in black and white
Main menu
Home About us Share a book
Biology Business Chemistry Computers Culture Economics Fiction Games Guide History Management Mathematical Medicine Mental Fitnes Physics Psychology Scince Sport Technics

Solid-phase organik syntheses - Burdges K.

Burdges K. Solid-phase organik syntheses - John Wiley & Sons, 2000. - 283 p.
ISBN 0-471-22824-9
Download (direct link): phaseorganicsynthesis2000.pdf
Previous << 1 .. 23 24 25 26 27 28 < 29 > 30 31 32 33 34 35 .. 82 >> Next

91. Thompson, L. A.; Moore, F. L.; Moon, Y.-C.; Ellman, J. A. Solid-Phase Synthesis of Diverse E- and F-Series Prostaglandins, J. Org. Chem. 1998,
63, 2066-2067.
92. Johnson, C. R.; Braun, M. R A Two-Step, Three-Component Synthesis of PGE1: Utilisation of a-Iodoenones in Pd(0)-Catalysed Cross-Couplings of Organoboranes, 7. Am. Chem. Soc. 1993, 775, 11014-11015.
93. Lorsbach, B. A.; Bagdanoff, J. Ò.; Miller, R. B.; Kurth, M. J. Isoxazolinoi-soquinoline Heterocycles via Solid-Phase Reissert and Suzuki Reactions, 7. Org. Chem. 1998, 63, 2244-2250.
94. Garigipati, R. S.; Adams, B.; Adams, J. L.; Sarkar, S. K. Use of Spin Echo Magic Angle Spinning *H NMR in Reaction Monitoring in Combinatorial Organic Synthesis, 7. Org. Chem. 1996, 61, 2911-2914.
95. Fraley, Ì. E.; Rubino, R. S. Two Methods for the Preparation of 2-Cyclo-hexenones from Resin-Bound 1,3-Cyclohexanedione, Tetrahedron Lett.
1997, 38, 3365-3368.
96. Backes, B. J.; Ellman, J. A. Carbon-Carbon Bond Forming Methods on Solid Support. Utilisation of Kenner’s “Safety-Catch” Linker, 7 Am. Chem. Soc. 1994,776, 11171-11172.
97. Yoo, S.-E.; Seo, J.-S.; Yi, K.-Y.; Gong, Y.-D. Solid Phase Synthesis of Biphenyltetrazole Derivatives, Tetrahedron Lett. 1997, 38, 1203-1206.
98. Thompson, L. A.; Ellman, J. A. Straightforward and General Method for Coupling Alcohols to Solid Supports, Tetrahedron Lett. 1994, 35, 93339336.
99. Russell, R. K; Murray, W. V. Efficient Synthesis of 5-(4'-Methyl[l,l'-biphenyl]-2-yl)-lH-tetrazole, 7. Org. Chem. 1993, 58, 5023-5024.
100. Chang, L. L.; Ashton, W. Ò.; Flanagan, K. L.; Strelitz, R. A.; MacCoss, Ì.; Greenlee, W. J.; Chang, R. S. L.; Lotti, V. J.; Faust, K. A.; Chen, T.-B.; Bunting, P.; Zingaro, G. J.; Kivlighn, S. D.; Siegl, P. K. S. Triazolinones as Nonpeptide Angiotensin II Antagonists. 1. Synthesis and Evaluation of Potent 2,4,5-Trisubstituted Triazolinones, 7. Med. Chem. 1993, 36, 25582568.
101. Pavia, M. R.; Whitesides, G. Ì.; Hangauer, D. G.; Hediger, Ì. E. A Method for Preparing and Selecting Pharmaceutically Useful Non-Peptide Compounds from a Structurally Diverse Universal Library; WO 95/04277,1995.
102. Tietze, L. F.; Hippe, Ò.; Steinmetz, A. Palladium-Catalysed Allylic Substitution on Solid Support, 7. Chem. Soc. Chem. Commun. 1998, 793-794.
103. Flegelova, Z.; Patek, M. Bis-Allylic Templates for Pd(0)-Catalysed Solid Phase Synthesis of Tertiary Amines, 7. Org. Chem. 1996, 67, 6735-6738.
104. Marquais, S.; AWt, M. Aryl-Aryl Cross Coupling on a Solid Support using Zinc Organic Reagents and Palladium Catalysis, Tetrahedron Lett. 1996,37, 5491-5494.
105. Chamoin, S.; Houldsworth, S.; Snieckus, V. The Stille Cross Coupling Reactions on Solid Support. Link to Solution Phase Directed ortho Metala-tion. An Ester Linker Approach to Styryl, Biaryl and Heterobiaryl Carboxylic Acids, Tetrahedron Lett. 1998, 39, 4175-4178.
106. Chamoin, S.; Houldsworth, S.; Kruse, C. G.; Bakker, W. I.; Snieckus, V. The Suzuki-Miyaura Cross Coupling Reactions on Solid Support. Link to Solution Phase Directed ortho Metalation. The Leznoff Acetal Linker Approach to Biaryl and Heterobiaryl Aldehydes, Tetrahedron Lett. 1998, 39, 41794182.
107. Snieckus, V. Directed ortho Metalation—Tertiary Amide and o-Carbamate Directors in Synthetic Strategies for Polysubstituted Aromatics, Chem. Rev. 1990, 90, 879-933.
Solid-Phase Organic Synthesis. Edited by Kevin Burgess Copyright © 2000 John Wiley & Sons, Inc. ISBNs: 0-471-31825-6 (Hardback); 0-471-22824-9 (Electronic)
In drug discovery there are principally two useful library formats. The first may be called “primary libraries” for use in high-throughput screening, where a priori no specific structure or substructure is obligatory as a starting point. Conversely, “focused (or biased) libraries” are purposefully constructed around a known starting structure having biological activity, to be used in optimizing the activity (or other properties) of the lead compound.
Our group has recently been particularly interested in primary libraries from which pharmaceutically attractive lead molecules might hopefully be found. One goal has been to assemble a portfolio of small-molecule libraries to be used in initial lead discovery against a broad panel of emerging and proven pharmaceutical targets. Relying exclusively on solid-phase methods, we have tried to achieve a blend between generating (i) scaffolds with proven pedigree in medicinal chemistry (e.g., (3-lactams, benzodiazepines);
(ii) other templates densely packed with functional groups that have received less systematic investigation; and (iii) “novel,” unexplored chemo-types. Among questions of significant interest are the relative merits of screening numerous libraries of moderate size (say 10,000-50,000 members) comprising many different template structures, versus screening numerically larger libraries (>>100,000 members) of a limited selection of chemotypes.
Previous << 1 .. 23 24 25 26 27 28 < 29 > 30 31 32 33 34 35 .. 82 >> Next