【文章名】SYNTHESIS OF 1,2,3,5-TETRAHYDRO-4,1-BENZOTHIAZEPINE-2-THIONE DERIVATIVES VIA CYCLIZATION OF 2-[(2-ISOTHIOCYANATOPHENYL)METHYLSULFANYL]ACETATES WITH SODIUM HYDRIDE
SYNTHESIS OF 1,2,3,5-TETRAHYDRO-4,1-BENZOTHIAZEPINE-2-THIONE DERIVATIVES VIA CYCLIZATION OF 2-[(2-ISOTHIOCYANATOPHENYL)METHYLSULFANYL]ACETATES WITH SODIUM HYDRIDE
[摘要]：A convenient method for the preparation of the title derivatives, 2-thioxo-1,2,3,5-tetrahydro-4,1-benzothiazepine-3-carboxylates and 2-alkylsulfany1-3,5-dihydro-4,1-benzothiazepine-3-carboxylates, has been developed. It is depends on cyclization of 2-[(2-isothiocyanatophenyemethylsulfanyl]acetates, generated in situ from the corresponding isocyanides on treatment with sulfur in the presence of a catalytic amount of selenium, using sodium hydride as a base. These isocyanides can be easily prepared from N-[(2-chloromethyl)phenyl]-formamides via an easy two-step sequence.
