Manufacturing process for pyrimidine derivatives
The invention relates to processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of such solid forms for the therapeutic treatment of warm-blooded animals.
1. A process for manufacturing a compound of formula 5,
or a stereoisomer, tautomer, or a salt thereof, wherein,
W represents CH;
R 1 represents N-morpholinyl;
R 2 represents hydrogen;
R 3 represents trifluoromethyl;
R 4 represents hydrogen, comprising the step of reacting a compound of formula 4
wherein Y 2 B— represents an acyclic boronic acid, an acyclic boronic ester or a cyclic boronic ester, R 1 and R 2 are as defined for formula 5,
with a compound of formula 4a
wherein Hal represents halogen, W, R 3 and R 4 are as defined for a compound of formula 5,
under Suzuki conditions to obtain a compound of formula 5;
optionally followed by a salt forming reaction.
2. The process of claim 1 wherein the Suzuki conditions involve the presence of a Pd-catalyst Pd(dbpf)Cl 2 .