申请人:API CORPORATION
公开号:US20210403427A1
公开(公告)日:2021-12-30
The present invention aims to provide a method for producing a (2S,5R)-5-(protected oxyamino)-piperidine-2-carboxylic acid derivative at a low cost that can be performed under mild reaction conditions not requiring a facility at an extremely low temperature, is safer, can control the quality of the desired product with ease, and shows good workability in the site of production. A method for producing a compound represented by the formula (2):
wherein PG
1
is an amino-protecting group, PG
2
is an amino-protecting group, PG
3
is a hydroxyl-protecting group, LG is a leaving group, and R is a hydrocarbon group having 1-8 carbon atoms and optionally having substituent(s), including a step of reacting a compound represented by the formula (1):
wherein each symbol is as defined above, with a hydroxylamine derivative represented by the formula PG
2
NHOPG
3
wherein each symbol is as defined above, in the presence of a base in a solvent.
本发明旨在提供一种低成本的方法,用于在温和反应条件下生产(2S,5R)-5-(保护氧氨基)-哌啶-2-羧酸衍生物,不需要极低温度设施,更安全,并且可以轻松控制所需产品的质量,在生产现场具有良好的可操作性。该方法包括以下步骤:与公式(1)所表示的化合物在溶剂中反应,其中PG1是氨基保护基,PG2是氨基保护基,PG3是羟基保护基,LG是离去基团,R是具有1-8个碳原子的烃基,并且可选地具有取代基,与公式PG2NHOPG3所表示的羟胺衍生物在碱的存在下反应。