Title:
METHOD FOR PREPARING OPTICALLY ACTIVE ELIGLUSTAT
Document Type and Number:
WIPO Patent Application WO/2020/020365
Kind Code:
A1
Abstract:
The present invention involves a method for isolating, by means of salt formation and resolution, a single optically active N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide as shown in formula (III) from four stereoisomers of N-[2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide as shown in formula (I); specifically, a method for isolating N-[(1R,2R)-2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide from an enantiomeric (RR,SS)N-[2-(2,3-dihydro-1,4-benzodioxan-6-yl)-2-hydroxy-1-(1-pyrrolidinylmethyl)ethyl]octanamide, by means of optical resolution by using a tartaric acid derivative or 4-hydroxydinaphtho[2,1-D: 1',2'-F][1,3,2]dioxaphosphepin-4-oxide or a derivative thereof, in particular D-(+)-di-p-methylbenzoyltartaric acid and (-)-4-hydroxydinaphtho[2,1-D: 1',2'-F][1,3,2]dioxaphosphepin-4-oxide, as a resolving agent.
Inventors:
FENG WENHUA (CN)
DU JIANXUN (CN)
TAO JIAYI (CN)
KONG DELONG (CN)
MA CHUNYING (CN)
CHU WEIMING (CN)
ZHANG MENGMENG (CN)
DU JIANXUN (CN)
TAO JIAYI (CN)
KONG DELONG (CN)
MA CHUNYING (CN)
CHU WEIMING (CN)
ZHANG MENGMENG (CN)
Application Number:
PCT/CN2019/097988
Publication Date:
January 30, 2020
Filing Date:
July 26, 2019
Export Citation:
Assignee:
INST MATERIA MEDICA CAMS (CN)
International Classes:
C07D319/18; C07B57/00
Domestic Patent References:
| WO2016166170A1 | 2016-10-20 |
Foreign References:
| CN105646442A | 2016-06-08 | |||
| CN106967042A | 2017-07-21 |
Attorney, Agent or Firm:
SHANGCHENG & PARTNERS (CN)
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