2023-07-21
专利权人	CENTAUR PHARM PVT LTD (CENT-Non-standard)
申请日期	2023-07-21
专利号	IN202321049222-A
成果简介	NOVELTY - Improved process of preparing quinazoline compound (I) involves reacting 2- chloroacetamido-5-chlorobenzophenone oxime compound (II) with p-toluene sulfonic acid in presence of non-polar solvents to obtain quinazoline compound (I). USE - Method for improved process of preparing quinazoline compound used for preparing chlordiazepoxide active pharmaceutical ingredient (claimed), chlordiazepoxide, lormetazepam, midazolam, lorazepam and oxazepam. ADVANTAGE - The method is an improved, simple, cost-efficient and environment friendly process for the preparation of quinazoline compound. DETAILED DESCRIPTION - Improved process of preparing quinazoline compound of formula (I) involves reacting 2- chloroacetamido-5-chlorobenzophenone oxime compound of formula (II) with p-toluene sulfonic acid in presence of non-polar solvents to obtain quinazoline compound of formula (I). An INDEPENDENT CLAIM is included for an one pot synthesis of 7-chloro-2-methylamino-5-pheny1-3H-1,4-benzodiazepine-4- oxide (chlordiazepoxide active pharmaceutical ingredient (API)) compound of formula (IIII), which involves: reacting 2-chloro-N-(4-chloro-2-((hydroxyimino)(phenyl)methyl) phenyl) acetamide based compound of formula (IV) with p-toluene sulfonic acid in presence of non-polar solvents to obtain 6-chloro-2-(chloromethyl)-4- phenylquinazoline-3-oxide compound of formula (V), which is in situ treated with monomethylamine to obtain 7-chloro-2-methylamino-5-pheny1-3H1,4-benzodiazepine-4-oxide (chlordiazepoxide API) compound of formula (III). R= H, For Cl.
IPC 分类号	A61K-031/551 ; A61P-025/00 ; C07D-239/82 ; C07D-403/12
国家	印度
专业领域	医药卫生
语种	英语
成果类型	专利
文献类型	科技成果
条目标识符	http://119.78.100.226:8889/handle/3KE4DYBR/21178
专题	中国科学院新疆生态与地理研究所
作者单位	CENTAUR PHARM PVT LTD (CENT-Non-standard)
推荐引用方式 GB/T 7714	TRIPATHI A P,RAIKWAR D K,PAWAR M P,et al. Improved process of preparing quinazoline compound used for preparing chlordiazepoxide active pharmaceutical ingredient, involves reacting 2-chloroacetamido-5-chlorobenzophenone oxime compound with p-toluene sulfonic acid in presence of non-polar solvents to obtain quinazoline compound. IN202321049222-A[P]. 2023.

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