- Amine-promoted asymmetric (4+2) annulations for the enantioselective synthesis of tetrahydropyridines: A traceless and recoverable auxiliary strategy
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Gone, without a trace: The in situ reaction of 2-(acetoxymethyl)buta-2,3- dienoate and a secondary amine produces a 2-methylene-3-oxobutanoate equivalent that can be used in asymmetric [4+2] annulations with N-tosylimines to provide tetrahydropyridines in
- Hu, Pengfei,Hu, Jian,Jiao, Jiajun,Tong, Xiaofeng
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- Metalloproteinase inhibitors, pharmaceutical compositions containing them, and their use
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The present invention is directed to compound of the formula I: STR1 wherein R1, R2, R3, R4, R5, X, Y, and STR2 are as defined herein. These compounds are useful for inhibiting the activity of a metalloproteinase by contacting the metalloproteinase with an effective amount of the inventive compounds.
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- Design and synthesis of novel conformationally restricted HIV protease inhibitors
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A set of HIV protease inhibitors represented by compound 2 has previously been described. Structural and conformational analysis of this compound suggested that conformational restriction of the P1/P2 portion of the molecule could lead to a novel set of potent protease inhibitors. Thus, probe compounds 3-7 were designed, synthesized, and found to be potent inhibitors of HIV protease.
- Salituro, Francesco G.,Baker, Christopher T.,Court, John J.,Deininger, David D.,Kim, Eunice E.,Li, Biquin,Novak, Perry M.,Rao, Bhisetti G.,Pazhanisamy,Porter, Margaret D.,Schairer, Wayne C.,Tung, Roger D.
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p. 3637 - 3642
(2007/10/03)
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