The steroid 3, with three independently-addressable, rigidly-positioned functional groups, has been synthesized in an efficient, multi-gram sequence from inexpensive cholic acid 1. Compound 3 should prove valuable as a starting point for combinatorial libraries with preorganised, co-directed arrays
A novel isoxazole-based scaffold for combinatorial chemistry
โ Scribed by S Batra; S.K Rastogi; B Kundu; A Patra; A.P Bhaduri
- Publisher
- Elsevier Science
- Year
- 2000
- Tongue
- French
- Weight
- 137 KB
- Volume
- 41
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
A novel isoxazole-based scaold has been identiยฎed for the generation of combinatorial libraries using solid-phase methods. This scaold has been utilized to aord high value synthetic intermediates through BaylisยฑHillman reaction, Wittig reaction, nitroaldol condensation, and imine and oxime formation. The utility of the scaold has been demonstrated by synthesizing a small library of 32 isoxazole substituted g-amino alcohol using four activated alkenes and eight amines.
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Combinatorial chemistry opens up new possibilities for research in medicinal chemistry in both the search for lead structures and their rapid optimization.['] Nevertheless, though many peptides are already the first milestones along this path, the optimization of sequences suitable for their combina