化合物2和化合物3经Suzuki反应,得到化合物4,收率不高 构建三氮唑得到化合物6,稳健性不好 氯代后,脱O-甲基,大量氢溴酸使用,腐蚀性强 化合物2制备化合物1的总收率24%
Overall, compound 1 was obtained in a 70% overall yield starting from boronic ester 2 the recrystallization of the penultimate intermediate 7 was key to control the purity and the color of the desired 4-chloro-1,2,3-triazole 1 第一步改善了收率 第二、三步更稳健 第五步替换掉了氢溴酸