Preparing Lisdexamphetamine for treating disorder e.g. binge-eating disorder, comprises reacting L-lysine monohydrochloride and amine protecting group, reacting obtained compound with acid activating compound, reacting isolated intermediate with D-amphetamine compound and deprotecting amide compound
	PUNE S V; AJITSINGH P J; PANDURANG P P; RAJPUT N A
	2023-10-04
专利权人	ALKEM LAB LTD (ALKE-Non-standard)
申请日期	2023-10-04
专利号	IN202321066394-A
成果简介	NOVELTY - Preparing Lisdexamphetamine (I) or its salt comprises: (a) reacting L-lysine monohydrochloride with amine protecting group in presence of base and suitable solvent to obtain diamino-protected L-lysine compound (II); (b) reacting diamino-protected L-lysine compound (II) with acid activating compound (III) in presence of base and suitable solvent to obtain anhydride intermediate (IV); (c) optionally, isolating the anhydride intermediate (IV); (d) reacting the anhydride intermediate (IV) with D-amphetamine compound (V) to obtain diamino-protected amide compound (VI); and (e) deprotecting the diamino protected amide compound (VI) to obtain Lisdexamphetamine or its salt. USE - Method for preparing Lisdexamphetamine for treating disorder such as attention deficit/hyperactivity disorder and binge-eating disorder. No biological data given. ADVANTAGE - The method provides Lisdexamphetamine with reduced level of impurities, in simple, scalable, and cost-effective manner. DETAILED DESCRIPTION - Preparing Lisdexamphetamine of formula (I) or its salt comprises: (a) reacting L-lysine monohydrochloride with amine protecting group in presence of base and suitable solvent to obtain diamino-protected L-lysine compound of formula (II); (b) reacting diamino-protected L-lysine compound (II) with acid activating compound of formula (III) in presence of base and suitable solvent to obtain anhydride intermediate of formula (IV); (c) optionally, isolating the anhydride intermediate of formula (IV); (d) reacting the anhydride intermediate compound (IV) with D-amphetamine compound (V) to obtain diamino-protected amide compound of formula (VI); and (e) deprotecting the diamino-protected amide compound (VI) to obtain Lisdexamphetamine or its salt. PG=amine protecting group; R=alkyl, or optionally substituted aryl; and X=halo such as Cl, Br, or I. INDEPENDENT CLAIMS are included for: 1. a method for preparing anhydride intermediate compound (IV); and 2. anhydride intermediate compound (IV).
IPC 分类号	C07C-231/02 ; C07C-237/06 ; C07C-269/04 ; C07C-271/22
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/20132
专题	中国科学院新疆生态与地理研究所
作者单位	ALKEM LAB LTD (ALKE-Non-standard)
推荐引用方式 GB/T 7714	PUNE S V,AJITSINGH P J,PANDURANG P P,et al. Preparing Lisdexamphetamine for treating disorder e.g. binge-eating disorder, comprises reacting L-lysine monohydrochloride and amine protecting group, reacting obtained compound with acid activating compound, reacting isolated intermediate with D-amphetamine compound and deprotecting amide compound. IN202321066394-A[P]. 2023.

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