RESUMEN

A practical method of synthesizing a highly selective EP4-receptor agonist 1 using Corey lactone 2 as a key intermediate was developed. Selective methanesulfonylation of the primary alcohol of the diol 8 under the newly devised conditions followed by the protection of the remaining secondary alcohol are key reactions in this new method. Further biological evaluation of 1a-b is also reported.

Asunto(s)

Receptores de Prostaglandina E/agonistas , Animales , Células Sanguíneas/efectos de los fármacos , Células Sanguíneas/metabolismo , Humanos , Interleucina-10/biosíntesis , Interleucina-10/sangre , Lipopolisacáridos/farmacología , Ratas , Subtipo EP4 de Receptores de Prostaglandina E , Transducción de Señal , Análisis Espectral , Factor de Necrosis Tumoral alfa/metabolismo