A base promoted multigram synthesis of aminoisoxazoles: valuable building blocks for drug discovery and peptidomimetics
A base promoted multigram synthesis of aminoisoxazoles: valuable building blocks for drug discovery and peptidomimetics
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DOI：
10.1039/c6ra02365g
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发表时间：
2016-01-01
期刊：
影响因子：
3.9
通讯作者：
Mykhailiuk, Pavel K.
中科院分区：
文献类型：
--
作者：
Chalyk, Bohdan A.;Kandaurova, Inna Y.;Mykhailiuk, Pavel K.
详细阐述了由市售氨基酸合成含异恶唑结构单元的实用多克金属无金属合成方法。关键反应是原位生成的氧化腈与炔烃/烯胺的区域选择性[3 + 2]-环加成反应。获得的结构单元用于制备生物活性化合物和肽模拟物。
A practical multigram metal free synthesis of isoxazole-containing building blocks from commercially available amino acids was elaborated. The key reaction was a regioselective [3 + 2]-cycloaddition of in situ generated nitrile oxides with alkynes/enamines. The obtained building blocks were used in the preparation of bioactive compounds and peptidomimetics.