公开(公告)号：KR101220148B1

公开(公告)日：2013-01-15

申请号：KR1020120048080

申请日：2012-05-07

Applicant: 강원대학교산학협력단

Inventor： 이필호 ,  박성국 ,  박영철

IPC: C07D231/12 ,  B01J23/44

Abstract: PURPOSE: A pyrazole derivative and a method for preparing the same are provided to be used as an important intermediate, and to synthesize a precision chemistry intermediate including agrochemicals. CONSTITUTION: A method for preparing a pyrazole derivative of chemical formula 1 comprises: a step of intramolecular cyclizing hydrazinecarboxylate derivatives of chemical formula 7 under the presence of TfOH, AuCl, AuCl_3, AuBr_3, Ph_3PAuCl, (C_6F_5)_3PAuCl, (4-CF_3-C_6H_4)_3PAuCl, (IPr)AuCl [IPr = N,N`-bis(2,6-diisopropylphenyl) imidazol-2-ylidine], (IMes)AuCl [IMes = N,N`-bis(2,4,6-trimethylphenyl) imidazol-2-ylidene], (IMes)AuCl [IMes = N,N`-bis(2,4,6-trimethylphenyl) imidazol-2-ylidene], AgNTf_2, AgOTf, AgSbF_6, AgAsF_6, AgPF_6 AgBF_4, AgNO_3, or AgClO_4 catalyst to prepare a 1,2-dihydro-pyrazol-3-one derivative of chemical formula 6; a step of reacting the derivative of chemical formula 6 with N-phenylbis(trifluoro methane sulfominide)(PhNTf_2) under the presence of a base to prepare a pyrazole triflate derivative of chemical formula 2; and a step of reacting the derivative of chemical formula 2 with an boronic acid derivative of chemical formula 3, a terminal alkyne derivative of chemical formula 4, or an organotin compound of chemical formula 5 under the presence of a palladium catalyst.

Abstract translation: 目的：提供吡唑衍生物及其制备方法作为重要的中间体，并合成含有农药的精密化学中间体。 构成：制备化学式1的吡唑衍生物的方法包括：在TfOH，AuCl，AuCl_3，AuBr_3，Ph_3PAuCl，（C_6F_5）_3PAuCl，（4-CF_3-）的存在下，分子内环化化学式7的肼甲酸酯衍生物的步骤， C 6 H 4）_3PAuCl，（IPr）AuCl [IPr = N，N'-双（2,6-二异丙基苯基）咪唑-2-基]]，（IMes）AuCl [IMes = N，N'-双 （三甲基苯基）咪唑-2-亚基]，（IMes）AuCl [IMes = N，N'-双（2,4,6-三甲基苯基）咪唑-2-亚基]，AgNTf_2，AgOTf，AgSbF_6，AgAsF_6，AgPF_6 AgBF_4， AgNO_3或AgClO_4催化剂以制备化学式6的1,2-二氢 - 吡唑-3-酮衍生物; 使化学式6的衍生物与N-苯基双（三氟甲烷砜）（PhNTf_2）在碱存在下反应，制备化学式2的吡唑三氟甲磺酸酯衍生物的步骤; 以及使化学式2的衍生物与化学式3的硼酸衍生物，化学式4的末端炔衍生物或化学式5的有机锡化合物在钯催化剂存在下反应的步骤。