GB1115037A - Improvements in or relating to indolylethylamines - Google Patents

Abstract

Compounds of the general Formula I <FORM:1115037/C2/1> wherein R1 and R2 each represents a hydroxy or alkoxy group, n1 = 1 or 2, n2 = 0 or 1, R3 represents a hydrogen atom or C1- 4 alkyl group and R4 represents a hydrogen atom, a C1- 4 alkyl group or a group of the Formula Ia <FORM:1115037/C2/2> and their acid addition salts are prepared by standard methods, such as reacting a compound of the Formula V <FORM:1115037/C2/3> with a compound of the Formula VI <FORM:1115037/C2/4> in which formulae R11 and R21 have the same meanings as R1 and R2 in Formula I of the desired product or represent one or more etherified or esterified hydroxy groups which, after the reaction, is or are converted into a free hydroxy group or groups by hydrolysis or hydrogenolysis, R41 has the same meaning as R4 in Formula I or represents an aralkyl group which, after the reaction, is replaced by a hydrogen atom by catalytic reduction, and X represents a halogen atom, in which case n3 = 1, or a double-bonded oxygen atom, in which case n3 = 0 and R41 is a hydrogen atom, the intermediately formed Schiff base being converted into the amine of Formula I by reduction, optionally followed by salt formation. The preparation of o-(2-bromoethoxy)-anisole is described. The compounds of the invention have sedative, anticonvulsant, analgesic and hypotensive activity and some of then have adrenolytic activity. They may be administered in the form of pharmaceutical preparations containing them together with a carrier. Reference has been directed by the Comptroller to Specification 942,548.