2-phenyl isopropyl esters as car☐yl terminus protecting groups in the fast synthesis of peptide fragments
摘要:
The esters of Fmoc aminoacids derived from 2-phenylisopropanol have been prepared by using 2-phenylisopropyltrichloroacetimidate 1. They prevent diketopiperazine formation during amino deprotection of dipeptides and can be cleaved in the presence of Boc and O-Bu(t). They are thus well suited for the protection of C-terminus when a Fmoc strategy is used to build up peptide fragments.
2-phenyl isopropyl esters as car☐yl terminus protecting groups in the fast synthesis of peptide fragments
摘要:
The esters of Fmoc aminoacids derived from 2-phenylisopropanol have been prepared by using 2-phenylisopropyltrichloroacetimidate 1. They prevent diketopiperazine formation during amino deprotection of dipeptides and can be cleaved in the presence of Boc and O-Bu(t). They are thus well suited for the protection of C-terminus when a Fmoc strategy is used to build up peptide fragments.
Solid-Phase Synthesis of Oxetane Modified Peptides
作者:Jonathan D. Beadle、Astrid Knuhtsen、Alex Hoose、Piotr Raubo、Andrew G. Jamieson、Michael Shipman
DOI:10.1021/acs.orglett.7b01466
日期:2017.6.16
Solid-phase peptide synthesis (SPPS) is used to create peptidomimetics in which one of the backbone amide C═O bonds is replaced by a four-membered oxetane ring. The oxetane containing dipeptide building blocks are made in three steps in solution, then integrated into peptide chains by conventional Fmoc SPPS. This methodology is used to make a range of peptides in high purity including backbone modified