Synthesis of 7-alkylidene-7,12-dihydroindolo(3,2-d)benzazepine-6-(5H)-ones (7-alkylidene-paullones) by N-cyclization oxidative Heck cascade and characterization as sirtuin modulators

被引：25
作者：
Denis, J. G. [1 ,2 ]
Franci, G. [3 ]
Altucci, L. [3 ]
Aurrecoechea, J. M. [4 ]
de Lera, A. R. [1 ,2 ]
Alvarez, R. [1 ,2 ]
机构：
[1] Univ Vigo, Dept Quim Organ, Fac Quim CINBIO, Vigo 36310, Spain
[2] Univ Vigo, Inst Invest Biomed Vigo IBIV, Vigo 36310, Spain
[3] Univ Naples 2, Dipartimento Biochim Biofis & Patol Gen, I-80138 Naples, Italy
[4] Univ Basque Country, Dept Quim Organ 2, Fac Ciencia & Tecnol, E-48080 Bilbao, Spain
来源：
ORGANIC & BIOMOLECULAR CHEMISTRY | 2015年 / 13卷 / 09期
关键词：
KINASE INHIBITORS; PAULLONES; INDOLES; ACTIVATION; ANALOGS; CORE;
D O I：
10.1039/c4ob02493a
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
An extension of our reported protocol to benzofused heterocyclic derivatives (benzofurans, indoles, isochromeneimines), involving a palladium-induced cascade of N-cyclization and oxidative Heck reactions of o-alkynylanilines, has allowed the preparation of indolobenzazepinones (paullones) with an alkylidene group at C7 in just 3-4 steps from ortho-iodoanilines. Some of these compounds behave as Sirt1 activators in biochemical assays.
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收藏
页码：2800 / 2810
页数：11
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