SYNTHESIS OF 4-SUBSTITUTED 11-PHENYL-1,2,3,4-TETRAHYDRO-5H-AZEPINO[3,4-B]QUINOLIN-5-ONE DERIVATIVES AS POTENTIAL PERIPHERAL BENZODIAZEPINE-RECEPTOR LIGANDS

被引：3

作者：

CAPPELLI, A

ANZINI, M

VOMERO, S

机构：

[1] Dipartimento Farmaco Chimico Tecnologico - Università di Siena - Banchi di Sotto

来源：

HETEROCYCLES | 1994年 / 38卷 / 06期

关键词：

D O I：

10.3987/COM-93-6662

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The synthesis of semirigid analogs of PK 11195, the highly specific peripheral benzodiazepine-receptor ligand, is reported. Compound (4) underwent the Wittig reaction with acetaldehyde to give olefin (7) which after allylic bromination was aminated to give the omega-amino esters (10a-c). These compounds were then hydrogenated and cyclized in boiling toluene with DMAP as catalyst. The standard procedure failed in the case of compound (10b), thus other cyclization procedures were examinated.

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页码：1265 / 1272

页数：8

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