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Process for the production of heterocycle substituted pyridine derivatives
专利权人:
EISAI R & D MANAGEMENT CO.; LTD.
发明人:
JUN NIIJIMA,SHINYA ABE,KAZUHIRO YOSHIZAWA,YUKI KOSAKA
申请号:
BRPI0821689
公开号:
BRPI0821689A2
申请日:
2008.12.25
申请国别(地区):
BR
年份:
2015
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 R 1 represents a hydrogen atom, etc.; R 2 represents a hydrogen atom, a C 1-6 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 C 1-6 alkyl groups; Z represents a single bond, a methylene group, an ethylene group, an oxygen atom, etc.; R represents a hydrogen atom or a C 1-6 alkyl group, etc.; R 3 represents a hydrogen atom or a halogen atom, etc.; and R 4 represents a hydrogen atom or a halogen atom; provided that when Z represents a single bond, or when R 3 represents a hydrogen atom, then R 1 , R 2 , and R 4 cannot all be a hydrogen atom at the same time.
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