反应详情

In step 1 of Scheme A, sulfanylpyrimidine compound a is treated with peracid or like oxidizing agent to afford sulfonylpyrimidine b. In step 2, sulfonylpyrimidine b is reacted with phenol compound c in the presence of base to provide phenoxypyrimidine compound d. Phenoxypyrimidine d is then treated with hydrazine in step 3 to yield hydrazinopyrimidine compound e. In step 4, hydrazinopyrimidine compound e undergoes a cyclization under basic conditions to afford a pyrazolone compound f. In step 5 the pyrazolone compound f is protected under basic conditions to give a protected pyrazol compound g. Partial deprotection of compound g in step 6 affords pyrazol compound h. In step 7 pyrazol compound h is reacted with alkylating agent i to give pyrazol ester compound j. In step 8 pyrazol ester i is deprotected to give a compound of formula II in accordance with the invention.