Patent ID: 6849649

Claim:
A process for the preparation of a compound of general formula I wherein R 1 , X and Y are as defined below comprising the steps of: a) reacting a compound of formula II wherein Prot is a suitable protecting group, with a compound of formula III Y—X—NH 2 (III) to give a compound of formula IV; then b) reacting compound of formula IV under suitable deprotecting conditions to give the compound of formula I wherein R 1 is C 1-6 alkyl which may be substituted by one or more substituents, which may be the same or different, selected from the list: halo, hydroxy, C 1-6 alkoxy, hydroxyC 1-6 alkoxy, C 1-6 alkoxyC 1-6 alkoxy, carbocyclyl, carbocyclyloxy, C 1-4 alkoxycarbocyclyloxy, heterocyclyl, heterocyclyloxy, —NR 2 R 3 , —NR 4 COR 5 , —NR 4 SO 2 R 5 , —CONR 2 R 3 , —S(O) p R 6 , —COR 7 and —CO 2 (C 1-4 alkyl); or R 1 is carbocyclyl or heterocyclyl, each of which may be substituted by one or more substituents from said list, which substituents may be the same or different, which list further includes C 1-6 alkyl; or R 1 is hydrogen, C 1-6 alkoxy, —NR 2 R 3 or —NR 4 SO 2 R 5 ; wherein R 2 and R 3 , which may be the same or different, are carbocyclyl or heterocyclyl (each of which may be substituted by C 1-4 alkyl, hydroxy or C 1-4 alkoxy); or are hydrogen or C 1-4 alkyl; or R 2 and R 3 together with the nitrogen to which they are attached form a pyrrolidinyl, piperidino, morpholino, piperazinyl or N—(C 1-4 alkyl)piperazinyl group; R 4 is hydrogen or C 1-4 alkyl; R 5 is C 1-4 alkyl, CF 3 , carbocyclyl, C 1-4 alkylcarbocyclyl, C 1-4 alkoxycarbocyclyl, heterocyclyl, C 1-4 alkoxy or —NR 2 R 3 ; R 6 is C 1-4 alkyl, carbocyclyl, heterocyclyl or NR 2 R 3 ; and R 7 is C 1-4 alkyl, carbocyclyl or heterocyclyl; p is 0, 1, 2 or 3; X is the linkage —(CH 2 ) n — or —(CH 2 ) q —O— (wherein Y is attached to the oxygen); wherein one or more hydrogen atoms in linkage X may be replaced independently by C 1-4 alkoxy; hydroxy; hydroxyC 1-3 alkyl; C 3-7 cycloalkyl; carbocyclyl; heterocyclyl; or by C 1-4 alkyl optionally substituted by one or more fluoro or phenyl groups; n is 3, 4, 5, 6 or 7; and q is 2, 3, 4, 5 or 6; and Y is phenyl or pyridyl, each of which may be substituted by one or more groups R 8 which may be the same or different, wherein R 8 is hydroxy; mercapto; halogen; cyano; acyl; amino; mono(C 1-4 alkyl)amino; di(C 1-4 alkyl)amino; carbocyclyl or heterocyclyl (either of which is optionally substituted by C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio or halogen); C 1-6 alkoxy; phenoxy; C 1-6 alkylthio; phenylthio; or alkyl optionally substituted by C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio, halogen or phenyl; or two R 8 groups on adjacent carbon atoms together with the interconnecting carbon atoms may form a fused 5- or 6-membered carbocyclic or heterocyclyic ring, optionally substituted by C 1-6 alkyl, haloC 1-6 alkyl, C 1-6 alkoxy, haloC 1-6 alkoxy, C 1-6 alkylthio or halogen; then c) optionally forming a salt.