Formation of Enantiopure 5-Substituted Oxazolidinones through Enzyme-Catalysed Kinetic Resolution of Epoxides
摘要:
Halohydrin dehalogenase from Agrobacterium radiobacter catalyzed the enantioselective ring opening of terminal epoxides with cyanate as a nucleophile, yielding 5-substituted oxazolidinones in high yields and with high enantiopurity (69-98% ee). This is the first example of the biocatalytic conversion of a range of epoxides to the corresponding oxazolidinones.
Formation of Enantiopure 5-Substituted Oxazolidinones through Enzyme-Catalysed Kinetic Resolution of Epoxides
摘要:
Halohydrin dehalogenase from Agrobacterium radiobacter catalyzed the enantioselective ring opening of terminal epoxides with cyanate as a nucleophile, yielding 5-substituted oxazolidinones in high yields and with high enantiopurity (69-98% ee). This is the first example of the biocatalytic conversion of a range of epoxides to the corresponding oxazolidinones.
[EN] PYRIDAZINONE-BASED BROAD SPECTRUM ANTI-INFLUENZA INHIBITORS<br/>[FR] INHIBITEURS ANTIGRIPPAUX À LARGE SPECTRE À BASE DE PYRIDAZINONE
申请人:HOFFMANN LA ROCHE
公开号:WO2018001948A1
公开(公告)日:2018-01-04
The present invention relates to compounds of formula (I): (I) or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
Provided are triazole derivatives of Formula I which are potent inhibitors of spleen tyrosine kinase and pharmaceutical composition. The triazole derivatives are useful in the treatment and prevention of diseases mediated by said enzyme, such as asthma, COPD, rheumatoid arthritis, and cancer.