Synthesis of capuramycin and its analogues via a Ferrier-type I reaction and their biological evaluation
Synthesis of capuramycin and its analogues via a Ferrier-type I reaction and their biological evaluation
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DOI：
10.1016/j.bmc.2022.117011
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发表时间：
2022-11-01
影响因子：
3.5
通讯作者：
Ichikawa，Satoshi
中科院分区：
文献类型：
--
作者：
Kusaka，Shintaro;Yamamoto，Kazuki;Ichikawa，Satoshi
以Ferrier-I型反应为关键步骤，完成了一种有前途的抗结核抗生素卡普霉素（1）的全合成。这种全合成是合成卡普霉素及其类似物的替代方法。3′-O-去甲基类似物（2）对耻垢分枝杆菌和鸟分枝杆菌具有与卡普霉素（1）相当的抗菌活性，由于2从合成的角度来看更容易获得，因此被认为具有作为卡普霉素类似物的先导结构的潜力。
The total synthesis of capuramycin (1), which is a promising anti-tubercular antibiotics, has been accomplished using Ferrier-type I reaction as a key step. This total synthesis is an alternative approach to the synthesis of capuramycin and its analogues. The 3′-O-demethyl analogue (2), which exhibits an equivalent antibacterial activity as capuramycin (1) againstMycobacterium smegmatisandMycobacterium avium,is suggested to have potential as a lead structure of capuramycin analogues because2is more accessible from a synthetic view point.