A highly efficient asymmetric hydrogenation of γ- and δ-ketoacids was developed by using a chiral spiro iridium catalyst (S)-1a, affording the optically active γ- and δ-hydroxy acids/lactones in high yields with excellent enantioselectivities (up to >99% ee) and turnover numbers (TON up to 100000). This protocol provides an efficient and practical method for enantioselective synthesis of Ezetimibe
Nitroderivatives of prostaglandins having improved pharmacological activity and enhanced tolerability are described. They can be employed for the treatment of glaucoma and ocular hypertension.
Gamma lactams as prostaglandin agonists and use thereof
申请人:Araldi Luca Gian
公开号:US20050288357A1
公开(公告)日:2005-12-29
1,2-substituted 5-pyrrolidinone compounds are provided, and methods of treatment and pharmaceutical composition that utilize or comprise one or more such compounds. Compounds of the invention are useful for a variety of therapies, including treating or preventing preterm labor, dysmenorrhea, asthma, hypertension, infertility or fertility disorder, undesired blood clotting, preeclampsia or eclampsia, an eosinophil disorder, sexual dysfunction, osteporosis and other destructive bone disease or disorder, renal dysfunction, an immune deficiency disorder, dry eye, ichthyosis, elevated intraocular pressure, sleep disorder, or gastric ulcer, inflammatory disorders and other diseases and disorders associated with the prostaglandin family of compounds.
Method for Production of Optically Active (1S)-3-Chloro-1-(2-Thienyl)-Propan-1-Ol
申请人:Breuer Michael
公开号:US20080319208A1
公开(公告)日:2008-12-25
A process for preparing optically active (1S)-3-chloro-1-(2-thienyl)propan-1-ol of the formula I
by, in a medium comprising 3-chloro-1-(2-thienyl)propan-1-one of the formula II
reducing this compound to the compound of the formula I by means of an alcohol dehydrogenase from the
Thermoanaerobacter
genus, and isolating the product formed in substantially enantiomerically pure form.
Synthesis of 1,3-dioxin-4-ones having chiral hydroxyalkyl groups at the 6-position by means of baker's yeast reduction and their uses for epc synthesis
Prochiral methyl ketones connected with 6-(4-oxo-1,3-dioxinyl) group directly or through methylene chain (1-3) gave, by treatment with fermenting baker's yeast, the corresponding (S)-alcohols which served as synthons for a variety of enantiomerically pure compounds.