Allenyl amines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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549 49, 549 51, 549 52, 549 53, 549 54, 549 55, 549 56, 549 58, A61K 3138, C07D33352

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active

051128527

ABSTRACT:
The present invention relates to allenyl amines, more specifically, .beta.-ethenylidene(substituted) ethanamines, possessing antihypertensive activity, and having the general formula ##STR1## wherein n is the integer 0, 1 or 2; each X independently is a substituent selected from the group consisting of loweralkyl, halo, --O--(loweralkyl), --S--(loweralkyl), --SO--(loweralkyl), --SO.sub.2 --(loweralkyl), CO.sub.2 R and CH.sub.2 OR, wherein R is loweralkyl and each loweralkyl group is from 1 to about 6 carbon atoms, or the pharmaceutically-acceptable addition salts thereof. These compounds are prepared by a novel reaction of a protected N,N-bis(trimethylsilyl)-4-methoxy-2-butynylamine compound with a metallo-organic compound, with subsequent removal of the silyl protecting groups to provide the desired compound.

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Claesson, A., and Sahlberg, C., Tetrahedron, 38(3), 363-8 (1982).
Sahlberg, C., Svante, B. R. Fagewall, I., Ask, A., and Claesson, A., J. Med. Chem. 26(7), 1036-42 (1983).

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