- Non-Peptide Fibrinogen Receptor Antagonists. 7. Design and Synthesis of a Potent, Orally Active Fibrinogen Receptor Antagonist
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The design, synthesis, and pharmacological evaluation of L-734,217, a potent, low-molecular weight, orally active fibrinogen receptor antagonist, is reported.A strategy for producing low-molecular weight inhibitors from the peptide c-A, previou
- Duggan, Mark E.,Naylor-Olsen, Adel M.,Perkins, James J.,Anderson, Paul S.,Chang, Charles T.-C.,et al.
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- A highly efficient synthesis of fibrinogen receptor antagonist L-734,217 via a novel chemoselective silyl-mediated conjugate addition of δ-lactams to 4-vinylpyridine
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A highly practical chromatography-free six-step synthesis of L-734,217 suitable for large scale preparation is described. The key chiral pyridine acid intermediate (R)-1 was prepared in four steps based on a novel chemoselective silyl-mediated conjugate a
- Chung, John Y. L.,Hughes, David L.,Zhao, Dalian,Song, Zhiguo,Mathre, David J.,Ho, Guo-Jie,McNamara, James M.,Douglas, Alan W.,Reamer,Tsay, Fuh-Rong,Varsolona, Richard,McCauley, James,Grabowski, Edward J. J.,Reider, Paul J.
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p. 215 - 222
(2007/10/03)
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- Asymmetric hydrogenation of 3-alkylidene-2-piperidones using Noyori's catalyst. Effect of N-substituents on the enantioselectivity
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The enantioselectivity in the asymmetric hydrogenation of 3-alkylidene-2-piperidones catalyzed by BINAP-Ru(II) complex was found to be significantly effected by the internal substituents on the lactam nitrogen, affording the corresponding 3-alkyl-2-piperidones in 52-92% ee.
- Chung, John Y. L.,Zhao, Dalian,Hughes, David L.,McNamara, James M.,Grabowski, Edward J. J.,Reider, Paul J.
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p. 7379 - 7382
(2007/10/02)
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