Synthesis of the Optically Active trans-Isomers of Diltiazem and Their Cardiovascular Effects and Ca-Antagonistic Activity.

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Abstract
Optically active trans-isomers of diltiazem were synthesized and their cardiovascular effects were evaluated in anesthetized dogs and in isolated guinea pig hearts.Both (+)-2 (2R, 3S) and (-)-2 (2S, 3R) were much less active than diltiazem (1, 2D, 3S) with short duration of action. No substantial enantiomeric difference in activity was seen between them. Their Ca-antagonistic activities on Ca2+-induced contractions in K+ -depolarized canine basilar arteries were also examined.Absolute stereochemistry of (+)-2 was determined to be 2R, 3S by X-ray crystallographic analysis.

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