SYNTHESIS OF AMINE SUBSTITUTED 4,5,6,7-TETRAHYDROBENZOTHIAZOLE COMPOUNDS

摘要

The present invention is related to an improved process for the preparation of amino-substituted 4,5,6,7-tetrahydrobenzothiazole compounds of formula I, such as the compound 2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention further relates to an improved synthesis of (R)-2-amino-4,5,6,7-tetrahydro-6-(n-propylamino)benzothiazole. The invention also relates to the methods and intermediates associated with the synthetic process.

主权项

1. A process for preparing a compound of formula I(HOTs) wherein R1 and R2 are each independently hydrogen or C1-6 alkyl, wherein each C1-6 alkyl is optionally and independently substituted with up to 3 occurrences of C1-6 alkyl, aryl or heteroaryl; the process comprising contacting a mixture, which comprises a compound of formula IIand a solvent, with a compound having the formulain the presence of a base, to provide a compound of formula I(HOTs), wherein the solvent is acetonitrile, a mixture of acetonitrile and water, IPA, a mixture of IPA and water, a mixture of acetonitrile and IPA, or a mixture of acetonitrile, IPA and water.