公开(公告)号：US20100137395A1

公开(公告)日：2010-06-03

申请号：US12514098

申请日：2007-11-05

申请人： Martin Sukopp ,  Oliver Kuhn ,  Carstein Gröning ,  Michael Keil ,  Jon J. Longlet

发明人： Martin Sukopp ,  Oliver Kuhn ,  Carstein Gröning ,  Michael Keil ,  Jon J. Longlet

IPC分类号： A01N43/56 ,  A01P7/04 ,  A01P7/02 ,  A01P5/00 ,  A61K31/415 ,  A61P33/00 ,  C07D231/44

CPC分类号： C07D231/44

摘要： The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent.

摘要翻译： 本发明涉及吡唑衍生物亚硫酰化的方法，其特征在于5-氨基-1- [2,6-二氯-4-（三氟甲基）苯基] -1H-吡唑-3-甲腈（II）是 与选自三氟甲基亚磺酸，三氟甲基亚磺酸酐和三氟甲基亚硫酸盐碱金属或碱土金属盐的亚磺酰化剂以及酸和/或盐的混合物在至少一种胺酸络合物的存在下反应，其中胺 选自叔胺，酸选自氢氟酸，盐酸，氢溴酸和氢碘酸以及磺酸衍生物，并加入卤化剂。