A modified synthesis of iodoazidoaryl prazosin

被引：42

作者：

Andrus, MB ^{[1
]}

Mettath, SN ^{[1
]}

Song, C ^{[1
]}

机构：

[1] Brigham Young Univ, Dept Chem & Biochem, Provo, UT 84602 USA

来源：

JOURNAL OF ORGANIC CHEMISTRY | 2002年 / 67卷 / 23期

关键词：

D O I：

10.1021/jo026217o

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The antihypertension agent iodoazidoaryl prazosin (IAAP) has been made using a convergent route involving addition of an acylated piperazine 7 to 2-chloroquinazoline 5. IAAP has been shown to function as a multidrug resistance (MDR) reversal agent and bind to P-glycoprotein, a transmembrane transport protein. A study is also reported involving palladium-catalyzed substitution with amine heterocycles. With N,N-bis(2,6-diisopropyl)dihydroimidazolium chloride (10) as the ligand (2 mol %) for palladium(II) acetate (2 mol %) in THF at room temperature, morpholine added to 5 in 81% yield.

引用

页码：8284 / 8286

页数：3

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