Title:
METHOD FOR PRODUCING INTERMEDIATE OF IGURATIMOD DERIVATIVES, METHOD FOR PRODUCING IGURATIMOD, IGURATIMOD HAVING NOVEL CRYSTAL STRUCTURE, AND METHOD FOR PRODUCING SAME
Document Type and Number:
WIPO Patent Application WO/2021/020481
Kind Code:
A1
Abstract:
The present invention is a method for producing an intermediate of iguratimod derivatives, a method for producing iguratimod, iguratimod having a novel crystal structure, and a method for producing the same. The present invention can raise the production efficiency of iguratimod derivatives by raising the yield and purity in individual production steps, and can provide: iguratimod crystals having a novel crystal form that have a reduced L-methyl form content, are less susceptible to becoming charged, and are exceptionally easy to handle; and a method for producing the iguratimod crystals.
Inventors:
HAYASHI YUKI (JP)
MORI HIROYUKI (JP)
MATSUURA KEISUKE (JP)
YOKOO YOSHIHIRO (JP)
YOSHIDA SHOTA (JP)
MORI HIROYUKI (JP)
MATSUURA KEISUKE (JP)
YOKOO YOSHIHIRO (JP)
YOSHIDA SHOTA (JP)
Application Number:
PCT/JP2020/029163
Publication Date:
February 04, 2021
Filing Date:
July 29, 2020
Export Citation:
Assignee:
TOKUYAMA CORP (JP)
International Classes:
A61P19/02; A61K31/352; A61K31/353; A61P29/00; A61P37/02; A61P37/08; C07C41/01; C07C43/267; C07C303/40; C07C311/03; C07C311/08; C07D311/22
Foreign References:
| CN107021891A | 2017-08-08 | |||
| CN106986797A | 2017-07-28 |
Other References:
LIU JIWEN, FU ZICE, WANG YINGCAI, SCHMITT MIKE, HUANG ALAN, MARSHALL DEREK, TONN GEORGE, SEITZ LISA, SULLIVAN TIM, LUCY TANG H., C: "Discovery and optimization of CRTH2 and DP dual antagonists", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 19, no. 22, 17 September 2009 (2009-09-17), pages 6419 - 6423, XP026703820
BZEIH TOURIN, LAMAA DIANA, FRISON GILLES, HACHEM ALI, JABER NADA, BIGNON JEROME, RETAILLEAU PASCAL, ALAMI MOUAD, HAMZE ABDALLAH: "Csp2–Csp2 and Csp2–N Bond Formation in a One-Pot Reaction between N-Tosylhydrazones and Bromonitrobenzenes: An Unexpected Cyclization to Substituted Indole Derivatives", ORGANIC LETTERS, vol. 19, no. 24, 5 December 2017 (2017-12-05), pages 6700 - 6703, XP55788000
BZEIH TOURIN, LAMAA DIANA, FRISON GILLES, HACHEM ALI, JABER NADA, BIGNON JEROME, RETAILLEAU PASCAL, ALAMI MOUAD, HAMZE ABDALLAH: "Csp2–Csp2 and Csp2–N Bond Formation in a One-Pot Reaction between N-Tosylhydrazones and Bromonitrobenzenes: An Unexpected Cyclization to Substituted Indole Derivatives", ORGANIC LETTERS, vol. 19, no. 24, 5 December 2017 (2017-12-05), pages 6700 - 6703, XP55788000
Attorney, Agent or Firm:
TAGUCHI, Masahiro et al. (JP)
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