氢溴酸依托唑啉的一种新颖且实用的不对称合成方法。
A novel and practical asymmetric synthesis of eptazocine hydrobromide.
作者信息
Li Ruipeng, Liu Zhenren, Chen Liang, Pan Jing, Lin Kuaile, Zhou Weicheng
机构信息
State Key Lab of New Drug & Pharmaceutical Process, Shanghai Key Lab of Anti-Infectives, Shanghai Institute of Pharmaceutical Industry, China State Institute of Pharmaceutical Industry, No. 285, Gebaini Rd., Shanghai 201203, P. R. of China.
出版信息
Beilstein J Org Chem. 2018 Sep 6;14:2340-2347. doi: 10.3762/bjoc.14.209. eCollection 2018.
In order to prepare eptazocine hydrobromide effectively, a novel, mild and practical asymmetric process was developed starting from 1-methyl-7-methoxy-2-tetralone under the catalysis of -(-trifluoromethylbenzyl)cinchonidinium bromide. The reaction conditions were optimized to obtain the product in excellent overall yield and purity.
为了有效地制备氢溴酸依他佐辛，以1-甲基-7-甲氧基-2-四氢萘酮为起始原料，在-(-三氟甲基苄基)辛可尼定溴化物的催化下，开发了一种新颖、温和且实用的不对称合成方法。对反应条件进行了优化，以优异的总收率和纯度获得产物。
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