首页> 外国专利> AN IMPROVED PROCESS FOR THE PREPARATION OF 5,6 -DIHYDRO -4H-4(S)-ETHYLAMINO-6(S)-METHYLTHIENO2,3-B THIOPYRAN-2-SULFONAMIDE- 7,7 -DIOXIDE AND ITS SALT

AN IMPROVED PROCESS FOR THE PREPARATION OF 5,6 -DIHYDRO -4H-4(S)-ETHYLAMINO-6(S)-METHYLTHIENO2,3-B THIOPYRAN-2-SULFONAMIDE- 7,7 -DIOXIDE AND ITS SALT

机译:改进的5,6-二氢-4H-4(S)-乙基氨基-6(S)-甲基硫代[2,3-B]硫吡喃-2-磺酰胺-7,7-二氧化物及其盐的制备方法

摘要

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 usingdibenzoyl -L- tartaric acid monohydrate or di-p-toluoyl-L-tarrtaric acidmonohydrate as a chiral resolving agent in presence of methanol to obtainhemitartarate salt, purifying it to obtain hemitartarate salt of 5,6-dihydro-4H-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 of0.1 % and further converting into its pharmaceutically acceptable salts,preferably hydrochloride salt.
机译:本发明涉及(顺式,反式)5,6-二氢-4H-4-的拆分乙氨基-6-甲基噻吩并[2,3-b]硫吡喃-2-磺酰胺-7,7-二氧化物使用二苯甲酰基-L-酒石酸一水合物或二对甲苯甲酰基-L-酒石酸一水合物作为手性拆分剂,在甲醇存在下获得纯化半乳糖精盐,得到5,6-二氢-4的半乳糖精盐H-4(S)-乙基氨基-6(S)甲基噻吩并[2,3-b]硫吡喃-2-磺酰胺-7,7-de> 99%的二氧化碳,化学纯度> 99.5%,顺式异构体含量为<0.1%,并进一步转化为其可药用盐,优选盐酸盐。

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