Lactam Enolate-Pyridone Addition: Synthesis of 4-Halocytisines

被引：16

作者：

Durkin, Patrick ^{[1
]}

Magrone, Pietro ^{[1
,2
]}

Matthews, Stella ^{[1
]}

Dallanoce, Clelia ^{[2
]}

Gallagher, Timothy ^{[1
]}

机构：

[1] Univ Bristol, Sch Chem, Bristol BS8 1TS, Avon, England

[2] Univ Milan, Dipartimento Sci Farmaceut Pietro Pratesi, I-20133 Milan, Italy

来源：

SYNLETT | 2010年 / 18期

基金：

英国工程与自然科学研究理事会;

关键词：

cytisine; 4-halocytisine; cyfusine; HALOGENATED CYTISINE DERIVATIVES; RECEPTOR PARTIAL AGONIST; SMOKING-CESSATION; NICOTINIC RECEPTORS; ALPHA-4-BETA-2; VARENICLINE; LIGANDS; ANALOGS;

D O I：

10.1055/s-0030-1259006

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The application of a lactam enolate-pyridone addition sequence, originally developed for cytisine, has been applied successfully to generate the first examples of 4-halocytisines. Variation of the lactam component provides cyfusine and 4-fluorocyfusine.

引用

页码：2789 / 2791

页数：3

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