Benzodioxane–benzamides as new bacterial cell division inhibitors
摘要:
A SAR study was performed on 3-substituted 2,6-difluorobenzamides, known inhibitors of the essential bacterial cell division protein FtsZ, through a series of modifications first of 2,6-difluoro-3-nonyloxybenzamide and then of its 3-pyridothiazolylmethoxy analogue PC190723. The study led to the identification of chiral 2,6-difluorobenzamides bearing 1,4-benzodioxane-2-methyl residue at the 3-position as potent antistaphylococcal compounds. (C) 2014 Elsevier Masson SAS. All rights reserved.
PROCESS FOR PREPARATION OF BENZO-FUSED HETEROARYL DERIVATIVES
申请人:Ballentine Scott A.
公开号:US20090247618A1
公开(公告)日:2009-10-01
The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.
The totalsynthesis of a dibenzofuran rhamnoside, kehokorin A, and its aglycone, kehokorin B, was achieved via a route including Suzuki-Miyaura cross-coupling followed by Ullmann ether synthesis to form a dibenzofuran, stepwise bromination at C7 of the dibenzofuran, a second Suzuki-Miyaura cross-coupling to install a 4-methoxyphenyl group at C7, and rhamnosylation.
[EN] PROCESSES FOR THE PREPARATION OF BENZO-FUSED DIOXIN DERIVATIVES<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION DE DÉRIVÉS D'HÉTÉROARYLE BENZO-CONDENSÉS
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2009120192A3
公开(公告)日:2010-01-21
PROCESSES FOR THE PREPARATION OF BENZO-FUSED DIOXIN DERIVATIVES
申请人:Janssen Pharmaceutica, N.V.
公开号:EP2280951A2
公开(公告)日:2011-02-09
[EN] PROCESS FOR THE PREPARATION OF BENZO-FUSED HETEROARYL DERIVATIVES<br/>[FR] PROCÉDÉ POUR LA PRÉPARATION DE DÉRIVÉS D'HÉTÉROARYLE BENZO-CONDENSÉS
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2009120192A2
公开(公告)日:2009-10-01
The present invention is directed to processes for the preparation of benzo-fused heteroaryl derivatives, useful for the treatment of epilepsy and related disorders. The present invention is further directed to processes for the preparation of intermediates in the synthesis of the benzo-fused heteroaryl derivatives.