[EN] AMINOPYRIMIDINES AS SYK INHIBITORS<br/>[FR] AMINOPYRIMIDINES EN TANT QU'INHIBITEURS DE LA SYK
申请人:MERCK SHARP & DOHME
公开号:WO2011075515A1
公开(公告)日:2011-06-23
The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
The present invention provides novel pyrimidine amines of formula (I) which are potent inhibitors of spleen tyrosine kinase, and are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD and rheumatoid arthritis.
A reductive coupling strategy towards ripostatin A
作者:Kristin D Schleicher、Timothy F Jamison
DOI:10.3762/bjoc.9.175
日期:——
nickel(0)-catalyzed coupling with a model epoxide. Several synthetic approaches toward the C10-C26 epoxide have been pursued. The C13 stereocenter can be set by allylation and reductivedecyanation of a cyanohydrinacetonide. A mild, fluoride-promoted decarboxylation enables construction of the C15-C16 bond by an aldol reaction. The product of this transformation is of the correct oxidation state and