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.

引用

页码：2800 / 2810

页数：11

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