1.
Bioorg Med Chem Lett
; 15(10): 2523-6, 2005 May 16.
Artigo
em Inglês
| MEDLINE
| ID: mdl-15863309
RESUMO
2-Piperidones were prepared bearing heptanoic acid or a thioether heptanoic acid at the 1-position as well as appropriately substituted at the 6-position to mimic the structure of prostaglandins. The stereochemical purity at the 6-position was determined to be 95% ee for an advanced synthetic intermediate. The 2-piperidones were identified as potent agonists at the EP4 prostanoid receptor. They displayed a high affinity (Ki 5-130 nM) at EP4 and subtype selectivity.
Assuntos
Lactamas/farmacologia , Piperidonas/farmacologia , Receptores de Prostaglandina E/agonistas , Lactamas/química , Ligantes , Piperidonas/química , Receptores de Prostaglandina E Subtipo EP4
2.
Org Lett
; 5(17): 3085-8, 2003 Aug 21.
Artigo
em Inglês
| MEDLINE
| ID: mdl-12916987
RESUMO
[reaction: see text] Variations in the reagents and stoichiometries used to generate CuH in situ, as well as the nature of the ligands present, have led to a very efficient and inexpensive method for effecting hydrosilylations of dialkyl ketones.