el-Diwani H, Nakkady S S, Hishmat O H, el-Shabrawy O A, Mahmoud S S
Natural Products Department, National Research Centre, Cairo, Egypt.
Pharmazie. 1992 Mar;47(3):178-81.
Acylation of 2,3-diphenyl-5-methoxy-indole using ethyl chloroformate or chloroacetyl chloride in dimethylformamide and sodium hydride yielded the N-substituted derivatives 1 and 2, respectively. While Friedel-Crafts acylation using chloroacetyl chloride afforded di-4,6-chloroacetyl derivative 3, the reaction of the N-chloroacetyl derivative 2 with amines, hydrazines, urea, semicarbazide hydrochloride, thiophenol, benzimidazole-2-thiol, thiosemicarbazide, 2-mercaptoethanol and thioglycolic acid was studied. Several of the compounds were tested for their effect on arterial blood pressure, antiinflammatory and ulcerogenic activities.
在二甲基甲酰胺中，使用氯甲酸乙酯或氯乙酰氯与氢化钠对2,3 - 二苯基 - 5 - 甲氧基吲哚进行酰化反应，分别得到N - 取代衍生物1和2。虽然使用氯乙酰氯进行傅克酰化反应得到了二 - 4,6 - 氯乙酰基衍生物3，但我们研究了N - 氯乙酰基衍生物2与胺、肼、尿素、盐酸氨基脲、苯硫酚、苯并咪唑 - 2 - 硫醇、氨基硫脲、2 - 巯基乙醇和巯基乙酸的反应。测试了其中几种化合物对动脉血压、抗炎和致溃疡活性的影响。
