The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) “latent” safety-catch linker: solid phase synthesis of ketopiperazines
Expedient synthesis of benzene tricarboxamide macrocycles derived from p-aminobenzoic acid
作者:Fred Campbell、Colin A. Kilner、Andrew J. Wilson
DOI:10.1016/j.tetlet.2009.12.137
日期:2010.3
The synthesis of macrocycles functionalized at the periphery in a regiospecific fashion is considered challenging. This Letter describes a six-step synthesis of N-alkylated benzene tricarboxamide macrocycles derived from p-aminobenzoic acid via the iterative coupling of Fmoc-protected monomers and cyclization of the resultant linear foldamers.
Provided are: useful novel compounds that exhibit antibacterial activity based on their actions for inhibiting GyrB of DNA gyrase and ParE of topoisomerase IV; and 2(1H)-quinolinone derivatives represented by formula [1]:
or pharmaceutically acceptable salts thereof.
Facile Synthesis of a High Molecular Weight Amphiphilic Aramid–ROMP Block Copolymer
作者:Michael Badoux、Susanne Drechsler、Subhajit Pal、Andreas F. M. Kilbinger
DOI:10.1021/acs.macromol.7b01989
日期:2017.12.12
report the facile synthesis of an amphiphilic rod–coil blockcopolymer obtained by the coupling of an amine-terminated poly(dimethylpropylamine norbornene imide) (PDMAPNI) and a pentafluorophenol ester-terminated poly(dimethoxybenzyl p-aminobenzoate) (PAram). Postpolymerization amide N-deprotection of the blockcopolymer yielded a strongly aggregating water-soluble rod–coil copolymer. Transmission electron
A latent aryl hydrazine ‘safety-catch’ linker compatible with N-alkylation
作者:Frédéric Berst、Andrew B Holmes、Mark Ladlow、Peter John Murray
DOI:10.1016/s0040-4039(00)01108-4
日期:2000.8
The preparation and use of a latent aryl hydrazine 'safety-catch' linker for solid-phase chemistry, which is compatible with N-alkylation, is reported. Its use is exemplified by the preparation of mono-ketopiperazines, whereby release from resin is effected via an intramolecular cyclitive cleavage strategy. (C) 2000 Elsevier Science Ltd, All rights reserved.
The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) “latent” safety-catch linker: solid phase synthesis of ketopiperazines
作者:Frédéric Berst、Andrew B. Holmes、Mark Ladlow
DOI:10.1039/b301701j
日期:——
The development and preparation of the 2,4-dimethoxybenzyl arylhydrazine (DMBAH) linker 3, a new class of âlatentâ safety-catch linker which is stable under Mitsunobu alkylation conditions and in the presence of amines and hydrazine, is reported. The utility of the new linker is exemplified by the synthesis of ketopiperazines (MKPs)
24 bearing up to four points of diversity using a cyclitive cleavage approach.