PROCESS FOR OBTAINING QUINAZOLINE DERIVATIVES

1460389 4-Substituted quinazoline cardiac stimulants PFIZER Ltd 24 July 1975 [25 July 1974 6 Jan 1975] 32805/74 and 416/75 Heading C2C The invention comprises novel compounds of the Formula I: wherein (i) R1 is a hydrogen atom or a lower alkyl group; (R2) n represents 1 to 3 optional substituents, each R2 being a hydroxy or lower alkoxy group, and n being 0 to 3, or any two of the moieties R2 constituting a methylenedioxy or ethylenedioxy group attached to adjacent positions of ring A; (ii) X represents -(CH 2 ) p - wherein p is 1 to 3, -CH=CH- or -CH 2 . CH=CH-; (iii) Y is attached to the 3- or 4-position of ring C and represents either: (a) a group of the formula -Z1-COR3 wherein Z1 is -CH 2 - or R3 is a lower alkyl group optionally substituted by an amino (as hereinbefore defined), hydroxy, lower alkoxy, aryl, or heteroaryl group; a lower alkenyl- or lower alkynyl-methyl group; a lower alkoxy group optionally substituted by an amino (as hereinbefore defined), aryl, heteroaryl, lower alkoxy or hydroxy group; an aryl group; an aryloxy group; or a heteroaryl group; and R4 is a hydrogen atom; a lower alkyl group optionally substituted by an amino (as hereinbefore defined), lower alkoxy, hydroxy, carbethoxy, aryl or heteroaryl group; a lower alkenyl- or lower alkynyl-methyl group; an aryl group or a heteroaryl group; (b) a group of the formula wherein R4 is as defined above and R5 is a group as defined for R3 above or is a group of the formula in which R7 is a hydrogen atom or a lower alkyl group and R6 is a group as defined for R4 above, or R6 and R7 taken together with the nitrogen atom to which they are attached form a saturated monocyclic heterocyclic ring; or, (c) a group of the formula wherein Z2 is Z1 or -O-, and R6 and R7 are as defined above, provided that when Z2 is R4 and R7 taken together may represent -(CH 2 ) 2 -, -(CH 2 ) 3 - or an o-phenylene group; and (iv) R is a hydrogen atom or a lower alkyl group attached to the same carbon atom as Y; provided that when X is -CH=CH- or -CH 2 CH=CH-, R is absent and Y is wherein R3, R6 and R' are as defined above, Y being attached to an unsaturated ring carbon atom; and their pharmaceutically acceptable acid addition salts. In the above compounds "lower" indicates up to 6 carbon atoms in the radical, aryl and heteroaryl include those radicals substituted by lower alkyl, lower alkoxy, hydroxy, halogen or acetamido, and "amino" means -NR 8 R 9 , wherein R 8 is H or lower alkyl, and R9 is H, lower alkyl, or