Preparing abrocitinib for treating moderate-to-severe atopic dermatitis, comprises reacting methylamino cyclobutane compound with acid, reacting acid salt of compound with base, reacting protected 7H-pyrrolo[2,3-d]pyrimidine compound with propane sulfonyl halide, and converting obtained compound
	BIJJULA R V K; SOMISETTI R N; NANDEPU H; NANDEPU R V
	2023-09-14
专利权人	METROCHEM API PVT LTD (METR-Non-standard)
申请日期	2023-09-14
专利号	IN202341062066-A
成果简介	NOVELTY - Preparing abrocitinib (I) comprises: (a) reacting methylamino cyclobutane compound (II) with an acid to obtain corresponding acid salt of compound (III'); (b) reacting the acid salt of compound (III') with a suitable base to obtain protected 7H-pyrrolo[2,3-d]pyrimidine compound (III); (c) reacting the compound (III) with propane sulfonyl halide to obtain amino-protected abrocitinib compound (IV); and (d) converting the compound (IV) into abrocitinib (I). USE - Method for preparing abrocitinib for treating moderate-to-severe atopic dermatitis. No biological data given. ADVANTAGE - The method provides abrocitinib (I) with purity of more than 99% by HPLC, and high yield in cost-effective manner. DETAILED DESCRIPTION - Preparing Abrocitinib of formula (I) comprises: (a) reacting methylamino cyclobutane compound of formula (II) with an acid to obtain corresponding acid salt of compound of formula (III'); (b) reacting the acid salt of compound (III') with a suitable base to obtain protected 7H-pyrrolo[2,3-d]pyrimidine compound of formula (III); (c) reacting the compound (III) with propane sulfonyl halide to obtain amino-protected abrocitinib compound of formula (IV); and (d) converting the compound (IV) into abrocitinib (I). P1,P2=amine protecting group; and n=1 or 2. INDEPENDENT CLAIMS are included for: a method for preparing compound (III); and amine-protected 7H-pyrrolo[2,3-d]pyrimidine compound of formula (III'a) and tosyl-substituted 7H-pyrrolo[2,3-d]pyrimidine compound of formula (III'b).
IPC 分类号	A61K-031/519 ; C07D-487/04
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/20407
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	BIJJULA R V K,SOMISETTI R N,NANDEPU H,et al. Preparing abrocitinib for treating moderate-to-severe atopic dermatitis, comprises reacting methylamino cyclobutane compound with acid, reacting acid salt of compound with base, reacting protected 7H-pyrrolo[2,3-d]pyrimidine compound with propane sulfonyl halide, and converting obtained compound. IN202341062066-A[P]. 2023.

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