AI Article Synopsis
- The text describes a method for synthesizing alpha,beta-unsaturated gamma-sultines using magnesium-mediated carbometalation on propargyl alcohols through a Grignard addition.
- Thio-rofecoxib, a selective COX-2 inhibitor, is produced using this synthesis method.
- Key performance metrics for thio-rofecoxib, including its IC(50) for COX-1 and COX-2 inhibition and stability in whole blood, are provided.
Article Abstract
Magnesium mediated carbometalation (Grignard addition) to appropriate propargyl alcohols to synthesize a cross-section of variably substituted alpha,beta-unsaturated gamma-sultines is described. Thio-rofecoxib, a selective COX-2 inhibitor (12), is synthesized by this method and its IC(50), microM COX-1 and COX-2 inhibition, and whole blood stability values reported.
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| http://dx.doi.org/10.1016/j.bmcl.2005.02.056 | DOI Listing |
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