PROSTAGLANDIN PRODRUGS .1. STABILIZATION OF DINOPROSTONE (PROSTAGLANDIN-E2) IN SOLID-STATE THROUGH FORMATION OF CRYSTALLINE C1-PHENYL ESTERS

被引:15
作者
MOROZOWICH, W
OESTERLING, TO
MILLER, WL
LAWSON, CF
WEEKS, JR
STEHLE, RG
DOUGLAS, SL
机构
[1] Research Laboratories, Upjohn Company, Kalamazoo, Michigan
关键词
Prodrugs—dinoprostone; stabilization in solid state of crystalline C[!sub]1[!/sub]‐phenyl esters; biological activity; Prostaglandins—dinoprostone; prodrugs;
D O I
10.1002/jps.2600680711
中图分类号
R914 [药物化学];
学科分类号
100701 ;
摘要
Dinoprostone para‐substituted phenyl esters were synthesized in attempt to improve the solid‐state stability of the parent prostaglandin. A phenol series covering a wide melting‐point range was employed, and a linear relationship was observed between the phenol melting points and the resulting prostaglandin C1‐ester melting points. The crystalline esters showed improved solid‐state stability over the parent compound, and many esters were biologically active. Copyright © 1979 Wiley‐Liss, Inc., A Wiley Company
引用
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页码:833 / 836
页数:4
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