Cuthbertson Alan, Indrevoll Bård
Amersham Health AS, Department of Medicinal Chemistry, Oslo, Norway.
Org Lett. 2003 Aug 7;5(16):2955-7. doi: 10.1021/ol035105w.
[structure: see text] The combination of the cysteine thiol protecting groups Trt, Acm, tBu, and MeBzl were used for the regioselective formation of an alpha-conotoxin dimer peptide containing four disulfide bridges. Additionally, a protocol is described whereby two one-pot oxidations were employed in order to improve the efficiency of the folding process. The target compound was produced in good yield.
[结构:见正文] 半胱氨酸硫醇保护基团Trt、Acm、tBu和MeBzl的组合用于区域选择性形成含有四个二硫键的α-芋螺毒素二聚体肽。此外,还描述了一种方案,其中采用了两次一锅法氧化以提高折叠过程的效率。目标化合物的产率良好。