Patent ID: 9598396
Date: 2017-03-21
CPC Classifications: A61K,A61P,C07D

Claim:
1. A process for preparing a compound of formula (I), including a stereochemically isomeric form thereof; wherein Y is CH R1 is aryl or Het; wherein aryl is phenyl or naphthalenyl; wherein Het is thienyl, pyrrolyl, pyrrolinyl, oxazolyl, thiazolyl, imidazolyl, pyrazolyl, isoxazolyl, isothiazolyl, oxadiazolyl, triazolyl, tetrazolyl, thiadiazolyl, furanyl, piperidinyl, pyridinyl, pyridazinyl, pyrimidinyl, piperazinyl, pyrazinyl, triazinyl, indolizinyl, azaindolizinyl, indolyl, indolinyl, benzothienyl, indazolyl, benzoxazolyl, benzimidazolyl, benzofuranyl, benzothiazolyl, benzotriazolyl, chromanyl, purinyl, quinolinyl, cinnolinyl, phthalazinyl, quinazolinyl, quinoxazolinyl, naphthyridinyl or pteridinyl; two carbon atoms on aryl or Het can be bridged (i.e. forming a bi- or tricyclic moiety) with a bivalent radical selected from each aryl, Het, bridged aryl or bridged Het can be substituted with one, two, three, four or five substituents each independently selected from halo, cyano, nitro, hydroxycarbonyl, C R wherein X wherein X wherein R R wherein X R each R each R5 and R6 is independently selected from hydrogen, halo, C R7 is hydrogen, methyl or fluoro; each R a N-oxide form thereof, a pharmaceutically acceptable addition salt thereof or a solvate thereof; characterized by a) reacting an intermediate of formula (II) with an appropriate reagent in a reaction-inert solvent with the formation of a compound of formula (I) with the variables as defined above; b) adding an excess of a base to an intermediate of formula (III) in the presence of an intermediate of formula (IV), wherein Halo is chloro or bromo, in a suitable solvent with the variables as defined above; or, if desired, converting compounds of formula (I) into each other following art-known transformations, and further, if desired, converting the compounds of formula (I), into a pharmaceutically acceptable acid addition salt by treatment with an acid, or into a pharmaceutically acceptable base addition salt by treatment with a base, or conversely, converting the acid addition salt form into the free base by treatment with alkali, or converting the base addition salt into the free acid by treatment with acid; and, if desired, preparing stereochemically isomeric forms or N-oxide forms thereof.