RESUMEN
Pfizer's atorvastatin (Lipitor) is a blockbuster drug for the treatment of cardiovascular diseases. In China, a critical polymorph patent of this drug has been recently invalidated by the Supreme People's Court for insufficiency of disclosure. Here, we discuss the particularities in patent litigation in China worth attention from the community.
Asunto(s)
Atorvastatina/administración & dosificación , Revelación/legislación & jurisprudencia , Inhibidores de Hidroximetilglutaril-CoA Reductasas/administración & dosificación , Patentes como Asunto/legislación & jurisprudencia , Enfermedades Cardiovasculares/tratamiento farmacológico , China , Humanos , Legislación de MedicamentosRESUMEN
TpRuPPh(3)(CH(3)CN)(2)PF(6) catalyzed the transformation of various 3-benzyl but-1-ynyl ethers into dienes and benzaldehyde at a catalyst loading of 5 mol %. This process represents an atypical pattern of transfer hydrogenation. This catalytic reaction can be applied to various derivatives of 2-ethynyl tetrahydrofurans and pyrans to cleave their ether rings and gives diene and tethered aldehyde functionalities, respectively.
RESUMEN
We report a new and efficient ruthenium-catalyzed reaction that transforms ethynyl alcohol into alkene and carbon monoxide. The most efficient catalysts are TpRu(PPh3)(CH3CN)2PF6 (10 mol %) and lithium triflate (20 mol %). The mechanism of this reaction was elucidated using an isotope-labeling experiment.
RESUMEN
We report a ruthenium-catalyzed reaction for various 3-benzyl but-1-ynyl ethers with suitable functionalities. Treatment of these substrates with TpRu(PPh3)(CH3CN)2PF6 (8.0 mol %) catalyst in 1,2-dichloroethane (80 degrees C, 12 h) afforded functionalized 1,3-dienes and benzyl aldehyde in good yields. This process is considered to be a tandem dealkoxylation and transfer hydrogenation. Deuterium-labeling experiments reveal that the migration of different hydrogen atoms proceeds regiospecifically. A plausible mechanism is proposed on the basis of the results of isotope experiment.