氰
试剂
产量(工程)
化学
溴化氰
光气
酰化
重氮甲烷
序列(生物学)
有机化学
硫霉素
二硫烷
组合化学
材料科学
抗生素
冶金
肽序列
催化作用
基因
生物化学
作者
Michael Prieschl,Joerg Sedelmeier,Kurt Püntener,Stefan Hildbrand,Jason D. Williams,C. Oliver Kappe
标识
DOI:10.1021/acs.joc.3c01110
摘要
The expeditious synthesis of an API building block, 2-cyanothiazole, from cyanogen gas and a readily available dithiane is reported. A previously undisclosed partially saturated intermediate is formed, which can be further functionalized and isolated by the acylation of the hydroxy group. Dehydration using trimethylsilyl chloride furnished 2-cyanothiazole, which could be further converted to the corresponding amidine. The sequence provided a 55% yield over 4 steps. We envision that this work will spark further interest in cyanogen gas as a reactive and cost-effective synthetic reagent.
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