Synthesis of polysubstituted benzofuran derivatives as novel inhibitors of parasitic growth
摘要:
A series of polysubstituted benzofuran derivatives was easily and rapidly prepared using a tandem Sonogashira coupling/cyclization reaction. Subsequent acylation afforded a small library of 39 new compounds that were assayed in cellulo on Plasmodium falciparum and Tiypanosoma brucei parasites. Some of them exhibited good inhibitory activity on T. brucei proliferation. (C) 2013 Elsevier Ltd. All rights reserved.
Reduction par les sels chromeux de bromures benzyliques ortho-o-acyles avec transposition du groupement acyle
作者:B. Ledoussal、A. Gorgues、A. Le Coq
DOI:10.1016/s0040-4020(01)87790-5
日期:——
σ-bonded organochromium (III) complexes resulting from the reduction of-O-acyl benzylicbromides with CrCl2., undergo an 1,5-transposition of the esteracyl functional group which allows, through selected experimental conditions either a selective access to the unmasked -hydroxybenl ketones or a new preparation of the 2-substituted benzo¦b¦furans . The scope and limitations of the method are presented
Chromium(II) salt mediated reductive transposition of an ester acyl group in ortho-O-acyl benzylic bromides: a ready access to unmasked ortho-hydroxybenzyl ketones and a new route to benzo[b]furans
作者:Beno�t Ledoussal、Alain Gorgues、Andr� Le Coq
DOI:10.1039/c39860000171
日期:——
The mono-σ-bonded organochromium(III) complexes (A) derived from (1) rearrange internally into (B) through an acylestergrouptransposition, selected experimental conditions allowing either a good access to the unmaskedortho-hydroxybenzylketones (2) or a newroute to the 2-substituted benzo[b]furans (3).
衍生自(1)的单σ键合有机铬(III)配合物通过酰基酯基转移在内部重新排列为(B),选择的实验条件使得可以很好地接触未掩盖的邻羟基苄基酮(2)或新的途径取代2-取代的苯并[ b ]呋喃(3)。
Process for the synthesis of derivatives of the benzofuran, chromene and
申请人:Agence Nationale de Valorisation de la Recherche
公开号:US04230624A1
公开(公告)日:1980-10-28
The invention relates to a process for the production of therapeutic compounds of the benzofuran, chromene and isochromene type of the general formula; ##STR1## in which formula, ##STR2## R.sub.1 and R.sub.3 =H, lower alkyl, aralkyl or cycloalkyl R.sub.2 =H or an organic radical and when D= ##STR3## R.sub.1 and R.sub.3 may represent an organic radical. The process comprising the cyclization in the liquid phase and in the presence of a base a compound of the formula; ##STR4## in which formula; R'=an alkyl, aryl or aralkyl radical and X.sup.- =an anion.