2y-chem, Ltd.

Xingzhong Zhang

Lei Zhang

Xungui He

Yanling Wang

Wensheng Tang

Jianping Guo

Xuezhang Wang

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). 

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Shanghai, China

Xingzhong Zhang