Preparing difelikefalin acetate, for treating moderate-to-severe pruritus associated with chronic kidney disease in adults undergoing hemodialysis, by anchoring Fmoc with resin, capping resin, deprotecting Fmoc, coupling next amino acid followed by removing side chain protecting group of amino acids
	REDDY M V; REDDY G V; RAJAN S T
	2023-08-23
专利权人	MSN LAB PRIVATE LTD R & D CENT (MSNM-Non-standard)
申请日期	2023-08-23
专利号	IN202341056371-A
成果简介	NOVELTY - Preparing difelikefalin acetate involves (a) anchoring Fmoc-Pic(PG1)-OH with resin; (b) capping the resin; (c) selectively deprotecting the Fmoc group; (d) coupling the next amino acid (Fmoc-D-Lys(PG2)-OH) to the compound obtained in step (c) in presence of a coupling agent; (e) repeating the steps (c) and (d) to obtain desired peptide sequence; (f) removing the side chain protecting groups of amino acids and cleavage of the peptide from the resin to provide difelikefalin or its salt; or, (d) coupling the next amino acid Fmoc-D-Lys(PG2)-OH to the compound obtained in step (c) in presence of a coupling agent to obtain Fmoc-D-Lys(PG2)-Pic(PG1)-Resin; (e) repeating the steps (c) and (d) by using Fmoc-D-Leu-OH, Fmoc-D-Phe-OH, Fmoc-DPhe-OH to obtain desired peptide sequence Fmoc-D-Phe-D-Phe-D-Leu-D-Lys(PG2)- Pic(PG1)-Resin; and (f) converting the obtained compound to get difelikefalin or its salt. USE - Method for preparing difelikefalin acetate, that used for the treatment of moderate-to-severe pruritus associated with chronic kidney disease in adults undergoing hemodialysis. No biological data is given. ADVANTAGE - The method is simple, safe, economic and suitable for the production of difelikefalin acetate in good yield and better quality. DETAILED DESCRIPTION - An INDEPENDENT CLAIM is included for a method for the preparation of Fmoc piperidine compound of formula (II) which involves: (a) selective deprotection of piperidine compound of formula (VII), by treating it with a deprotecting agent to provide piperidine based compound of formula (VIII); and (b) treating the compound of formula (VIII) with Fmoc protecting agent to provide the compound (II), where PG1'=Allyloxycarbonyl (Alloc); and PG3'=Tert.butoxy carbonyl (Boc).
IPC 分类号	A61P-021/00 ; A61P-025/16 ; C07C-229/36 ; C07C-049/755 ; C07D-309/38 ; C07F-009/6561 ; C07K-007/06
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/20716
专题	中国科学院新疆生态与地理研究所
作者单位	MSN LAB PRIVATE LTD R & D CENT (MSNM-Non-standard)
推荐引用方式 GB/T 7714	REDDY M V,REDDY G V,RAJAN S T. Preparing difelikefalin acetate, for treating moderate-to-severe pruritus associated with chronic kidney disease in adults undergoing hemodialysis, by anchoring Fmoc with resin, capping resin, deprotecting Fmoc, coupling next amino acid followed by removing side chain protecting group of amino acids. IN202341056371-A[P]. 2023.

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