异穿心莲内酯3,19-双酯类衍生物的合成与表征

Synthesis and characterization of 3,19-dicarbonyl-o-isoandrographolide derivatives

目的设计并合成异穿心莲内酯衍生物。方法以DCC为缩合剂，DMAP为催化剂，合成异穿心莲内酯3，19-双酯衍生物。结果合成并表征了9个异穿心莲内酯3，19-双酯衍生物及2个异穿心莲内酯19-单酯衍生物。异穿心莲内酯与羧酸及缩合剂DCC的摩尔比为1．0：2．5：2．5，于室温下反应4～6h。结论所合成化合物结构均经。HNMR、MS确证。

OBJECTIVE To design and synthesize a series of andrographolide derivatives for anti - HIV activity test. METHODS using DCC as condensing agent and DMAP as catalyst, novel 3, 19 -dicarbonyl -o -isoandrographolides were synthesized by esterification. RESULTS Eleven of the new isoandrographolide esters were synthesized and characterized, the tool ratio of isoandrographolide to acid to DCC was 1.0 ： 2.5 ： 2.5 for 4 - 6 h at room temperature. CONCLUSION The target compounds were identified by ^1HNMR and MS.