Title:
PREPARATION METHOD FOR S-CONFIGURATION PHENYLETHYLAMINE HYDROCHLORIDE COMPOUND
Document Type and Number:
WIPO Patent Application WO/2022/110612
Kind Code:
A1
Abstract:
The present invention relates to the technical field of the synthetic preparation for medicines, and relates to a preparation method for an S-configuration phenylethylamine hydrochloride compound. The preparation method comprises the following steps: step (1), performing a Friedel-Crafts reaction on m-dimethoxybenzene and acetyl chloride under a Lewis acid condition to generate an intermediate A; (2) reacting the intermediate A with hydroxylamine hydrochloride, without isolating the intermediate A, to generate an intermediate B; step (3), reducing the intermediate B under a reducing agent condition to obtain a compound C; step (4) resolving the compound C by means of an organic acid to obtain an organic salt of an S-configuration compound D; and step (5) dissociating the organic salt and then performing saltification to obtain a target product compound E. The preparation method of the present invention has the characteristics of simple purification, low cost, high efficiency, high yield and suitability for industrial mass production.
Inventors:
FENG YU (CN)
HUANG ZONGXI (CN)
YU ZHANGLI (CN)
LI SHOUXIN (CN)
TANG CHEN (CN)
ZHU TAO (CN)
QIAN WEI (CN)
XU HONG (CN)
HUANG ZONGXI (CN)
YU ZHANGLI (CN)
LI SHOUXIN (CN)
TANG CHEN (CN)
ZHU TAO (CN)
QIAN WEI (CN)
XU HONG (CN)
Application Number:
PCT/CN2021/086613
Publication Date:
June 02, 2022
Filing Date:
April 12, 2021
Export Citation:
Assignee:
CHENGDA PHARMACEUTICALS CO LTD (CN)
International Classes:
C07C213/08; C07C213/10; C07C217/58
Foreign References:
| CN112457204A | 2021-03-09 | |||
| CN107954882A | 2018-04-24 |
Other References:
SZYMON KLOSSOWSKI ET AL.: "Chemoenzymatic synthesis and application of a new, easily cleavable chiral auxiliary for the synthesis of peptidomimetics via an Ugi reaction", TETRAHEDRON ASYMMETRY, vol. 25, no. 5, 27 March 2014 (2014-03-27), XP028604719, ISSN: 0957-4166, DOI: 10.1016/j.tetasy.2014.01.016
Attorney, Agent or Firm:
BEIJING KEYI INTELLECTUAL PROPERTY FIRM (CN)
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