Abstract: The present invention relates to resolution of (cis,trans)5,6-dihydro-4H-4-ethylamino-6-methylthieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide using dibenzoyl-L-tartaric acid monohydrate or di-p-toluoyl-L-tarrtaric acid monohydrate as a chiral resolving agent in presence of methanol to obtain hemitartarate salt, purifying it to obtain hemitartarate salt of 5,6-dihydro-4H-4(S)-ethylamino-6(S)methylthieno[2,3-b]thiopyran-2-sulfonamide-7,7-dioxide with de of >99%, Chemical purity >99.5% with cis isomer content of <0.1% and further converting into its pharmaceutically acceptable salts, preferably hydrochloride salt.
Abstract: The present invention discloses novel compounds of the Formula (1), comprising benzothiazinone, benzoxazinone or benzoxazolinone moieties having antifungal activity, method for preparing these compounds and the use of these compounds as antifungal agents in prevention and treatment of fungal infections, and pharmaceutical preparations containing these novel compounds.
Type:
Grant
Filed:
October 16, 2009
Date of Patent:
March 6, 2012
Assignees:
Council of Scientific & Industrial Research;, FDC Ltd.
Abstract: The present invention relates to resolution of (cis, trans) 5,6-dihydro-4H-4-ethylamino-6-methylthieno[2,3-b] thiopyran-2-sulfonamide-7,7-dioxide using dibenzoyl-L-tartaric acid monohydrate or di-p-toluoyl-L-tarrtaric acid monohydrate as a chiral resolving agent in presence of methanol to obtain hemitartarate salt, purifying it to obtain hemitartarate salt of 5,6-dihydro-4 H-4 (S)-ethyl amino-6(S) methylthieno [2,3-b] thiopyran-2-sulfonamide-7,7-dioxide with de of >99% , Chemical purity >99.5% with cis isomer content of <0.1% and further converting into its pharmaceutically acceptable salts, preferably hydrochloride salt.