Title:
METHOD FOR SYNTHESIZING 8-AMINO-1-{[2-(TRIMETHYLSILYL)ETHOXY]METHOXY}OCTANE-3-ONE
Document Type and Number:
WIPO Patent Application WO/2023/071328
Kind Code:
A1
Abstract:
Disclosed is a method for synthesizing 8-amino-1-{[2-(trimethylsilyl)ethoxy]methoxy}octane-3-one, which belongs to the technical field of pharmaceutical chemical synthesis. The method comprises the steps of: firstly, protecting diphenylmethylamine with N-Boc, and then reacting the protected diphenylmethylamine with sodium hydride to prepare a sodium salt intermediate thereof, and subjecting the sodium salt intermediate and 1,5-dibromopentane to a substitution reaction to obtain intermediate-1; preparing the intermediate-1 into a zinc bromide intermediate, then reacting the zinc bromide intermediate with methyl 3-{[2-(trimethylsilyl)ethoxy]methoxy}propionate to produce intermediate-2, and subjecting the intermediate-2 to a catalytic hydrogenation deprotection reaction to obtain the lipoic acid intermediate 8-amino-1-{[2-(trimethylsilyl)ethoxy]methoxy}octane-3-one. The present technique has mild process conditions, the raw materials are easily available, the purity of each intermediate is high, the quality control and improvement of bulk drug production are facilitated and the method is suitable for industrial production.
Inventors:
WU LEI (CN)
QIAN XIANGYUN (CN)
ZHANG XIAOHONG (CN)
ZENG LING (CN)
QIAN XIANGYUN (CN)
ZHANG XIAOHONG (CN)
ZENG LING (CN)
Application Number:
PCT/CN2022/107743
Publication Date:
May 04, 2023
Filing Date:
July 26, 2022
Export Citation:
Assignee:
SUZHOU FUSHILAI PHARMACEUTICAL CO LTD (CN)
International Classes:
C07F7/08; C07C269/04; C07C271/14; C07F3/06
Foreign References:
| CN113717210A | 2021-11-30 | |||
| CN113429386A | 2021-09-24 | |||
| CN112469279A | 2021-03-09 | |||
| CN113185494A | 2021-07-30 |
Attorney, Agent or Firm:
JJS INTELLECTUAL PROPERTY AGENCY LTD. (CN)
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