The use of pre-prepared diaminodiacids has been established as an effective approach for the chemical synthesis of peptide disulfide bond mimics. A technical problem often encountered in the implementation of the diaminodiacids strategy is the use of heavy metal reagents to remove the side-chain protecting groups. In the present work, we reported the development of diaminodiacid that carry 4-(N-[1-(4,4-dimethyl-2,6-dioxocyclo-hexylidene)-3-methylbutyl]amino)benzyl (Dmab) and 1-(4,4-dimethyl-2,6-dioxocyclohex-1-ylidene)-3-methylbutyl (ivDde) protecting groups. This pair of protecting groups can be readily removed by mild hydrazinolysis during the solid-phase synthesis on resin. We demonstrated the use of Dmab/ivDde protected diaminodiacids in the successful synthesis of a disulfide surrogate of oxytocin.

已经建立了使用预先制备的二氨基二酸作为肽二硫键模拟物的化学合成的有效方法。在实施二氨基二酸策略中经常遇到的技术问题是使用重金属试剂去除侧链保护基。在目前的工作中，我们报道了带有4-（N- [1-（4,4-二甲基-2,6-二氧代环己己基）-3-甲基丁基]氨基）苄基（Dmab）的二氨基二酸的开发。 （4,4-二甲基-2,6-二氧代环己基-1-亚烷基）-3-甲基丁基（ivDde）保护基。在树脂上固相合成过程中，通过温和的肼解作用可轻松除去该对保护基。我们证明了在成功合成催产素的二硫键替代物中使用Dmab / ivDde保护的二氨基二酸。