Patent ID: 6727360
Filing Date: 2004-04-27
Classification: C07C,C07D,Y10S

Abstract:
A process for the preparation of a compound of formula (VI): or a pharmaceutically acceptable salt form thereof;wherein:r is an integer from 0 to 4; R1 is independently selected at each occurrence from the group consisting of: H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C6 cycloalkyl, C4-C12 cycloalkylalkyl, â€”NR1cR1d, â€”OR1e, and â€”SR1e; R1c and R1d are independently selected at each occurrence from the group consisting of: H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C6 cycloalkyl and C4-C12 cycloalkylalkyl; alternatively, R1c and R1d are taken together to form a heterocyclic ring selected from the group consisting of: piperidine, pyrrolidine, piperazine, N-methylpiperazine, morpholine and thiomorpholine, each heterocyclic ring optionally substituted with 1-3 C1-C4 alkyl groups; R1e is selected from the group consisting of: H, C1-C10 alkyl, C3-C6 cycloalkyl, and C4-C6 cycloalkylalkyl; R2 is selected from the group consisting of: H, C2-C4 alkenyl, C2-C4 alkynyl, C3-C6 cycloalkyl, C4-C10 cycloalkylalkyl, C1-C4 hydroxyalkyl, C1-C4 haloalkyl, and C1-C4 alkyl substituted with 0-5 R2a; R2a is independently selected at each occurrence from the group consisting of: H, C1-C10 alkyl, C2-C10 alkenyl, C2-C10 alkynyl, C3-C6 cycloalkyl, C4-C12 cycloalkylalkyl, halo, CN, C1-C4 haloalkyl, â€”OR2e, and â€”SR2e; and R2e is independently selected at each occurrence from the group consisting of: H, C1-C10 alkyl, C3-C6 cycloalkyl, and C4-C6 cycloalkylalkyl; the process comprising reacting a compound of formula (IV): with a compound of formula (V): in the presence of [1,1â€²-Bis(diphenylphosphino)ferrocene] palladium (II) chloride, sodium bicarbonate and a suitable solvent to give a compound of formula (VI).