Step saver: Carbonyl groups with lower reactivities can be transformed in the presence of more reactive ones by treatment with PPh3 (or PEt3) and TMSOTf prior to the reaction (see scheme; TMS=trimethylsilyl, Tf=trifluoromethanesulfonyl). This methodology can be applied to reduction and alkylation reactions, and enabled the short asymmetric totalsynthesis of (+)‐centrolobine with the highest overall
The first demonstration of a 100% atom-efficient selective reduction of less reactive ketones over aldehydes using heterogeneous catalysts is reported. Extremely high selectivities for intra- and intermolecular reductions of ketones over aldehydes were achieved. This system was also applicable to a column reactor, leading to a gram-scale synthesis.
DALBAVANCIN COMPOSITIONS FOR TREATMENT OF BACTERIAL INFECTIONS
申请人:Stogniew Martin
公开号:US20090298749A1
公开(公告)日:2009-12-03
The invention provides methods and compositions for treatment of bacterial infections. The composition may be a combination of factors, which include A
0
, A
1
, B
1
, B
2
, C
0
, C
1
, isoB
0
, and MAG, in the presence of low level solvent. Methods of the invention include administration of dalbavancin formulations for treatment of a bacterial infection, in particular a Gram-positive bacterial infection of skin and soft tissue. Dosing regimens include multiple dose administration of dalbavancin, which often remains at therapeutic levels in the bloodstream for at least one week, providing prolonged therapeutic action against a bacterial infection. Dosing regimens for renal patients are also included.
[EN] DEAZAPURINES AND USES THEREOF<br/>[FR] DEAZAPURINES ET LEURS UTILISATIONS
申请人:EISAI CO LTD
公开号:WO2003057696A1
公开(公告)日:2003-07-17
The present invention provides compounds having formula (I), wherein R1, R2, R3 and n are as described generally and in classes and subclasses herein, and additionally provides pharmaceutical compositions thereof, and methods for the use thereof in the treatment of inflammatory or autoimmune and proliferative disorders and as inhibitors of cell adhesion molecule expression and inflammatory cytokine signal transduction generally.