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实现了4-氨基苯磺酰胺、对溴苯乙酮和芳香醛之间的Mannich反应,直接合成了14个未见报道的β-氨基酮化合物,制备方法简便,反应条件温和,产物收率44%~92%.通过1HNMR,13CNMR,MS和HRMS表征并确证了目标分子的化学结构.生物活性试验显示,所得化合物具有一定的α-葡萄糖苷酶抑制活性和PPRE激动活性,由此发现某些含有磺胺结构的β-氨基酮具有抗糖尿病活性.
14 Mannich reactions between 4-aminobenzenesulfonamide, p-bromoacetophenone and aromatic aldehydes were carried out to directly synthesize 14 previously reported β-aminoketone compounds. The preparation method was simple and the reaction conditions were mild. The yield of product was 44 % ~ 92% .The chemical structure of the target molecule was characterized and confirmed by 1HNMR, 13CNMR, MS and HRMS.According to the biological activity test, the obtained compound has certain α-glucosidase inhibitory activity and PPRE agonistic activity, Beta-aminoketones containing a sulfonamide structure have anti-diabetic activity.