Patent ID: 7288658

Claim:
A process for the manufacture of a compound of formula wherein R 1 and R 1′ are each independently hydrogen, lower alkyl, lower alkoxy, halogen, cyano or alkylamino; R 2 is —N(R 3 ) 2 , —N(R 3 )(CH 2 ) n OH, —N(R 3 )S(O) 2 -lower alkyl, —N(R 3 )S(O) 2 -phenyl, —N═CH—N(R 3 ) 2 , —N(R 3 )C(O)R 3 or a cyclic tertiary amine of the formula each R 3 is independently hydrogen, C 3 - 6 -cycloalkyl, benzyl or lower alkyl; R 4 is hydrogen, hydroxy, lower alkyl, —(CH 2 ) n COO-lower alkyl, —N(R 3 )CO-lower alkyl, hydroxy-lower alkyl, cyano, —(CH 2 ) n O(CH 2 ) n OH, —CHO or a 5-or 6 membered heterocyclic group that is optionally bonded via an alkylene group; wherein the process comprises the steps of a) reacting a compound of formula with a compound of formula wherein R 1 and R 1′ are as defined above, to a compound of formula wherein the substituents are as defined above; b) converting the OH/═O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group selected from the group consisting of POCl 3 , PBr 3 , MeI and (F 3 CSO 2 ) 2 O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate and R 1 and R 1′ are as defined above; c) substituting the leaving group P with the group R 2 by reacting compound XV with HR 2 to form a compound of formula wherein R 1 and R 1′ and R 2 are as defined above; and d) hydrolyzing the nitrile function of compound XVI in an acidic medium comprising H 2 SO 4 , HCl or acetic acid, to form a compound of formula wherein the definition of the substituents is given above.