Synthesis of [1,5]benzothiazepine Derivatives

Various derivatives of 2,3-dihydro[1,5]benzothiazepin-4(5H)-ones were synthesized. Alternative route for the synthesis of 5-dimethylaminoethyl-2,3-dihydro[1,5]benzothiazepin-4(5H)-ones and 4-dimethylamionpropoxy-(2H,5H)-[1,5]benzothiazepines are described

Synthesis of Trans-thienyl-3-ethoxycarbonyl-2,3-dihydro[1,5]benzothiazepin-4(5h)-ones

A series of trans-thienyl-3-ethoxycarbonyl-2,3-dihydro[1,5]benzothiazepin-4(5H)-ones 6-8 was synthesized from thienylmethylidenemalonates 3a-3c and 2-aminobenzenethiol 3d in the presence of triethylamine hydrochloride at 160-degrees. The [1,5]benzothiazepines 6-8 were alkylated using 2-dimethylaminochloroethane, 3-dimethylaminochloropropane and 3-(N-piperidino)chloropropane in order to obtain the corresponding 5-aminoalkylbenzothiazepinones 9-14

A Novel Synthesis of Methyl Cis-(3-thienyl)glycidate With 2-aminothiophenol and the Synthesis of [1,5]benzothiazepine Derivatives

The synthesis of cis-2,3-dihydro-3-hydroxy-2-(3-thienyl)[1,5]benzothiazepin-4-(5H)-one derivatives is described starting from 2-aminothiophenol and methyl cis-(3-thienyl)glycidate. The structures were confirmed by H-1-nmr spectroscopy