TELEHA, Christopher A.,KOLODZIEJCZYK, Krzysztof,STAPPERS, Alfred Elisabeth,WEERTS, Koen Johan Herman
申请号：
ES13748242
公开号：
ES2607807T3
申请日:
2013.08.05
申请国别(地区):
ES
年份:
2017
代理人:
摘要：
A process for the preparation of a compound of formula (I) ** Formula ** wherein W is selected from the group consisting of ** Formula ** Each R4 is independently selected from the group consisting of hydrogen, F, Cl , Br, I, -OH, -OCH3, - OCH2CH3, -SC (1-4) alkyl, -SOC (1-4) alkyl, -SO2C (1-4) alkyl, -C (1-3) alkyl, -CO2Rd, -CONReRf, -CCRg and -CN； Where Rd is selected from the group consisting of H and -C (1-3) alkyl； Re is selected from the group consisting of H and -C (1-3) alkyl； Rf is selected from the group consisting of H and -C (1-3) alkyl； and Rg is selected from the group consisting of hydrogen, -CH2OH and -CH2CH2OH； J is selected from the group consisting of CH and N； R2 is selected from the group consisting of a cycloalkyl, spiro-substituted cycloalkenyl, thiophenyl, dihydrosulfonopyranyl, phenyl, furanyl, tetrahydropyridyl and dihydropyranyl； any of them can be independently substituted by one or two of the following: chlorine, fluoro, hydroxy, and C (1-4) alkyl； Z is selected from the group consisting of hydrogen, F, Cl and CH3； X is selected from the group consisting of ** Formula ** wherein Rw is selected from the group consisting of hydrogen, -C (1-4) alkyl, -CO2C (1-4) alkyl, -CONH2, -CONHC (1 -4) alkyl, -CON (C (1-4) alkyl) 2 45 and -COC (1-4) alkyl； or a tautomer or a pharmaceutically acceptable salt of that type； consisting of ** Formula ** the reaction of a compound of formula (X) with a compound of formula (XI) or a mixture of SEM protected regioisomers of that type, wherein ** Formula ** is selected from the group that It consists of ** Formula ** in the presence of carbon monoxide gas or a source of carbon monoxide； in the presence of an organic and inorganic base； in the presence of a suitably selected coupling system consisting of a palladium compound and a ligand； in an organic solvent； at a temperature between 60 ° C and 120 ° C approximately obtaining the corresponding compound of formula (XII)； ** Formula ** deprotecting the compound
