FUSED PYRIMIDINE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF

摘要

This invention relates to a process for the preparation of new, optionally racemic or optically active fused pyrimidine derivatives of the general formula I (I) wherein m is 0 or 1; and if m = 0, then R is hydrogen or lower alkyl; R1 is hydrogen or R and R1 together form a group of the Formula -(CH=CH)2-in which case the dotted line is a further carbon-carbon bond while in all other cases between the positions linked by the dotted line there is only a single bond; R2 is hydrogen or hydroxy and R3 is hydrogen; or R2 is hydroxy and R3 is hydroxymethyl or R2 and R3 together form a valency bond; R6 is hydrogen; a phenyl group which may be optionally substituted by up to three atoms or groups selected from lower alkoxy, hydroxy, methylenedioxy, nitro, cyano, lower dialkylamino, lower alkanoylamino and halogen; trihalogenomethyl; a 5- or 6-membered monocyclic heteroaryl group containing one or two nitrogen atoms and/or 1 oxygen atom and which may be optionally substituted by lower alkyl or nitro; carboxy; or lower alkoxycarbonyl; R7 and R8 are hydrogen or together form a valency bond; R9 is hydrogen or hydroxy; R10 is hydrogen, phenyl, lower alkyl, carboxy, lower alkoxycarbonyl, cyano, methyliminomethyl, a carbamoyl group optionally substituted by one or two lower alkyl groups, a carboxylic acid hydrazido group, a group of the Formula -(CH2)q-COO-lower alkyl - wherein q is 1 or 2; or a group of the general Formula -CO-NH-N=R12 - wherein R12 is benzylidene, furfurylidene or nitrofurfurylidene; or R9 and R10 together form a group of the Formula -(CH2)p- wherein p = 3, 4, 5 or 6; n = 0 or 1 with the proviso that if n = 0, then R and R1 are hydrogen, R2 and R3 are hydrogen or together form a valency bond; R6 is phenyl or carboxy; R7 and R8 together form a valency bond; R9 is hydrogen and R10 is carboxy or lower alkoxycarbonyl; and if m = 1, then R is lower alkyl; R1 is hydrogen; R2 and R3 together form a valency bond; R4 and R5 together form a valency bond; R6 is phenyl or nitrophenyl; R7 and R8 together form a valency bond; R9 is hydrogen; R10 is carboxy or lower alkoxycarbonyl and n = 1. The new compounds possess valuable pharmaceutical properties, being especially effective against atherosclerosis, influencing not only the serum lipids, but also decreasing the quantity of the lipids and cholesterol deposited on the walls of the veins.