Development of an efficient liquid-phase peptide synthesis protocol using a novel fluorene-derived anchor support compound with Fmoc chemistry; AJIPHASE®
作者:Daisuke Takahashi、Takashi Yamamoto
DOI:10.1016/j.tetlet.2012.02.006
日期:2012.4
The development of a novel fluorene-type anchor support molecule and a liquid-phase peptide synthesis protocol (AJIPHASE®) is reported. With this support molecule, the synthesis of a protected peptide with a freecarboxylgroup could be carried out by repeated coupling/deprotection reactions and isolation by simple precipitation. Cleavage is performed under mild acidic conditions (2% TFA/CHCl3 or
Particular compounds having a fluorene skeleton are superior in broad utility and stability, as a protecting reagent for liquid phase synthesis of amino acids and/or peptides.
具有芴骨架的特定化合物在广泛的应用和稳定性方面优越,作为氨基酸和/或肽液相合成的保护试剂。
BENZYLIC COMPOUND
申请人:TAKAHASHI Daisuke
公开号:US20110160433A1
公开(公告)日:2011-06-30
The present invention provides a protecting reagent that can be removed in a high yield even under acidic conditions and can afford a resulting product at a high purity in an organic synthesis reaction such as peptide synthesis and the like. The inventive protecting reagent is particular benzylic compound having only one hydroxyl group substituted by an organic group having an aliphatic hydrocarbon group having a carbon number of not less than 14.
Compounds having a diphenylmethane skeleton are superior in broad utility and stability, and are useful as a protecting reagent (anchor) of amino acid and/or peptide in the liquid phase synthesis and the like of a peptide having a C-terminal etc., which are of a carboxamide(-CONHR)-type, and in organic synthetic reaction methods (particularly peptide liquid phase synthetic methods), and may be contained in a kit for peptide liquid phase synthesis.
Particular compounds having a fluorene skeleton are superior in broad utility and stability, as a protecting reagent for liquid phase synthesis of amino acids and/or peptides.