Preparing 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid used in mirogabalin besylate preparation, involves reacting 2-(3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3-en-6-yl)acetic acid and chiral amino acid, converting the amino acid salt to product
	SANKAPELLY D K; MALLEPALLI S R; SHAIK N M; ALLA R
	2023-09-16
专利权人	LEE PHARMA LTD (LEEP-C)
申请日期	2023-09-16
专利号	IN202341062361-A
成果简介	NOVELTY - Preparing 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid of (I), involves: (a) treating 2-(3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3-en-6-yl)acetic acid or their ester of (II) with a chiral amino acid in a solvent to obtain chiral amino acid salt of 2-((1R,5S,6S)-3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3- en-6-yl)acetic acid or their ester compound of (IIIa); (b) converting chiral amino acid salt (IIIa) to 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid (I). USE - Improved process for preparing 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid used in preparation of mirogabalin besylate for treating peripheral neuropathic pain (PNP), including diabetic PNP and post-herpetic neuralgia. No biological data given. ADVANTAGE - The process is highly safe, stable, cost-effective, and eco-friendly; avoids expensive reagents; minimize impurities by avoiding deprotection step after resolution; and exhibit short reaction time, with high productivity and purity. DETAILED DESCRIPTION - Preparing 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid of formula (I), involves: (a) treating 2-(3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3-en-6-yl)acetic acid or their ester of formula (II) with a chiral amino acid in a solvent to obtain chiral amino acid salt of 2-((1R,5S,6S)-3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3- en-6-yl)acetic acid or their ester compound of formula (IIIa); (b) converting chiral amino acid salt (IIIa) to 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid (I). R=H, or carboxylic acid protecting group.
IPC 分类号	A61P-025/00 ; C07C-227/34 ; C07C-229/08 ; C07C-405/00 ; C07C-069/70
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/20367
专题	中国科学院新疆生态与地理研究所
作者单位	LEE PHARMA LTD (LEEP-C)
推荐引用方式 GB/T 7714	SANKAPELLY D K,MALLEPALLI S R,SHAIK N M,et al. Preparing 2-((1R,5S,6S)-6-(aminomethyl)-3-ethylbicyclo[3.2.0]hept-3-en-6-yl)acetic acid used in mirogabalin besylate preparation, involves reacting 2-(3-ethyl-6-(nitromethyl)bicyclo[3.2.0]hept-3-en-6-yl)acetic acid and chiral amino acid, converting the amino acid salt to product. IN202341062361-A[P]. 2023.

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