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Optimization of solid supports for combinatorial chemical synthesis.
1IRORI, 11149 N. Torrey Pines Road, La Jolla, CA 92037, USA.
Medicinal Research Reviews
|September 30, 1999
Summary
This review details resin selection for small molecule synthesis and introduces novel solid-phase synthesis methods. New techniques utilize activated resins and grafted surface supports for efficient library generation.
Area of Science:
- Organic Chemistry
- Materials Science
Background:
- Resins were traditionally used for peptide and oligonucleotide synthesis.
- Advancements in combinatorial chemistry have expanded resin applications to small molecule library synthesis.
Purpose of the Study:
- To review resin selection criteria for solid-phase small molecule synthesis.
- To introduce novel solid-phase synthesis methodologies and supports.
Main Methods:
- Methodology for selecting ideal resin beads for small molecule synthesis.
- Explanation of UniSphere-200 resin manufacturing.
- Description of a new approach using activated resin-bound building blocks.
- Introduction of the MicroTube grafted surface solid support.
Main Results:
- A comprehensive methodology for resin selection is presented.
- A novel solid-phase synthesis strategy using resin-linked building blocks is proposed.
- The MicroTube support enables large-scale discrete molecule synthesis via directed sorting.
Conclusions:
- Resins are increasingly vital for small molecule synthesis.
- New methods and supports offer efficient and scalable approaches for analog and library generation.