- A Green approach towards the synthesis of chiral alcohols using functionalized alginate immobilized Saccharomyces cerevisiae cells
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The stereochemistry of the drug molecule is gaining greater therapeutic importance and thus much attention was drawn in synthesis of chiral compounds by the pharmaceutical industry. In this study Saccharomyces cerevisiae cells immobilized on functionalize
- Muthineni, Narmada,Arnipally, Manikanta Swamy,Bojja, Sridhar,Meshram, Harshadas Mitaram,Srivastava, Ajay Kumar,Adari, Bhaskar Rao
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p. 233 - 237
(2016/12/09)
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- The discovery of novel, potent and highly selective inhibitors of inducible nitric oxide synthase (iNOS)
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By careful analysis of experimental X-ray ligand crystallographic protein data across several inhibitor series we have discovered a novel, potent and selective series of iNOS inhibitors exemplified by compound 8.
- Cheshire, David R.,?berg, Anders,Andersson, Gunilla M.K.,Andrews, Glen,Beaton, Haydn G.,Birkinshaw, Timothy N.,Boughton-Smith, Nigel,Connolly, Stephen,Cook, Tony R.,Cooper, Anne,Cooper, Sally L.,Cox, David,Dixon, John,Gensmantel, Nigel,Hamley, Peter J.,Harrison, Richard,Hartopp, Paul,K?ck, Helena,Leeson, Paul D.,Luker, Timothy,Mete, Antonio,Millichip, Ian,Nicholls, David J.,Pimm, Austen D.,St-Gallay, Steve A.,Wallace, Alan V.
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supporting information; experimental part
p. 2468 - 2471
(2011/06/17)
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- Asymmetric Schmidt reaction of hydroxyalkyl azides with ketones
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An asymmetric equivalent of the Schmidt reaction permits stereocontrol in ring expansions of symmetrical cyclohexanones. The procedure involves the reaction of chiral 1,2- and 1,3-hydroxyalkyl azides with ketones under acid catalysis; the initial reaction affords an iminium ether that can be subsequently opened with base. A systematic study of this reaction is reported, in which ketone substrates, chiral hydroxyalkyl azides, and reaction conditions are varied. Selectivities as high as ca. 98:2 are possible for the synthesis of substituted caprolactams, with up to 1,7-stereoselection involved in the overall process. The fact that either possible migrating carbon is electronically identical provides an unusual opportunity to study a ring-expansion reaction controlled entirely by stereoelectronic factors. The mechanism of the reaction and the source of its stereoselectivity are also discussed.
- Sahasrabudhe, Kiran,Gracias, Vijaya,Furness, Kelly,Smith, Brenton T.,Katz, Christopher E.,Reddy, D. Srinivasa,Aube, Jeffrey
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p. 7914 - 7922
(2007/10/03)
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- Novel use of phenylheteroakylamine derivatives
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There is disclosed the use of a compound of formula (I) wherein R1, R2, X, Y, V, W and Z are as defined in the specification, and pharmaceutically acceptable salts, enantiomers or racemates thereof, in the manufacture of a medicament, for the treatment or prophylaxis of diseases or conditions in which inhibition of nitric oxide synthase activity is beneficial. Certain novel compounds of formula (Ia) and pharmaceutically acceptable salts thereof, and enantiomers and racemates thereof are disclosed; together with processes for their preparation, compositions containing them and their use in therapy. The compounds of formulae (I) and (Ia) are inhibitors of the enzyme nitric oxide synthase and are thereby particularly useful in the treatment or prophylaxis of inflammatory disease.
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- [3H]-(R)-NPTS, a radioligand for the type 1 glycine transporter.
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The synthesis of NPTS, 6, a potent inhibitor of the type 1 glycine transporter (GlyT1) is described, as well as preparation of 6 in optically active and tritiated form for use as a radioligand for affinity displacement assay of GlyT1.
- Lowe 3rd., John A,Drozda, Susan E,Fisher, Katherine,Strick, Christine,Lebel, Lorraine,Schmidt, Christopher,Hiller, Donna,Zandi, Kathleen S
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p. 1291 - 1292
(2007/10/03)
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- 1,7-asymmetric induction in a nitrogen ring expansion process facilitated by in situ tethering
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(formula presented) There are only a few methods for the asymmetric ring expansion of prochiral ketones. Symmetrically substituted cyclohexanones can be converted to the corresponding ring-expanded caprolactam with excellent 1,7-diastereoselectivity (≥93%
- Furness, Kelly,Aubé, Jeffrey
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p. 495 - 497
(2008/02/11)
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