公开(公告)号：CA2667565A1

公开(公告)日：2008-05-15

申请号：CA2667565

申请日：2007-11-05

Applicant: BASF AG

Inventor： KUHN OLIVER ,  SUKOPP MARTIN ,  GROENING CARSTEN ,  LONGLET JON J ,  KEIL MICHAEL

IPC: C07D231/44 ,  A01N43/00 ,  A01N43/56 ,  A61K31/415 ,  A61P33/00

Abstract: The present invention relates to a process for the sulfinylation of a pyr azole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoro methyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylati ng agent S in the presence of at least one amine acid complex wherein the am ine(s) are selected from secondary and/or tertiary amines and the acid(s) ar e selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent , wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, brom o, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof, wherein the temperature of the reaction mixture at no time exceeds 39°C.

公开(公告)号：CA2667559A1

公开(公告)日：2008-05-15

申请号：CA2667559

申请日：2007-11-05

Applicant: BASF AG

Inventor： GROENING CARSTEN ,  KEIL MICHAEL ,  KUHN OLIVER ,  LONGLET JON J ,  SUKOPP MARTIN

IPC: C07D231/44 ,  A01N43/00 ,  A01N43/56 ,  A61K31/415 ,  A61P33/00

Abstract: The present invention relates to a process for the sulfinylation of a pyr azole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoro methyl)phenyl]-1H-pyrazole-3- carbonitrile (II) is reacted with a sulfinylat ing agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfini c 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 a t least one amine acid complex wherein the amine(s) are selected from tertia ry amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydr obromic and hydroiodic acid and sulfonic acid derivatives, and with the addi tion of a halogenating agent.

公开(公告)号：CA2667562A1

公开(公告)日：2008-05-15

申请号：CA2667562

申请日：2007-11-05

Applicant: BASF AG

Inventor： SUKOPP MARTIN ,  KUHN OLIVER ,  GROENING CARSTEN ,  KEIL MICHAEL ,  LONGLET JON J

IPC: C07D231/44 ,  A01N43/00 ,  A01N43/56 ,  A61K31/415 ,  A61P33/00

Abstract: The present invention relates to a process for the sulfinylation of a pyr azole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoro methyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylati ng agent S in the presence of at least one amine acid complex wherein the am ine(s) are selected from cyclic secondary amines and the acid(s) are selecte d from sulfonic acid derivatives, and with the addition of a halogenating ag ent, wherein S is [CF3S(O)]2O; or CF3S(O)X wherein X means fluoro, chloro, b romo, iodo, a hydroxy group, or an alkaline or alkaline earth metal salt of the hydroxy group; or mixtures thereof.