Title:
PREPARATION METHOD FOR ANTI-CANCER DRUG LANOSTEROL DERIVATIVE
Document Type and Number:
WIPO Patent Application WO/2018/214327
Kind Code:
A1
Abstract:
The present invention pertains to the technical field of drug synthesis and relates to a preparation method for a novel anti-cancer drug lanosterol derivative. In the method, lanosterol is used as a starting material to produce an intermediate LD-a through protection by tert-Butyldimethylsilyl (TBS), the intermediate LD-a undergoes a Sharpless asymmetric double hydroxylation reaction under the action of osmium tetroxide (OsO4) to produce a vicinal diol compound LD-b, the compound LD-b undergoes Swern oxidation under alkaline conditions of triethylamine to produce an α-hydroxyketone compound LD-c, LD-c is acylated with acetic anhydride to obtain an intermediate LD-d, LD-d undergoes TBS deprotection to obtain an intermediate LD-e, and finally the intermediate LD-e is epoxidized to give a target lanosterol derivative LD. The present invention has relatively mild reaction conditions in the preparation steps and short synthesis steps, avoids the use of highly toxic or expensive reagents, produces a product with high purity, and can be used for industrial production.
Inventors:
XIE WEIDONG (CA)
Application Number:
PCT/CN2017/100112
Publication Date:
November 29, 2018
Filing Date:
September 01, 2017
Export Citation:
Assignee:
INSTITUTE OF DONGGUAN SUN YAT SEN UNIV (CN)
RUKING BIOTECH LTD (CN)
RUKING BIOTECH LTD (CN)
International Classes:
C07J75/00; A61K31/58; A61K31/695; A61P35/00
Foreign References:
| CN103204898A | 2013-07-17 | |||
| CN105377372A | 2016-03-02 |
Attorney, Agent or Firm:
BEI&OCEAN (CN)
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