SYNTHESIS OF NEW AMIDE-LINKED N-HYDROXYUREA 5-LIPOXYGENASE INHIBITORS BY AN INTRAMOLECULAR OXYGEN TO NITROGEN ACYL TRANSFER

被引：5

作者：

DELLARIA, JF

SALLIN, KJ

RODRIQUES, K

机构：

[1] Immunosciences Research Area, Department 47K, Abbott Laboratories, Abbott Park

来源：

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 1993年 / 3卷 / 02期

关键词：

D O I：

10.1016/S0960-894X(01)80898-2

中图分类号：

R914 [药物化学];

学科分类号：

100701 [药物化学];

摘要：

A convergent and efficient synthesis of amide-linked N-hydroxyurea 5-lipoxygenase inhibitors is reported. The synthesis involves a one-pot, three-step procedure where an appropriately substituted N-hydroxy-N-[2-((tert-butyloxycarbonyl)amino)ethyl]urea isp O-acylated with the desired acid chloride. The O-acyl intermediate was N-deprotected in situ, and the resulting amine salt neutralized to induce an intramolecular acyl transfer from oxygen to nitrogen.

引用

页码：305 / 308

页数：4