Sampson W R, Patsiouras H, Ede N J
Chiron Technologies Pty. Ltd., Clayton, Victoria, Australia.
J Pept Sci. 1999 Sep;5(9):403-9. doi: 10.1002/(SICI)1099-1387(199909)5:9<403::AID-PSC213>3.0.CO;2-S.
A comparative study has been undertaken between Hmb-protected amino acid and pseudoproline building block analogues for use in the solid phase synthesis of 'difficult' peptides. Both of these derivatives act by blocking inter- and intramolecular hydrogen bonding, which has been shown to be a major cause of poor synthesis/quality/efficiency. While the two were shown to result in substantial improvements in the purity of crude peptides, pseudoproline incorporation was found to be superior to Hmb backbone protection. This was due to slow and incomplete coupling of the amino acid immediately following the Hmb amino acid.
针对用于“困难”肽固相合成的六氢甲基苯并咪唑（Hmb）保护的氨基酸和拟脯氨酸结构单元类似物进行了一项比较研究。这两种衍生物均通过阻断分子间和分子内氢键起作用，而氢键已被证明是合成不佳/质量差/效率低的主要原因。虽然这两种方法都能显著提高粗肽的纯度，但发现引入拟脯氨酸优于Hmb主链保护。这是由于紧跟Hmb氨基酸之后的氨基酸偶联缓慢且不完全。
