Spasmolytic and hypotensive benzyl isoquinoline derivs. - prepd. e.g. by reacting phenylethyl phenyl:acetamide deriv. with phosphorus oxy:tri:chloride and dehydrogenating the resulting prod.

摘要

Benzylisoquinolines of formula (I):- and their acid-addition salts, except the 4-chlorophenoxy -iso-butyrates, are new. In (I) R and R1 are 3-5A alkyl when R=R1, or 1-5C alkyl when R and R1 are different, provided that when R is et and R1 is Me or when R is Ne and R1 is Et these cpds. are excluded). (I) are Spasmolytics and coronary and peripheral vasolidators with similar hypotensive and spasmolytic activity as papering but which decrease the pulse and the contractive force of the left ventricle so that the work load of the heart is reduced. A typical cpd., 6,7-diethoxy-1-(3,4-diisoprop-oxybenzyl) isoquinoline was prepd. in 31.6% yield by treating N- 2-(3,4-diethoxyphenyl)ethyl -3,4-diixopropoxy -phenylacetamide with POCl3 and dehydrogenating the prod with Pd/C.