Department of Chemistry, Fudan University, Shanghai 200433, China.
J Org Chem. 2013 Apr 5;78(7):3400-4. doi: 10.1021/jo400071h. Epub 2013 Mar 11.
CuBr-catalyzed coupling reaction of 2-halobenzonitriles with hydrazine carboxylic esters and CuBr/4-hydroxy-l-proline-catalyzed coupling reaction of 2-bromobenzonitriles with N'-arylbenzohydrazides proceed smoothly at 60-90 °C to provide substituted 3-aminoindazoles through a cascade coupling/condensation (or coupling/deacylation/condensation) process. A wide range of 3-aminoindazoles with substituents at both the 1-position and the phenyl ring part can be prepared from the corresponding coupling partners.
CuBr 催化的 2-卤代苯甲腈与肼羧酸酯的偶联反应和 CuBr/4-羟基-L-脯氨酸催化的 2-溴代苯甲腈与 N'-芳基苯甲酰肼的偶联反应在 60-90°C 下顺利进行，通过级联偶联/缩合（或偶联/脱酰基/缩合）过程提供取代的 3-氨基吲唑。可以从相应的偶联试剂制备具有 1-位和苯基环部分取代基的各种 3-氨基吲唑。
