CETRIZINE SYNTHESIS, IN OPRD PAPER

Synthetic scale: 50 – 150 Kg
Step 1: 4-chlorobenzophenoneorganic reduction (sodium borohydride), methyltrioctylammonium chloride phase-transfer catalyst(toluene/water)
Step 2: thionyl chloride chlorination(toluene)
Step 3: N-(2-hydroxyethyl)piperazineamine alkylation (toluene)
Step 4: free amine liberation NaOHwater/ toluene
Step 5: 2-chloro-N,Ndimethylacetamide O-alkylation(toluene), HCl workup
Step 6: Amide hydrolysis, NaOH / water
Features: single solvent system toluene/water.