96125-57-4

Upstream product

• 4584-46-7 (2-chloroethyl)dimethylamine hydrochloride 
• 96125-56-3 (-)-cis-2-(4-methoxyphenyl)-3-hydroxy-8-chloro-2,3-dihydro-1,5-benzothiazepin-4(5H)-one 

Downstream Products

• 96125-59-6 (-)-(2R,3R)-cis-3-acetoxy-8-chloro-5-<2-(dimethylamino)ethyl>2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one hydrochloride 
• 110284-22-5 (-)-(2R,3R)-cis-3-acetoxy-8-chloro-5-<2-(dimethylamino)ethyl>2,3-dihydro-2-(4-methoxyphenyl)-1,5-benzothiazepin-4(5H)-one 

Relevant academic research and scientific papers

1,5-benzothiazepine derivatives and preparation thereof

Novel 1,5-benzothiazepine derivatives of the formula: STR1 wherein X is hydrogen atom, a halogen atom or a lower alkyl group; R1 is a lower alkyl group or a lower alkoxy group; R2 is hydrogen atom, a lower alkyl group, a substituted

Synthesis of Halogen-Substituted 1,5-Benzothiazepine Derivatives and Their Vasodilating and Hypotensive Activities

In an attempt to improve the effectiveness and duration of the action of diltiazem (1), a 1,5-benzothiazepine calcium channel blocker, its derivatives (2) with halogen substituents on the fused benzene ring were synthesized.These compounds were evaluated for their effects on vertebral and coronary blood flows and antihypertensive activity.The structure-activity relationships are discussed.The 8-chloro derivative ((+)-2b), the most potent compound in this series, was selected for clinical evaluation as a cerebral vasodilating and antihypertensive agent.

8-Chloro-1,5-benzothiazepine derivatives

Novel 8-chloro-1,5-benzothiazepine derivatives of the formula: STR1 wherein R1 is hydrogen, lower alkyl or a group of the formula: R4 CO--, each of R2 and R3 is lower alkyl and R4 is hydrogen or lower alkyl, and a pharmaceutically acceptable acid addition salt thereof are disclosed. Said derivative (I) and a pharmaceutically acceptable acid addition salt thereof are useful as hypotensive agents and/or coronary or cerebral vasodilators.