Hao Jing-shan
2006
Citations
0
Influential Citations
0
Citations
Journal
Fine Chemical Intermediates
Abstract
A Practical synthesis method of 1-(4-fluorobenzoyl)-4-(4-trifluoromethoxylbenzoyl)piperidine 1 was described. 4-Flurobenzoyl chloride 3 was treated with 1.5 equiv. of methylisonipecotate 2 in DCM in the presence of triethylamine to form compound 4 in 93.5% yield. The compound 4 then treated with aqueous LiOH to produce 5 in 97.8% yield. After the compound 5 was converted into 7 in 94.6% yield,the compound 7 then coupled with Grignard agent of compound 8 to obtain compound 1 in 71.8% yield. The overall yield of four steps was 62.1%.