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PROCESS FOR PRODUCTION OF HETEROCYCLE-SUBSTITUTED PYRIDINE DERIVATIVE
专利权人:
EISAI R&D MANAGEMENT CO.; LTD.
发明人:
NIIJIMA, JUN,YOSHIZAWA, KAZUHIRO,KOSAKA, YUKI,ABE, SHINYA
申请号:
EP08863620
公开号:
EP2226320A4
申请日:
2008.12.25
申请国别(地区):
EP
年份:
2012
代理人:
摘要:
It is an object of the present invention to provide an efficient method for manufacturing heterocycle-substituted pyridine derivatives. The present invention provides a method for manufacturing a compound represented by the following formula (I):the method including reacting a compound represented by the following formula (III):and a compound represented by the following formula (II):in a solvent and in the presence of a palladium catalyst and a base,wherein R1 represents a hydrogen atom, etc. R2 represents a hydrogen atom, a C1-6 alkyl group, an amino group that may be protected with a protective group, etc. one of X and Y represents a nitrogen atom and the other represents a nitrogen atom or an oxygen atom Q represents a leaving group the ring A represents a 5- or 6-member heteroaryl ring or a benzene ring, which may have one or two halogen atoms or C1-6 alkyl groups Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc. R represents a hydrogen atom or a C1-6 alkyl group, etc. R3 represents a hydrogen atom or a halogen atom, etc. and R4 represents a hydrogen atom or a halogen atomprovided that when Z represents a single bond, or when R3 represents a hydrogen atom, then R1, R2, and R4 cannot all be a hydrogen atom at the same time.
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