Preparing ritlecitinib used for treating severe alopecia areata, involves reacting 7H-pyrrole[2,3-d]pyrimidine derivative with piperidine derivative followed by deprotecting the amine protected group, converting (6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine into ritlecitinib
	SOMISETTI N R; NANDEPU H; NANDEPU V R
	2023-09-07
专利权人	METROCHEM API PVT LTD (METR-Non-standard)
申请日期	2023-09-07
专利号	IN202341060086-A
成果简介	NOVELTY - Preparing ritlecitinib of (I) or its salts, involves: (a) reacting 1-chloro-7H-pyrrole[2,3-d]pyrimidine derivative of (II) with specific isomer of 5-amino-2-methyl-1-piperidine derivative of (III) to provide amine protected group substituted 5-((7H-pyrrolo[2,3-d] pyrimidin-4-yl)amino)-2-methylpiperidine derivative of (IV); (b) deprotecting amine protected group substituted 5-((7H-pyrrolo[2,3-d] pyrimidin-4-yl)amino)-2-methylpiperidine derivative (IV) to provide 5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl) amino)-2-methylpiperidine derivative of (V); (c) deprotecting 5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl) amino)-2-methylpiperidine derivative of (V) to provide ((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine derivative of (VI) or its salt; (d) converting ((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine derivative of (VI) into ritlecitinib of (I); and (e) optionally converting ritlecitinib into its salt. USE - Process for peparing ritlecitinib or its salts used for the treatment of severe alopecia areata in adults and adolescents 12 years and older. No biological data given. ADVANTAGE - The process is more economical, easy to scale up and commercially viable. DETAILED DESCRIPTION - Preparing ritlecitinib of formula (I) or its salts, involves: (a) reacting 1-chloro-7H-pyrrole[2,3-d]pyrimidine derivative of formula (II) with specific isomer of 5-amino-2-methyl-1-piperidine derivative of formula (III) to provide amine protected group substituted 5-((7H-pyrrolo[2,3-d] pyrimidin-4-yl)amino)-2-methylpiperidine derivative of formula (IV); (b) deprotecting amine protected group substituted 5-((7H-pyrrolo[2,3-d] pyrimidin-4-yl)amino)-2-methylpiperidine derivative (IV) to provide 5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl) amino)-2-methylpiperidine derivative of formula (V); (c) deprotecting 5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl) amino)-2-methylpiperidine derivative of (V) to provide ((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine derivative of formula (VI) or its salt; (d) converting ((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine derivative of (VI) into ritlecitinib of (I); and (e) optionally converting ritlecitinib into its salt; or (i) deprotecting 5-((7H-pyrrolo[2,3-d]pyrimidin-4-yl) amino)-2-methylpiperidine derivative of (V) in the presence of an acid without using any metal catalyst to provide ((3R,6S)-6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine derivative of (VI). P1, P2=amine protecting group. INDEPENDENT CLAIMS are included for: 1. a compound, which is selected from, e.g., amine protected group substituted 5-((7H-pyrrolo[2,3-d] pyrimidin-4-yl)amino)-2-methylpiperidine derivative of formulae (IVa), or (IVb); and 2. a process for the purification of ritlecitinib tosylate of compound of formula (Ia), which involves: slurrying or crystallizing the ritlecitinib tosylate of (Ia) from a suitable solvent selected from methanol, ethanol, isopropanol, butanol, t-butanol, acetonitrile, water and/or mixtures.
IPC 分类号	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/20467
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	SOMISETTI N R,NANDEPU H,NANDEPU V R. Preparing ritlecitinib used for treating severe alopecia areata, involves reacting 7H-pyrrole[2,3-d]pyrimidine derivative with piperidine derivative followed by deprotecting the amine protected group, converting (6-methylpiperidin-3-yl)-7H-pyrrolo [2,3-d]pyrimidin-4-amine into ritlecitinib. IN202341060086-A[P]. 2023.

条目包含的文件
条目无相关文件。

除非特别说明，本系统中所有内容都受版权保护，并保留所有权利。