The photolabile hydrazine linker of the present invention is based on the o-nitro-veratryl group, which is capable of releasing hydrazide derivatives upon UV irradiation. The linker allows for a new solid-phase peptide synthesis (SPPS) strategy which is fully orthogonal to the most commonly used protecting groups and chemical methods in SPPS and shows excellent compatibility with peptide composition, notably the 20 naturally occurring α-amino acid residues (even in their side-chain protected form) are accepted in the C-terminal of the peptide hydrazides. Furthermore, the linker unit can be applied to synthesize combinatorial libraries of biological interesting heterocyclic compounds, such as pyranopyrazoles.
本发明的光敏式
肼连接剂基于邻硝基维拉特基团,能够在紫外辐射下释放
肼衍
生物。该连接剂允许一种全新的固相肽合成(
SPPS)策略,与
SPPS中最常用的保护基和
化学方法完全正交,并且与肽组成非常兼容,特别是在肽
肼酰的C末端接受20种天然存在的
α-氨基酸残基(即使是它们的侧链保护形式)。此外,该连接单元可用于合成
生物感兴趣的
杂环化合物的组合式库,如
吡喃
吡唑。