瑞莫拉宁的化学酶脱酰化。
Chemoenzymatic deacylation of ramoplanin.
机构信息
Dipartimento di Scienze Farmaceutiche, Via Venezian 21, 20133 Milano, Italy.
出版信息
Bioorg Med Chem Lett. 2012 Aug 15;22(16):5283-7. doi: 10.1016/j.bmcl.2012.06.046. Epub 2012 Jun 21.
PMID:22795330
Abstract
The chemoenzymatic deacylation of ramoplanin A2 is described for the first time: ramoplanin A2 was Boc-protected and hydrogenated to Boc-protected tetrahydroramoplanin, which was subsequently deacylated using an acylase from Actinoplanes utahensis NRRL 12052. The chemoenzymatic process proceeded with 80% overall yield, which favourably compares with the previously described chemical deacylation.
摘要
本文首次描述了雷莫拉宁 A2 的化学酶脱酰基反应：雷莫拉宁 A2 经 Boc 保护和氢化得到 Boc 保护的四氢雷莫拉宁，随后用 Actinoplanes utahensis NRRL 12052 中的酰基酶进行脱酰基反应。化学酶法的总收率为 80%，与先前描述的化学脱酰基反应相比具有优势。
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