Acid-catalyzed addition of N-hydroxyurea to 1-aryl alcohol derivatives:: A new synthesis of Zileuton

被引:5
作者
Copp, RR [1 ]
Fohey, BT [1 ]
Lannoye, G [1 ]
机构
[1] Abbott Labs, Specialty Prod Div, N Chicago, IL 60064 USA
关键词
alkylation; hydroxamic acids and derivatives; regioselection;
D O I
10.1081/SCC-100105880
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
A highly efficient synthesis of Zileuton is described in which the key step involves a site-specific alkylation of hydroxyurea under acid catalysis. Various aryl alcohol electrophiles were tested and the reaction was found to be highly substrate-specific, favoring benzothiophene and benzofuran-based alcohols.
引用
收藏
页码:3081 / 3086
页数:6
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