method of preparation of new materials, the morphiname

摘要

1301243 Morphinan derivatives YAMANOUCHI PHARMACEUTICAL CO Ltd 4 June 1971 [20 June 1970 2 Feb 1971 9 Feb 1971] 19101/71 Heading C2C The invention comprises compounds of formula and their acid addition salts, wherein R is a C 1-5 aliphatic hydrocarbon group. These compounds are prepared by (1) heating in presence of acid a #SP4/SP-, #SP4a(5)/SP- or #SP4a(8a)/SP-octahydro-, or a 4-, 4a-, 5- or 8a-hydroxydecahydro-1-(alpha- RSP1/SP - p - methylbenzyl) - 2 - R - isoquinoline, wherein RSP1/SP is H, CONH 2 , CN or CO 2 H (possibly esterified), or (2) reacting I(R=H) with a compound introducing the N-hydrocarbyl group. Intermediates also prepared are I(R=CN); alpha-cyano- and -carbamyl-1-p-methylbenzyl- 5,6,7,8 - tetrahydroisoquinolines; the analogous carbamyl-methylbenzyl-2-methyl-1,2,3,4,5,6,7,8- octahydroisoquinoline; 1 - p - methylbenzyl- 1,2,5,6,7,8 - hexahydroisoquinoline and its 2- methyl-3,4-dihydro derivative. Therapeutic compositions for oral or parenteral administration comprise compounds of the above formula, which have antitussive activity.