发明名称 METHOD FOR PRODUCING CARBOXAMIDES
摘要 The present invention relates to a process for the preparation of carboxamide derivatives of formula (I) as described herein starting from a pyrazole carbonyl derivative and an amine in absence of an additional acid acceptor.
申请公布号 US2017015632(A1) 申请公布日期 2017.01.19
申请号 US201515300805 申请日期 2015.03.30
申请人 BAYER CROPSCIENCE AKTIENGESELLSCHAFT 发明人 PAZENOK SERGII
分类号 C07D231/14 主分类号 C07D231/14
代理机构 代理人
主权项 1. A process for the preparation of one or more carboxamide derivatives of formula (I) wherein R1 and R2 are independently selected from hydrogen, optionally halo-substituted C1-C4-alkyl, or optionally halo-substituted C3-C7-cycloalkyl, optionally hydrogen or C1-C2-alkyl, optionally hydrogen or methyl, even more preferably hydrogen; Z1, Z2 and Z3 are independently selected from the group consisting of hydrogen C1-C4-alkyl, halo-substituted C1-C4-alkyl, C3-C6-cycloalkyl, halo-substituted C3-C6-cycloalkyl, optionally Z1 and Z2 are independently selected from halo-substituted C1-C4-alkyl and Z3 is C1-C4-alkyl, optionally Z1 and Z2 are independently selected from halo-substituted C1-C2-alkyl and Z3 is C1-C2-alkyl; Hal is selected from F, Cl, Br or I, optionally Cl, comprising reacting one or more compounds of the formula (II) wherein Z1, Z2 and Z3 are independently selected from the group consisting of hydrogen, C1-C4-alkyl, halo-substituted C1-C4-alkyl, C3-C6-cycloalkyl, halo-substituted C3-C6-cycloalkyl, optionally Z1 and Z2 are independently selected from halo-substituted C1-C4-alkyl and Z3 is C1-C4-alkyl, optionally Z1 and Z2 are independently selected from halo-substituted C1-C2-alkyl and Z3 is C1-C2-alkyl; and the leaving group is C1-C4-alkoxy, or a halogen selected from F, Cl, Br or I, or with one or more amine derivatives of formula (III) or a salt thereof (III′) wherein R1 and R2 are independently selected from hydrogen, optionally halo-substituted C1-C4-alkyl, or optionally halo-substituted C3-C7-cycloalkyl, optionally hydrogen or C1-C2-alkyl, optionally hydrogen or methyl, optionally hydrogen; Hal is selected from F, Cl, Br or I, optionally preferably Cl X is selected from the group consisting of F−, Cl−, Br−, I−, HSO4−, CH3COO−, BF4−, CH3SO3−, p-Toluensulphonate, CF3COO− or CF3SO3−; in the absence of an acid acceptor in addition to compound (III) or (IY).
地址 Duesseldorf DE