作者:Guoliang Zhang、David Favela、Winston L. Chow、Rishab N. Iyer、Alexander J. Pell、David E. Olson
DOI:10.1021/acs.orglett.2c02516
日期:2022.8.26
Basic amines are key elements of many biologically active natural products and pharmaceuticals. Given their inherent reactivity, it is often necessary to protect basic amines during target-directed synthesis, which results in wasteful protection/deprotection sequences. We report a step-economical approach enabling the protection of secondary amines as carbamates prior to their conversion to tertiary
碱性胺是许多具有生物活性的天然产物和药物的关键元素。鉴于其固有的反应性,在靶向合成过程中通常需要保护碱性胺,这会导致保护/脱保护序列的浪费。我们报告了一种分步经济的方法,能够在仲胺通过 CO 2的正式挤出转化为叔胺之前将其保护为氨基甲酸酯。该方法适用于 iboga 生物碱 (±)-conodusine A 和 (±)-conodusine B 的合成。