Title:
INDUSTRIAL PREPARATION METHOD FOR HIGH-OPTICAL-PURITY RIMEGEPANT INTERMEDIATE
Document Type and Number:
WIPO Patent Application WO/2022/160937
Kind Code:
A1
Abstract:
The present invention provides an industrial preparation method for a high-optical-purity Rimegepant intermediate. Specifically, the present invention provides a chiral resolution method for an isomer mixture of a compound of formula III, wherein R is H or a hydroxyl protective group; moreover, the method comprises the steps: (a) performing chiral resolution on the isomer mixture of the compound of formula III by using optically active camphorsulfonic acid as a resolving agent to obtain a single configurational compound of formula III or camphorsulfonate thereof, wherein the optically active camphorsulfonic acid is L-camphorsulfonic acid or D-camphorsulfonic acid. The method in the present invention is mild in reaction conditions, simple and convenient in operation, high in yield especially in total yield, and is suitable for industrial production.
Inventors:
GUO WANCHENG (CN)
FANG JIE (CN)
WU HUAFANG (CN)
WANG GUOPING (CN)
FANG JIE (CN)
WU HUAFANG (CN)
WANG GUOPING (CN)
Application Number:
PCT/CN2021/135472
Publication Date:
August 04, 2022
Filing Date:
December 03, 2021
Export Citation:
Assignee:
AURISCO PHARAMCEUTICAL TIANJIN INC (CN)
YANGZHOU AURISCO PHARMACEUTICAL CO LTD (CN)
YANGZHOU AURISCO PHARMACEUTICAL CO LTD (CN)
International Classes:
C07D221/04
Foreign References:
| CN102066358A | 2011-05-18 | |||
| CN101955462A | 2011-01-26 | |||
| CN109988073A | 2019-07-09 |
Other References:
LEAHY DAVID K., FAN YU, DESAI LOPA V., CHAN COLLIN, ZHU JASON, LUO GUANGLIN, CHEN LING, HANSON RONALD L., SUGIYAMA MASANO, ROSNER : "Efficient and Scalable Enantioselective Synthesis of a CGRP Antagonist", ORGANIC LETTERS, vol. 14, no. 18, 21 September 2012 (2012-09-21), American Chemical Society, US, pages 4938 - 4941, XP055956188, ISSN: 1523-7060, DOI: 10.1021/ol302262q
Attorney, Agent or Firm:
XU&PARTNERS, LLC. (CN)
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