Various 3-aryl-1H-indazol-5-amine derivatives were synthesized by Pd-catalyzed Suzuki–Miyaura cross-couplingreaction of (NH) free 3-bromo-indazol-5-amine with arylboronic acids under microwave-assisted conditions. The coupling reaction can be carried out under the conditions with dioxane/H2O as solvent, Pd(OAc)2 and RuPhos as catalyst system, and K3PO4 as a base in good to excellent yields.
在微波辅助条件下,通过(Pd)催化的(NH)游离3-溴-吲哚-5胺与芳基硼酸的Suzuki-Miyaura交叉偶联反应,合成了各种3-芳基-1 H-吲哚5胺衍生物。可以在以二恶烷/ H 2 O为溶剂,Pd(OAc)2和RuPhos为催化剂体系,以K 3 PO 4为碱的条件下以良好或优异的产率进行偶联反应。
[EN] INDAZOLES AND AZAINDAZOLES AS LRRK2 INHIBITORS<br/>[FR] INDAZOLES ET AZAINDAZOLES EN TANT QU'INHIBITEURS DE LRRK2
申请人:E SCAPE BIO INC
公开号:WO2021007477A1
公开(公告)日:2021-01-14
The present invention is directed to indazole and azaindazole compounds which are inhibitors of LRRK2 and are useful in the treatment of CNS disorders.