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1. (WO2018028420) POLYCRYSTALLINE FORM OF DEHYDROPHENYLAHISTIN-LIKE COMPOUND, AND MANUFACTURING AND PURIFICATION METHOD AND APPLICATION THEREOF.

Pub. No.:    WO/2018/028420    International Application No.:    PCT/CN2017/094066
Publication Date: Fri Feb 16 00:59:59 CET 2018 International Filing Date: Tue Jul 25 01:59:59 CEST 2017
IPC: C07D 403/06
A61K 31/496
A61P 35/00
A61P 31/10
Applicants: MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.
青岛海洋生物医药研究院股份有限公司
Inventors: LI, Wenbao
李文保
WANG, Shixiao
王世潇
DING, Zhongpeng
丁忠鹏
HOU, Yingwei
侯英伟
GUAN, Huashi
管华诗
Title: POLYCRYSTALLINE FORM OF DEHYDROPHENYLAHISTIN-LIKE COMPOUND, AND MANUFACTURING AND PURIFICATION METHOD AND APPLICATION THEREOF.
Abstract:
A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.