两个埃博霉素生物合成中间体修饰化合物的合成

Synthesis of Two Modified Intermediates in Epothilone Biosynthesis

为了使用前体定向生物合成技术研究埃博霉素的生物合成过程并对其进行分子改造,选定了两个中间体修饰化合物2-甲基噻唑-4-羧酸2-乙酰氨基乙硫基硫酯和(E)-2-甲基-3-(2-甲基噻唑-4-基)丙烯酸2-乙酰氨基乙硫基硫酯进行了化学全合成的研究.合成方法比已有的合成方法更易操作,经济性更好.所有化合物经红外光谱、质谱、核磁共振谱及元素分析确证了结构.

In order to investigate the biosynthesis of epothilones and generate novel biosynthetic epothilone analogues by a precursor-directed biosynthesis, two modified intermediates for epothilone biosynthesis were designed and synthesized, which were （2-methylthiazol-4-yl）carboxylic 2-acetamidoethylthiol thioester and （E）-2-methyl-3-（2-methyl-4-thiazoly）acrylic 2-acetamidoethylthiol thioester. The new synthetic procedures utilized were more inexpensive and convenient, and the structures of these compounds were confirmed by IR, MS, ^1H NMR and ^13C NMR spectra and elemental analysis.