Palladium-Catalyzed Oxidative Ethoxycarbonylation of Aromatic C−H Bond with Diethyl Azodicarboxylate
作者:Wing-Yiu Yu、Wing Nga Sit、Kin-Man Lai、Zhongyuan Zhou、Albert S. C. Chan
DOI:10.1021/ja710555g
日期:2008.3.1
(DEAD) together with Oxone or K2S2O8. Substrates such as 2-arylpyridines, pyrrolidinone, acetylindoline, quinoline, and oximes were ethoxycarbonylated with excellent chemo- and regioselectivities. The catalytic reaction is probably initiated by chelation-assisted cyclopalladation of the ortho-C−H bond. Preliminary studies suggested that reactive ethoxyacyl radicals generated from thermal decomposition
Diastereoselective Addition of Chlorotitanium Enolate of <i>N</i>-Acyl Thiazolidinethione to <i>O</i>-Methyl Oximes: A Novel, Stereoselective Synthesis of α,β-Disubstituted β-Amino Carbonyl Compounds via Chiral Auxiliary Mediated Azetine Formation
作者:Narendra B. Ambhaikar、James P. Snyder、Dennis C. Liotta
DOI:10.1021/ja029871u
日期:2003.4.1
thiazolidin-2-thiones to O-methyl aldoximes. The “anti” azetines can be subsequently converted to the corresponding α,β-disubstituted β-amino carbonyl compound with retention of stereochemistry. The formation of azetine and the product of its “hydrolytic” opening has been confirmed by X-ray crystallographic analyses.
Imidazo-containing compounds (e.g., imidazoquinolines, imidazonaphthyridines, and imidazopyridines) with an oxime substituent at the 1-position, pharmaceutical compositions containing the compounds, intermediates, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases are disclosed.
GLYCOSYLTRANSFERASE REVERSIBILITY FOR SUGAR NUCLEOTIDE SYNTHESIS AND MICROSCALE SCANNING
申请人:Thorson Jon S.
公开号:US20130004979A1
公开(公告)日:2013-01-03
The present invention generally relates to materials and methods for exploiting glycosyltransferase reversibility for nucleotide diphosphate (NDP) sugar synthesis. The present invention provides engineered glycosyltransferase enzymes characterized by improved reaction reversibility and expanded sugar donor specificity as compared to corresponding non-mutated glycosyltransferase enzymes. Such reagents provide advantageous routes to NDP sugars for subsequent use in a variety of biomedical applications, including enzymatic and chemo-enzymatic glycorandomization.
The present invention discloses compounds of formula I or pharmaceutically acceptable salts, esters, or prodrugs thereof:
which inhibit serine protease activity, particularly the activity of hepatitis C virus (HCV) NS3-NS4A protease. Consequently, the compounds of the present invention interfere with the life cycle of the hepatitis C virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HCV infection. The invention also relates to methods of treating an HCV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.