Studies On The Synthesis Of Aromatase Inhibitor Fadrozole

The mechanisms and development of a breast cancer drug-aromatase inhabitor were briefly reviewed, and fadrozole, as a new selective, nonsteroidal aromatase inhibitor was introduced and synthesized in this thesis.The synthetic methods of fadrozole were discussed and an optimized 14- step synthetic route was chosen in the thesis. In order to reduce the cost and simplify the operating procedures, all the reaction conditions were investigated intensively. The preparations of several key intermediates were improved. The total yield reached 5.9%.The structure of target product was determined by ~1H-NMR spectra and mass spectra.