By A. Abell
ISBN-10: 0080552633
ISBN-13: 9780080552637
ISBN-10: 0762306149
ISBN-13: 9780762306145
Peptidomimetics have came across large program as bioavailable, and sometimes effective mimetics of traditional peptides. They shape the foundation of significant sessions of enzyme inhibitors, they act as receptor agonists and antagonists, and so they have even been used to imitate DNA constitution. fresh advances within the use of solid-phase natural synthesis have prepared the ground for the coaching of libraries of those buildings to permit the speedy optimization of theri organic houses and accordingly healing power. we're additionally commencing to achieve a better realizing of the structural gains of this category of compounds that effect their skill to permeate membranes, and their cost of clearance and metabolism. This quantity brings jointly a lot of those serious concerns via highlighting fresh advances in a few center peptidomimetic-based study.
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The thiomorpholinone ring could then be generated via intramolecular amide formation. Cleavage with HF/anisole then freed the thiomorpholine-3-one derivatives 68 from the solid support. The authors note that when bulky substituents are used at R I (Ph, i-Pr), poor purity was obtained. However, with simple substitutions at R l (H, Me, Et), the authors report that excellent results were obtained. Scheme 15. The Houghton synthesisof diazepines. 20 O. WALLACE, D. WHITEHOUSE, and D. DODD Scheme 16. Synthesisof thiomorpholine-3-ones.
Removal of the trityl group, acylation of the unmasked thiol, removal of Fmoc and subsequent reductive amination gave the amino acid 67. The thiomorpholinone ring could then be generated via intramolecular amide formation. Cleavage with HF/anisole then freed the thiomorpholine-3-one derivatives 68 from the solid support. The authors note that when bulky substituents are used at R I (Ph, i-Pr), poor purity was obtained. However, with simple substitutions at R l (H, Me, Et), the authors report that excellent results were obtained.
Hoekstra, W. ; Greco, M. ; Yabut, S. ; Hulshizer, B. ; Maryanoff, B. E. Tetrahedron Lett. 1997, 38, 2629. 71. Brady, S. E; Stauffer, K. ; Lumma, W. ; Smith, G. ; Ramjit, H. ; Lewis, S. ; Lucas, B. ; Gardell, S. ; Lyle, E. ; Appleby, S. ; Cook, J. ; Holahan, M. ; Stranieri, M. , J. J,; Lin, J. ; Naylor-Olsen, A. ; Vacca, J. P. J. Med. Chem. 1998, 41,401. 72. Corbett, J. ; Graciani, N. ; Mousa, S. ; DeGrado, W. E Bioorg. Med. Chem. Lett. 1997, 7, 1371. 73. Esser, C. ; Kevin, N. ; Chapman, K. T. Bioorg.
Advances in Amino Acid Mimetics and Peptidomimetics, Volume 2, Volume 2 (Advances in Amino Acid Mimetics and Peptidomimetics) (Advances in Amino Acid Mimetics and Peptidomimetics) by A. Abell
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