Embodiments of this disclosure, among others, encompass methods for generating alkenes under mild thermolytic conditions that can provide almost total conversion of a precursor compound to an alkene without isomerization or the need to chromatographically purify the final product By selectively blocking the amino and carboxy groups of the deπvatized amino acid, the methods of the disclosure provide for the synthesis of a peptide having the vinylglycine moiety at either the carboxy or the amino terminus of the peptide The mild conditions for the thermolytic removal of an o-NO
2
-phenyl substituted aryl group ensure that there is minimal if any damage to thermally sensitive conjugates such as a peptide bearing the vinylglycine The methods of the present disclosure have practical applications for the preparation of unsaturated compounds under mild, thermolytic conditions.
本公开的实施例包括在温和的热解条件下生成烯烃的方法,该方法可以将前体化合物几乎完全转化为烯烃,而无需异构化或层析纯化最终产物。通过选择性阻断去保护
氨基和羧基的
氨基酸,本公开的方法提供了合成具有
乙烯基甘氨酸基团的肽的方法,该肽的
乙烯基甘氨酸基团可以位于肽的羧基或
氨基端。温和的条件下热解去除o-
NO2-苯基取代芳基基团,确保对热敏感的共轭物如带有
乙烯基甘氨酸的肽的最小甚至没有损伤。本公开的方法在温和的热解条件下制备不饱和化合物具有实际应用价值。