DESCRIPTION: Pyrimethamine is obtained in three steps, with p- chlorophenylketonitrile as starting material. The latter is treated with ethyl propionate in the presence of sodium hydride, producing 2- propionyl-p-chlorophenylketonitrile, which undergoes o-alkylation, producing an intermediate substance which through condensation with guanidine nitrate provides pyrimethamine.
MAIN ADVANTAGES: The product and intermediates are obtained with a high degree of purity. Yields are high. Laboratory operations are reasonably simple.
MAIN APPLICATIONS: As an antimalarial drug recommended by WHO.
STAGE OF DEVELOPMENT: In the process of optimization.
PERSONS IN CHARGE: Nubia Boechat, Andre Gemal and Benjamin Gilbert
UNIT/DEPARTMENT/DIVISION: Instituto de Tecnologia em Farmacos de Manguinhos-FARMANGUINHOS / Department of Research and Technological Development