系列烟酸前体药物的合成

Synthesis of a series of nicotinic acid prodrugs

目的寻找活性更强、副作用更小的烟酸前体药物。方法以烟酸为起始原料 ,采用酰氯法 ,通过酯键或酰胺键 ,分别与对乙酰氨基酚、香草醛、磺胺甲唑、L 苯丙氨酸甲酯、盐酸普鲁卡因及诺氟沙星等药物相偶联 ,合成了 6个新目标化合物。结果化合物的结构均经红外光谱、核磁共振氢谱、质谱及其元素分析确证。

Aim To screen out nicotinic acid prodrugs with better activity and less side effects.Methods By employing the acyl chloride method,6 new title compounds were synthesized from nicotinic acid with paracetamol,vanilla aldehyde, L phenylalanine methyl ester,sulfamethoxazole,procaine hydrochloride,and norfloxacin respectively by the ester bond or amide linkage.Results Their chemical structures were determined by IR, 1H NMR,MS and elemental analysis.Conclusion The acyl chloride method was feasible to the synthesis of nicotinic acid prodrugs.