Synthesis of 6-aryl-4-aminopicolinate and 2-aryl-6-aminopyrimidine-4-carboxylate by direct Suzuki coupling

摘要

Amino-3-chloro-6- (4-chloro-2-fluoro-3-methoxyphenyl) pyridine-2-carboxylate, And 4-amino-3-chloro-5-fluoro-6- (4-chloro-2-fluoro-3- Lt; / RTI The improved method eliminates the protection / deprotection steps in current chemical processes, thus eliminating or reducing the direct Suzuki coupling step with various raw materials, equipment and cycle times eliminated or reduced, as well as variations in other process conditions, Use of ABA-diMe and changes in pH, catalyst concentration, solvent composition and / or post-treatment procedure. The present invention has been extended to include the synthesis of 2-aryl-6-aminopyrimidine-4-carboxylate.