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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。
Triptolide is a new tropane alkaloid derived from the stem of Erycibe obtusifolia Benth. It has a strong miotic effect and is clinically used to treat glaucoma. This paper reported the synthesis of 6β-acetoxytropinone as raw material, by halogenation, hydrolysis, reduction and N-demethylation reactions such as the synthesis of tamifol (8). It was confirmed by spectrometry that the structure of 8 was completely identical with that of natural inclusion A. Department of racemic synthetic products, its mechanism of action and the same natural products, while the intensity is halved.