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A Practical Procedure for the Synthesis of Esonarimod, (R,S)-2-Acetylthiomethyl-4- (4-methylphenyl)-4-oxobutanoic Acid, an Antirheumatic Agent. II
- Source :
- Synthetic Communications. 33:2657-2670
- Publication Year :
- 2003
- Publisher :
- Informa UK Limited, 2003.
-
Abstract
- An efficient large-scale synthesis of Esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, was established. A small amount of water increased the yield of the Michael addition of thioacetic acid (4) to 2-methylene-4-(4-methylphenyl)-4-oxobutanoic acid (2) to give 1. Multikilogram amounts of 1 (over 25 kg) were successfully obtained using this procedure. In addition, this procedure was repeated nine times, and reproducible results were obtained. See Ref. [1]
Details
- ISSN :
- 15322432 and 00397911
- Volume :
- 33
- Database :
- OpenAIRE
- Journal :
- Synthetic Communications
- Accession number :
- edsair.doi...........d7b81fc200c26144affae4e3cdfbb3da