Partial synthesis of major human metabolites of docetaxel
摘要:
The structures and synthesis of the four major human metabolites of docetaxel are reported. These metabolites, i.e. compounds 3, 4a,b and 5, are side-chain oxidation derivatives. They were prepared by partial synthesis from the previously described amino-taxoid 8 using mixed-carbonates as acylation reagents. In vitro biological activities are detailed.
with a proximal alkoxy group is reported. This reaction, in the presence of a [Rh(cycloocta‐1,5‐diene)Cl]2/propane‐1,3‐diylbis(diphenylphosphane) system under a CO atmosphere, constitutes a powerful tool for selectively accessing carbo‐ and heterobicyclo[5.3.0] frameworks featuring an enol ether moiety. Through this procedure, a straightforward access to guaiane skeletons with a tertiary hydroxy group
Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis.
US8334290B2
申请人:——
公开号:US8334290B2
公开(公告)日:2012-12-18
[EN] CETP INHIBITORS<br/>[FR] INHIBITEURS DE LA CETP
申请人:MERCK & CO INC
公开号:WO2007070173A2
公开(公告)日:2007-06-21
[EN] Compounds of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis. I [FR] La présente invention concerne des composés de la formule I, y compris des sels pharmaceutiquement acceptables des composés, qui sont des inhibiteurs de la CETP et qui sont utiles pour augmenter le cholestérol HDL, réduire le cholestérol LDL et traiter ou prévenir l'athérosclérose. I