The patent badge is an abbreviated version of the USPTO patent document. The patent badge does contain a link to the full patent document.
The patent badge is an abbreviated version of the USPTO patent document. The patent badge covers the following: Patent number, Date patent was issued, Date patent was filed, Title of the patent, Applicant, Inventor, Assignee, Attorney firm, Primary examiner, Assistant examiner, CPCs, and Abstract. The patent badge does contain a link to the full patent document (in Adobe Acrobat format, aka pdf). To download or print any patent click here.
Patent No.:
Date of Patent:
Sep. 09, 2025
Filed:
Dec. 14, 2022
Chengda Pharmaceuticals Co., Ltd., Jiaxing, CN;
Yu Feng, Jiaxing, CN;
Hong Xu, Jiaxing, CN;
Jiaxuan Wu, Jiaxing, CN;
Danhui Song, Jiaxing, CN;
Weihui Zhong, Jiaxing, CN;
Fei Ling, Jiaxing, CN;
Chao Xu, Jiaxing, CN;
CHENGDA PHARMACEUTICALS CO., LTD., Jiaxing, CN;
Abstract
The present disclosure relates to the field of drug synthesis, and discloses a method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone. In the preparation method according to the present disclosure, for the first time, trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as shown in Formula I is obtained from amino-substituted pentanal and a thiazolyl sulfoxide compound as raw materials by Mislow-Evans rearrangement reaction and subsequent Lewis acid catalysis. The method for the preparation of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone as an intermediate of halofuginone according to the present disclosure has high yields and stable qualities, provides a new reference route for the synthesis of trans-N-benzyloxycarbonyl-(3-hydroxy-2-piperidinyl)-2-propanone, avoids the reduction of pyridine, and overcomes the disadvantage of requiring the use of an expensive metal catalyst Rh/Al2O3.