Study on the Six-Step Synthesis of the Anti-hepatitis C Virus Drug Vepatasvir
Compound 1 is prepared by condensation reaction using 1b and 1a,which have already been mass-produced and supplied domestically,as raw materials.Under the action of cesium carbonate,compound 1 and 2a react to form compound 2.Subsequently,compound 2 reacted with ammonium acetate to form compound 3.Compound 3 undergoes oxidative dehydrogenation reaction to generate the important compound 4.By separating the tert butoxycarbonyl group from compound 4,compound 5 can be prepared.Compound 5 undergoes amide condensation reaction with MOC-D-phenylglycine under the action of 2-chloro-4,6-dimethoxy-1,3,5-triazine to obtain the target compound vipatavir(Compound 6).This synthesis method has the advantages of short route,cheap and easy to obtain raw materials,mild reaction conditions in each step,simple operation,safety,etc.