灵芝生物碱甲和乙的合成

SYNTHESIS OF GANODERMA ALKALOID A AND B

灵芝为担子菌类多孔菌科灵芝属植物的子实体。人工培养的有赤芝、紫芝、薄盖灵芝和树舌等。灵芝是我国广泛流传的珍贵药物之一。近年来,对于灵芝的临床疗效和药理作用做了多方面的研究,证明对慢性气管炎、慢性肝炎、冠心病、白细胞减少症、慢性克山病和神经衰弱等都有一定的疗效,特别是对神经系统和肝脏功能具有调节作用。

Ganoderma alkaloid A (Ⅰ_A, 1-isopentyl-2-formyl-5-hydroxy-methylpyrrole) and B (Ⅰ_B, 1-phenylethy 1-2-formyl-5-hydroxymethylpyrrole) were discovered in the hypha of deep fermented Ganoderma capense. Both are new pyrrole alkaloids. In order to provide samples for bioassay, we completed the synthesis of these new alkaloids and their acetyl derivatives. The route of synthesis included six steps. Thewhole yields were 20.7% for Ⅰ_A and 24.7% for Ⅰ_B. Synthetic Ⅰ_A and Ⅰ_B were found to be identical with the natural compounds by comparison of spectral data. Ⅰ_A and Ⅰ_B showed some antiinflammatory activity in animal experiments.