Synthesis of novel 1-methyl-1H-pyridazino[3,4-b]indoles

被引：16

作者：

Riedl, Z

Monsieurs, K

Krajsovszky, G

Dunkel, P

Maes, BUW

Tapolcsányi, P

Egyed, O

Boros, S

Mátyus, P

Pieters, L

Lemière, GLF

Hajós, G

机构：

[1] Hungarian Acad Sci, Chem Res Ctr, Inst Biomol Chem, H-1525 Budapest, Hungary

[2] Univ Antwerp, Dept Chem, B-2020 Antwerp, Belgium

[3] Semmelweis Univ, Dept Organ Chem, H-1092 Budapest, Hungary

[4] Univ Antwerp, Dept Pharmaceut Sci, B-2610 Antwerp, Belgium

来源：

TETRAHEDRON | 2006年 / 62卷 / 01期

关键词：

fused pyridazines; fused indoles; ring closure; Suzuki coupling; antitrypanosomal activity;

D O I：

10.1016/j.tet.2005.09.136

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

New synthetic pathways have been elaborated to 1-methyl-1H-pyridazino[3,4-b]indoles starting from halopyridazin-3(2H)-ones. Suzuki cross-coupling reaction of chloro, iodo, dichloro, and dibromo substituted pyridazin-3(2H)-ones with 2-pivaloylaminophenylboronic acid followed by hydrolysis of the amide and subsequent ring closure via condensation gave fused indoles. Some of these compounds showed biological activity as antitrypanosomal agents. (c) 2005 Elsevier Ltd. All rights reserved.

引用

页码：121 / 129

页数：9

共 32 条

[1] New synthesis of benzo-δ-carbolines, cryptolepines, and their salts:: In vitro cytotoxic, antiplasmodial, and antitrypanosomal activities of δ-caribolines, benzo-δ-carbolines, and cryptolepines [J].