Method for the preparation of tertiary amines, a compound useful therefor and alpha-2-receptor active tetrahydroisoquinoline derivatives

摘要

The invention relates to the preparation of teriatry amines of the formula (V) where R is alkyl and R6 and R7 are alkyl groups which are optionally substituted or where R6 and R7 form a ring or ring system, via a substrate which is a compound of the formula (I) wherein Y is the fraction of a solid or soluble support, where Y may include a residue of a functional group having been attached to said support, said functional group having been hydroxy, amino, thio, epoxy or halogen, R1 is aryl, heteroaryl, alkyl chain or a ring or ring system, which may include a heteroatom, or R1 is nothing, and R2 is vinyl; CH2CH2X, where X is halogen; or R3C=CHR4 or R3CH-CH2R4X, where R3 and R4 are the same or different and are alkyl, acyl, carbonyl, cyano or nitro groups and X is halogen. The invention particularly relates to the preparation of alpha-2-receptor active tetrahydroisoquinoline derivatives.