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公开(公告)号:WO0021922A3
公开(公告)日:2000-11-09
申请号:PCT/EP9908135
申请日:1999-10-11
发明人: CASADO MICHEL , RATTON PATRICK , STEPHAN DOMINIQUE , VIAUVY AGNES
IPC分类号: C07B61/00 , C07C201/12 , C07C205/12 , C07C253/14 , C07C255/49 , C07C255/50 , C07C17/12
CPC分类号: C07C253/14 , C07C201/12 , C07C255/50 , C07C205/12
摘要: (57) Abstract The invention relates to a process for the preparation of a compound of formula (I): wherein, R represents C1-4 alkoxy; fluorine, chlorine or bromine; and R represents hydrogen or C1-4 alkoxy; which process comprises the reaction of the corresponding orthonitrohalobenzene of formula (II): wherein R and R are as hereinbefore defined and X represents a fluorine, chlorine or bromine atom, with, when X represents a fluorine atom: a) an alkali metal cyanide, in a non aqueous solvent optionally in the presence of a catalyst; or when X represents a chlorine atom: b) cuprous cyanide and a source of bromide selected from hydrogen bromide, bromine and a tetraalkylammonium bromide; optionally in the presence of an alkali metal bromide or an alkaline earth metal bromide; or c) an alkali metal cyanide or a tetraalkylammonium cyanide, in the presence of an alkali metal bromide or an alkaline earth metal bromide; or c) an alkali metal cyanide or a tetraalkylammonium cyanide, in the presence of cuprous bromide and a phase transfer catalyst; or d) cuprous cyanide and lithium iodide; or when X represents a bromine atom: e) cuprous cyanide optionally in the presence of a catalyst selected from an alkali metal bromide or an alkaline earth metal bromide; or f) an alkalie metal cyanide in the presence of a catalytic amount of cuprous cyanide and a phase transfer catalyst.
摘要翻译: (57)摘要本发明涉及制备式(I)化合物的方法:其中R 1表示C 1-4烷氧基; 氟,氯或溴; 并且R 2表示氢或C 1-4烷氧基; 该方法包括相应的式(II)的邻硝基苯:其中R 1和R 2如上所定义,X代表氟,氯或溴原子,当X表示氟原子时:a )碱金属氰化物,在非水溶剂中,任选地在催化剂存在下; 或当X表示氯原子时:b)氰化亚铜和选自溴化氢,溴和四烷基溴化铵的溴化物源; 任选地在碱金属溴化物或碱土金属溴化物的存在下; 或c)碱金属氰化物或四烷基氰化铵在碱金属溴化物或碱土金属溴化物的存在下反应; 或c)在溴化亚铜和相转移催化剂存在下的碱金属氰化物或四烷基氰化铵; 或d)氰化亚铜和碘化锂; 或当X表示溴原子时:e)氰化亚铜,任选地在选自碱金属溴化物或碱土金属溴化物的催化剂存在下; 或f)在催化量的氰化亚铜和相转移催化剂存在下的碱金属氰化物。