105487-93-2Relevant academic research and scientific papers
A new synthetic route to 1,5-benzothiazepines. Synthesis of derivatives of diltiazem
Harada,Morimoto,Nagasawa,Takamura,Inoue,Oh-Ihsi,Takeda
, p. 1986 - 1989 (2007/10/02)
Several derivatives of diltiazem (9a-c) have been synthesized from the oxamate (6) through the carbon-carbon ring closure of the sulfur-stabilized benzylic anion and the ester carbonyl group, followed by stereoselective reduction of the C3-carb
Synthesis of Halogen-Substituted 1,5-Benzothiazepine Derivatives and Their Vasodilating and Hypotensive Activities
Inoue, Hirozumi,Konda, Mikihiko,Hashiyama, Tomiki,Otsuka, Hisao,Takahashi, Kaoru,et al.
, p. 675 - 687 (2007/10/02)
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.
