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Classical acetamidomalonate addition/decarboxylative hydrolysis as the key step for the generation of the amino acidic moiety starting from 4-ethylsulfonyl-α-bromoacetophenone prepared in two steps from commercially available 4-acetyl-benzenesulfonyl chloride. This then treated with sodium sulfite in basic aqueous conditions yielded the sodium sulfinate.
Roberto Pellicciari Prof.1,; Rosa C. Rizzo Dr.,; Gabriele Costantino Prof.,; Maura Marinozzi Prof.,; Laura Amori Dr.,; Paolo Guidetti Dr.,; Hui-Qiu Wu Dr.,; Robert Schwarcz Dr. Modulators of the Kynurenine Pathway of Tryptophan Metabolism: Synthesis and Preliminary Biological Evaluation of (S)-4-(Ethylsulfonyl)benzoylalanine, a Potent and Selective Kynurenine Aminotransferase II (KAT II) Inhibitor. ChemMedChem. 2006, 1 (5), 528-531.
Hazard Statements: H314-H318
Causes severe skin burns and eye damage. Causes serious eye damage.
Precautionary Statements: P260u-P303+P361+P353-P305+P351+P338-P301+P330+P331-P405-P501a
IF ON SKIN (or hair): Remove/Take off immediately all contaminated clothing. Rinse skin with water/shower. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. Store locked up. Dispose of contents/container in accordance with local/regional/national/international regulations.