新缩瞳剂包公藤甲素人工合成研究

STUDIES ON SYNTHESIS OF BAOGONGTENG A——A NEW MYOTIC AGENT

摘要: 包公藤甲素是从包公藤(Erycibe obtusifolia Benth.)茎中提得的一个新莨菪烷生物碱,具有强烈的缩瞳作用,临床用于治疗青光眼。本文报道用合成的6β-乙酰氧基托品酮为原料,经卤代、水解、还原和N-去甲基化等反应合成包甲素(8)。经光谱测定证实8与天然包甲素的结构完全一致。合成品系外消旋体,其作用机理与天然品相同,而强度则减半。

Abstract: Baogongteng A, isolated from Eryeibe obtusifolia Benth., is a new tropane alkaloid used for treating glaucoma. Using synthetic 6β-acetoxy-tropinone as starting material, racemic Baogongteng A(8) was synthesized. Synthetic Baogongteng A also shows myotic activities in rabbits, but the potency is half of that of the natural product.