申请人：Dipharma Francis S.r.l.
公开号：EP1847538A1
公开（公告）日：2007-10-24
A process for the preparation of a compound of formula (I) or a salt thereof, both as the isomeric mixture and the individual isomers,
wherein Q is =CR8- or =N-; each R1, R2, R3 and R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and - N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and
each R5, R6, R7 and R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), or a salt thereof,
wherein Q, R1, R2, R3, R4, R5, R6 and R7 are as defined above,
to said compound of formula (I), or a salt thereof, in the presence of a catalyst, if necessary in an organic solvent; and, if desired, converting a compound of formula (I) to a salt thereof to another compound of formula (I); and/or, if desired, resolving an isomeric mixture of a compound of formula (I) in the individual isomers.
一种制备式（I）化合物或其盐的方法，包括其异构混合物和单体异构体，其中Q = CR8-或= N-;每个R1、R2、R3和R4独立地选自氢、卤素、羟基、硝基、C1-C6烷基，可选地取代羟基；C1-C6烷基硫代基；C1-C6烷氧基，可选地取代卤素或C1-C6烷氧基；苯基-C1-C6烷基；苯基-C1-C6烷氧基；以及-N（RaRb）其中每个Ra和Rb独立地选自氢或C1-C6烷基，或Ra和Rb连同它们连接到的氮原子形成饱和杂环环；以及每个R5、R6、R7和R8独立地选自氢、卤素、羟基、C1-C6烷基，可选地取代羟基；C1-C6烷基硫代基；C1-C6烷氧基，可选地取代卤素；C1-C6烷基-羰基，C1-C6烷氧基-羰基和噁唑-2-基；包括在有机溶剂中在催化剂的存在下将式（IV）化合物或其盐转化为所述式（I）化合物或其盐，并且如果需要，将式（I）化合物转化为其盐以获得另一种式（I）化合物；如果需要，在单体异构体中分离式（I）化合物的异构混合物。
