Stereoselective Synthesis of 1,2-Disubstituted β-Amino Alcohols by Nucleophilic Addition to N-tert-Butanesulfinyl α-Alkoxyaldimines
摘要:
N-tert-Butanesulfinyl alpha-alkoxyaldimines are readily prepared from protected (S)-lactals without epimerization at the alpha-stereocenter. Addition of ethyl and phenyl Grignard reagents, as well as the titanium enolate of methyl acetate, to the N-tert-butanesulfinyl aldimines provides 1,2-disubstituted beta-amino alcohols in good yields (73-98%) and with high diastereoselectivities. Either syn- or anti-amino alcohol products can be obtained by the appropriate choice of alcohol protecting groups and/or reaction conditions. Finally, deprotection of the addition products provides straightforward access to either syn- or anti-1,2-amino alcohols.
[EN] PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER<br/>[FR] DÉRIVÉS DE LA PIPÉRIDINONE EN TANT QU'INHIBITEURS DE MDM2 POUR LE TRAITEMENT DU CANCER
申请人:AMGEN INC
公开号:WO2011153509A1
公开(公告)日:2011-12-08
The present invention provides MDM2 inhibitor compounds of Formula (I), wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
[EN] PYRAZOLOPYRIMIDINE COMPOUNDS<br/>[FR] COMPOSÉS DE PYRAZOLOPYRIMIDINE
申请人:UNIV HEALTH NETWORK
公开号:WO2014075168A1
公开(公告)日:2014-05-22
The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.
本教学提供了由结构式(1-0)表示的化合物,或其药用盐。还描述了药物组合物及其使用方法。
PIPERIDINONE DERIVATIVES AS MDM2 INHIBITORS FOR THE TREATMENT OF CANCER
申请人:BARTBERGER Michael David
公开号:US20110319378A1
公开(公告)日:2011-12-29
The present invention provides MDM2 inhibitor compounds of Formula I,
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
Piperidinone derivatives as MDM2 inhibitors for the treatment of cancer
申请人:Gribble, Jr. Michael
公开号:US08569341B2
公开(公告)日:2013-10-29
The present invention provides MDM2 inhibitor compounds of Formula I,
wherein the variables are defined above, which compounds are useful as therapeutic agents, particularly for the treatment of cancers. The present invention also relates to pharmaceutical compositions that contain an MDM2 inhibitor.
The present teachings provide a compound represented by structural formula (1-0), or a pharmaceutically acceptable salt thereof. Also described are pharmaceutical compositions and methods of use thereof.