Preparation method of selegiline hydrochloride isomer

• Main Authors: TIAN LEI, WANG ZHIBANG, BAI JUN, CAI YULEI, LIAO JIEHAI, WANG ZHE, CHENG JUN, PENG JIEWEI
• Format: Patent
• Language: Chinese; English
• Published: 09.06.2023
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The invention discloses a preparation method of a selegiline hydrochloride isomer, specifically, D-phenylalaninol is used as a raw material, and the selegiline hydrochloride S-isomer is prepared through cyclization, protection, ring opening, alkynylation, deprotection and methylation. Compared with the prior art, the raw material source is wide, the preparation process is easy to operate, the yield is high, and the method is suitable for industrial production. The HPLC purity of the intermediate in each step can be greater than or equal to 97% without complicated post-treatment; and the HPLC purity of the product can be more than 99.5% without recrystallization. 本发明公开了一种盐酸司来吉兰异构体的制备方法，具体的，以D-苯丙氨醇为原料，经环合、保护、开环、炔基化、脱保护、甲基化制得盐酸司来吉兰S-异构体，与现有技术相比，本发明使用的原料来源广泛，制备工艺操作简单，且收率高，无需复杂的后处理就可以使每步中间体的HPLC纯度≥97％；无需重结晶，就可使产物的HPLC纯度＞99.5％。