Target: Cetirizine

06 July 2012 - The Free Chemical Abstract Service

cetirizine synthesis Reiter 2012  Target: Cetirizine
Authors:Reiter, Trinka, Bartha ,Pongo, Volk, Simig
Publication: DOI
Synthetic scale: 50 - 150 Kg
Step 1: 4-chlorobenzophenone organic reduction (sodium borohydride), methyltrioctylammonium chloride phase-transfer catalyst (toluene/water)
Step 2: thionyl chloride chlorination (toluene)
Step 3: N-(2-hydroxyethyl)piperazine amine alkylation (toluene)
Step 4: free amine liberation NaOH water/ toluene
Step 5: 2-chloro-N,Ndimethylacetamide O-alkylation (toluene), HCl workup
Step 6: Amide hydrolysis, NaOH / water
Features: patent noninfringing, single solvent system toluene/water.