公开(公告)号：US20240228451A1

公开(公告)日：2024-07-11

申请号：US18556727

申请日：2022-04-21

申请人： Panafina, Inc.

发明人： Zeeshan Kamal ,  Apparao Bokka ,  Gopalakrishna Akurathi ,  Gary Richard Lee

IPC分类号： C07D305/12 ,  C07C51/347 ,  C07C51/487 ,  C07C67/14 ,  C07C67/31 ,  C07C67/313 ,  C07D309/30 ,  C07D309/32

CPC分类号： C07D305/12 ,  C07C51/347 ,  C07C51/487 ,  C07C67/14 ,  C07C67/31 ,  C07C67/313 ,  C07D309/30 ,  C07D309/32

摘要： Provided according to embodiments of the invention are methods of forming a lipstatin derivative, (S)-1-((2S,3S)-3-ethyl-4-oxooxetan-2-yl) tridecan-2-yl formyl-L-alaninate. Such methods include one or more reaction steps that include the Mitsunobu coupling of N-formyl L-alanine in the presence of di-t-butyl azodicarboxylate (DBAD) and triphenylphosphine. Compounds formed by a method of the invention, compositions that include a compound formed by a method of the invention, and methods of inhibiting lipase activity and/or treating pancreatitis using a compound formed by a method of the invention are also provided.