(S)-萘普生-1,4-二氢吡啶类化合物的合成与生物活性

以(S)-萘普生为原料制得的(S)-萘普生氯甲酯与1,4-二氢吡啶-3,5-二羧酸单酯在无水K₂CO₃存在下于DMF中反应得到的粗产品经梯度结晶或柱层析纯化得标题化合物. 合成的7种目标化合物收率21%～73%, 经¹H NMR, IR, MS确证了结构. 家兔离体血管平滑肌收缩试验研究表明, 大部分目标化合物对苯肾上腺素诱导的血管收缩有松弛作用.

Synthesis and Bioactivity of 1,4-Dihydropyridine Moiety Substituted (S)-Naproxen

The target compounds were synthesized by the reaction chloromethyl ester of (S)-naproxen with 1,4-dihydropyridine-3,5-dicarboxylic monoester in DMF in the presence of K₂CO₃, and purified by gradient crystallization or column chromatography on silica gel. The yields of seven new compounds were 21%～73%. The structures of the compounds were confirmed by ¹H NMR, IR and MS spectra. The effect of such new compounds on the contrac-tion of aorta smooth muscle was observed on the isolated arotic strips of rabbits, and most of them could re-lax constricting strip induced by phenylephrine.