PROCESS FOR PREPARATION OF CALCIUM ANTAGONISTICS

摘要

The present invention is directed to a new class of cyclic guanidines of the formula: in which Q is represented by a substituent selected from the group consisting of (CH2)n in which n is an integer from 2-10, A is a substituent selected from the group consisting of -NH-(CH2)m in which m is an integer from 0-5, a piperidino substituent, or a piperazino substituent; both Ar and Ar1 are each independently represented by a phenyl ring, each of which may be optionally substituted with up to 3 substituents, each selected from the group consisting of halogen, alkyl, alkoxy, hydroxy, and trifluoromethyl; and R is represented by either hydrogen or an alkyl; R1 is represented by hydrogen or an alkyl; the tautomers, and optical isomers thereof; and the pharmaceutically acceptable acid addition salts thereof; with the provisos that: 1) when Q is represented by (CH2)2,3,or 4 , then A is not represented by NH-(CH2)o; and 2) when Q is represented by (CH2)2 and R is an alkyl; then A is not NH-(CH2), and to their use as calcium antagonists.