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ballwarm

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Highly efficient and regioselective acylation of pharmacologically interesting cordycepin catalyzed by lipase in the eco-friendly solvent 2-methyltetrahydrofuran

A total of nine lipases and three proteases were tested for enzymatic regioselective acylation(s) of cordycepin with vinyl acetate in organic media. The highest conversion with better initial reaction rate was achieved with immobilized Candida antarctica lipase B (Novozym 435). An eco-friendly solvent 2-methyltetrahydrofuran (MeTHF) was thought to be the most suitable reaction medium. Novozym 435 was found to be a useful biocatalyst for the 25-g scale syntheses of cordycepin acetate (96.2% isolated yield), and the biocatalyst displayed excellent regioselectivity and high operational stability during the transformation. The 5′-substituted cordycepin derivative was the sole detectable product from each acylation reaction. Novozym 435 could be recycled for the synthesis of cordycepin derivative on a 25-g scale and 63% of its original activity was maintained after being reused for 7 batches. MeTHF could be considered as an eco-friendly solvent for the large scale use in biotransformation.
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genhunter

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ballwarm: 金币+7, 翻译EPI+1, 有帮助 2016-03-05 19:43:00
环保溶剂2-甲基四氢呋喃中脂肪酶催化的高效构像选择性酰化有药用价值的虫草素

尝试了九种脂肪酶和三种蛋白酶在有机溶剂对虫草素进行乙酸乙烯酯选择性酰化。固定化南极假丝酵母脂肪酶 B(Novozym 435)具有较好的初始反应速率和最高的转化率。一种环保溶剂2-甲基四氢呋喃(methf)是最合适的反应介质。Novozym 435作为生物催化剂在25克级规模合成中非常有效(收率96.2%),表现出优异的选择性和转换过程较好的稳定性。5′取代的虫草素衍生物是酰化反应的唯一测到的产物。在25克的规模合物中可以回收利用, 重复利用7次后仍保持原活性的63% 。在生物转化中methf是一种环保的,可以大量使用的溶剂。
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2楼2016-03-05 19:19:30
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