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Process for producing a phenyl substituted heterocyclic derivative by coupling using a transition metal catalyst
专利权人:
TEIJIN PHARMA LIMITED
发明人:
KOMIYAMA, MASATO,YAJIMA, NAOKI,KUROKAWA, MASAYUKI
申请号:
ES10746307
公开号:
ES2459722T3
申请日:
2010.02.26
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A process comprising reacting a compound represented by the following formula (1): wherein, in the formula (1) ** Formula ** 5 R1 represents a hydrogen atom or halogen atom; R2 represents a hydrogen atom, cyano group, nitro group, halogen atom, formyl group or halomethyl group; A represents a hydrogen atom, C1 to C8 alkyl group, C3 to C6 cycloalkyl group, phenyl group, fluorine atom (only when X is a bond), or protecting group for a hydroxyl group (only when X is an oxygen atom ), in which A may be substituted with 1 to 3 substituents, such substituent representing a group selected from the group consisting of a halogen atom, C1 to C4 alkyl group, C1 to C4 alkoxy group, C1 to C4 alkylthio group, group C3 to C6 cycloalkyl, phenyl group, phenoxy group and pyridyl group; X represents a bond (only when A is a phenyl group or fluorine atom) or oxygen atom; and Y represents a leaving group and a compound represented by the following formula (2): in which in formula (2) ** Formula ** H represents a hydrogen atom; R3 represents COOR3a or COR3b; R3a represents a hydrogen atom, C1 to C4 alkyl group or ester type protecting group for a carboxyl group; R3b represents an amide-like protecting group for a carboxyl group, the protecting group forming an amide with a neighboring carbonyl group; R4 represents a halogen atom or C1 to C4 alkyl group; in the presence of a transition metal compound, in which the transition metal in the transition metal compound is different from nickel, to produce a phenyl substituted heterocyclic derivative represented by the following formula (3): ** Formula * *Un procedimiento que comprende hacer reaccionar un compuesto representado por la siguiente fórmula (1): en la que, en la fórmula (1)**Fórmula** 5 R1 representa un átomo de hidrógeno o átomo de halógeno; R2 representa un átomo de hidrógeno, grupo ciano, grupo nitro, átomo de halógeno, grupo formilo o grupo halometilo; A representa un átomo de hidrógeno, grupo alquilo C1 a C8, grupo cicloalquilo
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