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31. 发明申请

WO9519352A3 PROCESS FOR THE PREPARATION OF 2-(4,4-DIFLUORO-BUT-3-ENYLTHIO)-BENZ-THIAZOLES AND -BENZOXADES 审中-公开
标题翻译：制备2-（4,4-DIFLOROR-BUT-3-乙基） - 苯并噻唑和苯并恶唑的方法
公开(公告)号：WO9519352A3
公开(公告)日：1996-01-18
申请号：PCT/GB9500003
申请日：1995-01-04
申请人： ZENECA LTD , BANSAL HARJINDER SINGH , CLEARE PETER JOHN VERNON
发明人： BANSAL HARJINDER SINGH , CLEARE PETER JOHN VERNON
IPC分类号： C07D263/58 , C07D277/74 , C07D263/60 , C07D277/84
CPC分类号： C07D263/58 , C07D277/74
摘要： A process for the preparation of a compound of formula (I) wherein R?1, R2, R3 and R4¿ are each independently hydrogen, optionally substituted alkyl, optionally substituted alkenyl, alkynyl, cycloalkyl, alkylcycloalkyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted aryloxy, optionally substituted arylalkoxy, alkoxy, alkenyloxy, alkynyloxy, hydroxyalkyl, alkoxyalkyl, alkylthio, alkenylthio, alkynylthio, haloalkyl, haloalkenyl, haloalkynyl, haloalkoxy, haloalkenyloxy, haloalkynyloxy, haloalkylthio, haloalkenylthio, haloalkynylthio, halogen, hydroxy, cyano, nitro, -NR?5R6, -NR7COR8, -NR7CSR8, -NR9SO¿2R10, -N(SO¿2-R?11), -(SO¿2?-R?12), -COR13, -CONR14R15, -COOR16, -OCOR17¿, -OSO¿2?R?18, -SO¿2NR?19R20, -SO¿2R?21, -SOR22, -CSNR23R24, -SiR25R26R27¿, -OCH¿2CO2R?28, -OCH¿2?CH2CO2R?29, -SO¿2Z, -CONR30SO2R31, -NHCONR32R33, -NHCSNR32R33, or an adjacent pair of R?1, R2, R3 and R4¿ when taken together form a fused 5- or 6-membered carbocyclic or heterocyclic ring; R?5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27, R28, R29, R30, R31, R32 and R33¿ are each independently selected from hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, optionally substituted aryl and optionally substituted arylalkyl; Z is halogen; and X is oxygen or sulphur, which comprises (a) reacting a substituted ortho-nitro or -nitroso phenol or a substituted ortho-nitro or -nitroso thiophenol of formula (II), wherein R1-R4 and X have the values previously defined, and y is 1 or 2, with a reducing agent comprising an alkali metal dithionite in an alkaline reaction medium in the presence of carbon disulphide, to form the substituted 2-mercaptobenz-oxazole or -thiazole of formula (III) wherein R1-R4 and X have the values previously defined, acidifying the reaction mixture and collecting the 2-mercaptobenz-oxazole or -thiazole; and (b) reacting the 2-mercaptobenz-oxazole or -thiazole (III), with a compound of formula (IV) CF¿2?=CH-CH2-CH2-L wherein L is a good leaving group to form the compound of formula (I).
摘要翻译：在（a）在碱性反应介质中使取代的邻硝基或亚硝基苯酚或取代的邻硝基或亚硝基苯酚与碱金属连二亚硫酸盐还原剂与碱金属连二亚硫酸盐还原剂反应制备方法的二硫化碳，形成取代的2-巯基苯并恶唑或噻唑，酸化反应混合物并收集2-巯基苯并恶唑或噻唑; 然后（b）使2-巯基苯并恶唑或噻唑与式（Ⅳ）化合物CF2 = CH-CH2-CH2-L（Ⅳ）反应，其中L是一个好的离去基团。

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