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Prostaglandin prodrugs I: Stabilization of dinoprostone (prostaglandin E2) in solid state through formation of crystalline C1-phenyl esters

✍ Scribed by W. Morozowich; T. O. Oesterling; W. L. Miller; C. F. Lawson; J. R. Weeks; R. G. Stehle; S. L. Douglas


Publisher
John Wiley and Sons
Year
1979
Tongue
English
Weight
405 KB
Volume
68
Category
Article
ISSN
0022-3549

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✦ Synopsis


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.