Contravir Pharmaceuticals, Inc.

Chemagis Ltd.

2y-chem, Ltd.

Yanling Wang

Lei Zhang

Xungui He

Jie Li

Chuanjun Liu

Jirang Zhu

Qingzhong Cheng

Mingyong Yuan

Joseph Kaspi

Michael Brand

Wensheng Tang

Jianping Guo

Xuezhang Wang

Xingzhong Zhang

Yuang Wang

Yuan Wang

The invention is directed to processes for synthesizing bicyclic nucleoside antiviral compounds and for synthesizing the intermediates used in the process. The invention is also directed to novel intermediate compounds useful in the process. The antiviral compounds are useful in the treatment of herpes zoster (i.e., varicella zoster virus, VZV, shingles) and for the prevention of post herpetic neuralgia (PHN) resulting from this viral infection.

Method of preparation of antiviral compounds and useful intermediates thereof

The chiral compound S-5-substituted-N-2'-(thienyl-2-yl-)ethyl-tetralin-2-amine or its chiral acid salts and preparation method thereof are disclosed, and the method for preparing Rotigotine by using the chiral compound is also disclosed. Racemic 5-substituted-N-2&#x2032;-(thien-2-yl-)ethyl-tetralin-2-amine (compound 1) is resolved by using a conventional chiral acid to obtain an optically pure chiral acid salt of S-5-substituted-N-2&#x2032;-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2&#x2032;-(thien-2-yl-)ethyl-tetralin-2-amine (compound 2). The compound 2 or chiral acid salt thereof is alkylated and deprotected to produce rotigotine (compound 5). 

S-5-substituent-N-2'-(thiophene-2-yl)ethyl-tetralin-2-amine or chiral acid salts thereof and use for preparing Rotigotine

The present invention provides a novel montelukast intermediate and a simple and straightforward process for preparing it. According to the present invention, by using this intermediate and the process, essentially as described herein, montelukast acid and salts thereof are obtained.

Process for preparing 1-(mercaptomethyl)cyclopropaneacetic acid, a useful intermediate in the preparation of montelukast and salts thereof

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Shanghai, China

Yanling Wang