Preparing methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound used for preparing Bilastine, involves reacting 1-[4-(2-chloroethyl)-phenyl]-2- methyl-propan-1-one compound with N-chlorosuccinamide to provide 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one
	BOPPANA D; SOMISETTI N R; NANDEPU H; NANDEPU V R
	2023-08-17
专利权人	METROCHEM API PVT LTD (METR-Non-standard)
申请日期	2023-08-17
专利号	IN202341055183-A
成果简介	NOVELTY - Preparing methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound (I) involves reacting 1-[4-(2-chloroethyl)-phenyl]-2- methyl-propan-1-one compound (II) with N-chlorosuccinamide to provide a 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one compound (III), reacting 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one compound (III) with trimethoxymethane to provide a methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound (I). USE - Method for preparing methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound used for preparing Bilastine (claimed). ADVANTAGE - The method can develop a commercially viable and eco-friendly process for the preparation of Bilastine intermediates with high yields and purity. DETAILED DESCRIPTION - Preparing methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound of formula (I) involves (A) reacting 1-[4-(2-chloroethyl)-phenyl]-2- methyl-propan-1-one compound of formula (II) with N-chlorosuccinamide to provide a 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one compound of formula (III), (B) reacting 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one compound of formula (III) with trimethoxymethane to provide a methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound of formula (I). An INDEPENDENT CLAIM is included for a method for preparing Bilastine of formula (VIII), which involves: (a) preparing a pure methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound of formula (I); and (b) converting the methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound of formula (I) into Bilastine of formula (VIII).
IPC 分类号	C07C-045/46 ; C07C-049/233 ; C07C-057/58 ; C07D-401/04
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/20791
专题	中国科学院新疆生态与地理研究所
作者单位	METROCHEM API PVT LTD (METR-Non-standard)
推荐引用方式 GB/T 7714	BOPPANA D,SOMISETTI N R,NANDEPU H,et al. Preparing methyl 2-[4-(2-chloroethyl)-phenyl]-2-methyl-propionate compound used for preparing Bilastine, involves reacting 1-[4-(2-chloroethyl)-phenyl]-2- methyl-propan-1-one compound with N-chlorosuccinamide to provide 2-chloro-1-[4-(2-chloroethyl)-phenyl]-2-methyl-propan-1-one. IN202341055183-A[P]. 2023.

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