目的 合成地拉羅司并對(duì)工藝進(jìn)行優(yōu)化研究。方法 以水楊酸為原料，經(jīng)與二氯亞砜氯化、水楊酰胺脫水環(huán)合和對(duì)羧基苯肼開環(huán)重排3步得到口服鐵螯合劑地拉羅司。結(jié)果 地拉羅司合成總收率為59.36%。結(jié)論 對(duì)工藝進(jìn)行了改進(jìn)，提高了地拉羅司合成收率。

Objective To synthesize deferasirox and optimize its synthetic technology. Methods Deferasirox, an orally available iron chelator, was synthesized by cyclization of salicylaldehyde chloride with salicylamide and 4-hydrazinobenzoic acid, in which salicylaldehyde chloride was prepared with salicylic acid and thionyl chloride under normal temperature. Results Deferasirox was prepared with an overall yield of 59.36%. Conclusion The improved technology could increase the yield of deferasirox.

2012年度大學(xué)生科技創(chuàng)新項(xiàng)目（2012DKC14）