Microwave-assisted amide synthesis on silica-supported carbodiimide

ORGN 64

Shahnaz Ghassemi, Biotage, Inc, Charlottesville, VA 22911 and Peter. C. Rahn, R & D, Biotage, Inc, P.O. Box 8006, Charlottesville, VA 22906.
Microwave is used for rapid optimization of amide synthesis using silica-supported carbodiimide reagent. The effect of solvent, concentration, stoichiometry, coupling additive and time were studied to determine optimum set of reaction conditions. Using the optimized microwave reaction conditions an array of compounds was synthesized utilizing the combination of microwave and Syntage carbodimidine cartridges followed by the Flash purification of the product. The combination of microwave heating of Syntage carbodimidine cartridge and flash purification resulted in reducing the overall reaction time and eliminated multiple handling steps and overall the yield was higher than traditional synthesis and purification steps.
 

New Reactions and Methodology, Metal-Mediated Reactions, Heterocycles and Aromatics
8:00 PM-10:00 PM, Sunday, March 28, 2004 Anaheim Convention Center -- Hall A, Poster

Sci-Mix
8:00 PM-10:00 PM, Monday, March 29, 2004 Anaheim Convention Center -- Hall A, Sci-Mix

Division of Organic Chemistry

The 227th ACS National Meeting, Anaheim, CA, March 28-April 1, 2004