Patent ID: 6225465
Filing Date: 2001-05-01
Classification: C07D,Y02P

Abstract:
A process for preparing compounds of formula (I): ##STR14##whereinA.sup.1 is NR.sup.1 or CHR.sup.1 ;R.sup.1 is H, T--C.sub.1-6 alkyl, T--C.sub.1-6 oxoalkyl, T--C.sub.2-6 alkenyl, T--C.sub.3-4 oxoalkenyl, T--C.sub.3-4 oxoalkynyl, T--C.sub.3-4 alynyl, C.sub.3-6 cycloalkyl, Ar or Het, optionally subsituted by one or more of halo, --OR', --CN, --NR'.sub.2, --NO.sub.2, --CF.sub.3, --CO.sub.2 R', --CONR'.sub.2, Ar--C.sub.0-6 alkyl or Het-C.sub.0-6 alkyl, wherein T is H, C.sub.3-6 cycloalkyl, Het or Ar,R.sup.2 is CH.sub.2 CO.sub.2 R.sup.3 ;R.sup.3 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl or Ar--C.sub.0-4 alkyl;R.sup.5 is W--(CR'.sub.2).sub.q --Z--(CHR').sub.m, andR.sup.6 is H, C.sub.1-6 alkyl, Ar--C.sub.0-6 alkyl, Het-C.sub.0-6 alkyl, or C.sub.3-6 cycloalkyl-C.sub.0-6 alkyl, orR.sup.5 and R.sup.6 together form a 5- or six-membered Het ring which is substituted by W,W is R.sup.9 R""N--, R'R""NR'N--, R'R""NR'NCO--, R'.sub.2 NR'NC(.dbd.NR')--, R'ONR'C(.dbd.NR')--, ##STR15##R' is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl or Ar--C.sub.0-4 alkyl;R"" is R', --C(O)R' or --C(O)OR'"";R'"" is H, C.sub.1-6 alkyl or Ar--C.sub.0-4 alkyl;R.sup.7 is R', --CF.sub.3, --SR', or --OR';R.sup.8 is R', C(O)R', CN, NO.sub.2, SO.sub.2 R' or C(O)OR.sup.15 ;R.sup.9 is H, C.sub.1-6 alkyl, C.sub.3-7 cycloalkyl-C.sub.0-4 alkyl, Het-C.sub.0-4 alkyl or Ar--C.sub.0-4 alkyl;X is N.dbd.CR', C(O) or O;Y is absent, S or O;Z is (CH.sub.2).sub.t, Het, Ar or C.sub.3-7 cycloalkyl;q is 0 to 3;m is 0 to 2; andt is 0 to 2;which process comprises:reacting a compound of formula (II): ##STR16##whereinA.sup.1 and R.sup.2 are as defined above for formula (I); andR.sup.10 is Br, I, FSO.sub.3 --, ClSO.sub.3 -- or CF.sub.3 SO.sub.3 -;with a Pd catalyst, carbon monoxide and an amine of the formula (III) ##STR17##wherein R.sup.5 and R.sup.6 are defined as above in formula (I) except that any basic nitrogen group in R.sup.5 or R.sup.6 is protected, and thereafter removing any protecting groups.