Transition-metal-free azide insertion of <i>N</i>-triftosylhydrazones using a non-metallic azide source
作者:Xueyu Li、Jin-Na Song、Swastik Karmakar、Ying Lu、Ye Lv、Peiqiu Liao、Zhaohong Liu
DOI:10.1039/d2cc05442f
日期:——
Benzylic azides, an important class of active organic synthons, were synthesized in high yields from the easily accessible N-triftosylhydrazones with stable TMSN3 under mild conditions. The reaction features high efficiency and excellent functional group tolerance, as illustrated by gram-scale synthesis and the synthesis of drug-like molecules. Mechanistic studies reveal that azidation occurs at the
苄基叠氮化物是一类重要的活性有机合成子,在温和条件下从易于获得的具有稳定 TMSN 3的N -triftosylhydrazone 以高产率合成。该反应具有高效和优异的官能团耐受性,如克级合成和类药分子的合成所示。机理研究表明,通过叠氮离子消除 N 2,在缺电子的重氮碳中发生叠氮化。
INHIBITORS OF AKT ACTIVITY
申请人:Merck & Co., Inc.
公开号:EP1850843A2
公开(公告)日:2007-11-07
[EN] INHIBITORS OF AKT ACTIVITY<br/>[FR] INHIBITEURS D'ACTIVITE D'AKT
申请人:MERCK & CO INC
公开号:WO2006091395A2
公开(公告)日:2006-08-31
[EN] The instant invention provides for compounds that inhibit Akt activity. In particular, the compounds disclosed selectively inhibit one or two of the Akt isoforms. The invention also provides for compositions comprising such inhibitory compounds and methods of inhibiting Akt activity by administering the compound to a patient in need of treatment of cancer. [FR] La présente invention a trait à des composés inhibiteurs de l'activité d'Akt. En particulier, les composés de l'invention sont des inhibiteurs sélectifs d'une ou de deux isoformes d'Akt. L'invention a également trait à des compositions comportant de tels composés inhibiteurs et des procédés d'inhibition de l'activité d'Akt par l'administration du composé à un patient qui a besoin d'un traitement du cancer.