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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-H335
Causes severe skin burns and eye damage. May cause respiratory irritation.
Precautionary Statements: P260-P264b-P271-P280-P301+P330+P331-P303+P361+P353-P304+P340-P305+P351+P338-P310-P363-P501c
Do not breathe dust/fume/gas/mist/vapours/spray. Wash face, hands and any exposed skin thoroughly after handling Use only outdoors or in a well-ventilated area. Wear protective gloves/protective clothing/eye protection/face protection. IF SWALLOWED: Rinse mouth. Do NOT induce vomiting. IF ON SKIN (or hair): Remove/Take off immediately all contaminated clothing. Rinse skin with water/shower. IF INHALED: Remove to fresh air and keep at rest in a position comfortable for breathing. IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continue rinsing. Immediately call a POISON CENTER or doctor/physician. Wash contaminated clothing before reuse. Dispose of contents/ container to an approved waste disposal plant