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A versatile and inexpensive apparatus for rapid parallel synthesis on solid support: description and synthesis
A K Saha1, L Liu, R L Simoneaux
1Medicinal Chemistry Department, Janssen Research Foundation, Welsh & McKean Roads, Spring House, Pennsylvania 19477, USA. suaaj@msn.com
Journal of Combinatorial Chemistry
|April 13, 2001
Summary
A novel, portable apparatus enables cost-effective solid-phase and parallel synthesis of compound libraries. This versatile tool supports multi-milligram scale synthesis with programmable gas and vacuum control for efficient resin handling.
Area of Science:
- Organic Chemistry
- Synthetic Chemistry
- Chemical Engineering
Background:
- Solid-phase synthesis is crucial for creating compound libraries.
- Existing portable tools for parallel synthesis are limited in capacity and functionality.
- There is a need for accessible, adaptable equipment for multi-milligram scale synthesis.
Purpose of the Study:
- To introduce a new, inexpensive, and practical apparatus for solid-phase chemistry and parallel synthesis.
- To address the gap in portable tools for synthesizing compound libraries in multi-milligram quantities.
- To demonstrate the apparatus's utility in synthesizing imidazole-based compound libraries.
Main Methods:
- The apparatus features reaction blocks with varying tube capacities (4 mL to 150 mL).
- Insert tubes with frit ends facilitate resin washing and inert atmosphere maintenance.
- An electronic controller allows programmable inert gas pulsing for mixing and vacuum for washing.
Main Results:
- The apparatus provides flexibility with configurations for 36 x 4 mL or 24 x 150 mL reaction tubes.
- It enables efficient resin manipulation through controlled gas and vacuum application.
- Successful synthesis of 4-methaneamine imidazole libraries demonstrated the apparatus's practical utility.
Conclusions:
- This apparatus offers a practical and cost-effective solution for solid-phase and parallel synthesis.
- Its portable nature and programmable features enhance flexibility for multi-milligram compound library synthesis.
- The demonstrated utility in synthesizing imidazole libraries highlights its potential for broader applications in drug discovery and materials science.