Patent · US Active

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

US8614337B2 · kind B2 · utility

1Cited by

5References

21Claims

0Family size

Assignee

2Y-CHEM, LTD. · CN

Inventors

Xungui He · Shanghai, CN
Jianping Guo · Shanghai, CN
Yanling Wang · Xi'an, CN
Wensheng Tang · Shanghai, CN
Xingzhong Zhang · Shanghai, CN
Xuezhang Wang · Shanghai, CN
Yuan Wang · Beijing, CN

Key dates

Filing date	Sep 7, 2010
Grant date	Dec 24, 2013
Priority date	—
Expiry date	Sep 7, 2030

Classification

Technology area (CPC C)Chemistry; Metallurgy
CPC primaryC07B57/00
WIPO fieldOrganic fine chemistry
WIPO sectorChemistry

Abstract

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′-(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′-(thien-2-yl-)ethyl-tetralin-2-amine, which is then dissociated to obtain S-5-substituted-N-2′-(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).

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.