摘要
以(±)-1,2-丙二胺为起始原料,D-(-)-酒石酸为拆分剂,经拆分得(S)-1,2-丙二胺二酒石酸盐;再与氯化钾反应得(S)-1,2-丙二胺二盐酸盐;然后在氢氧化钠催化下与氯乙酸缩合制备(S)-N,N,N',N'-1,2-丙二胺四乙酸;最后与甲酰胺环合制得心脏保护剂右雷佐生。总收率为35.7%,其结构经1H NMR和IR确证。
Dexrazoxane,a cardiac medicine,was synthesized in 35.7% overall yield starting from racemic 1,2-diaminopropane.The resolution of 1,2-diaminopropane with D-(-)-tartaric acid followed by reaction with potassium chloride resulted in(S)-1,2-diaminopropane dihydrochloride,which was further converted into the title compound in two steps.The structure was confirmed with 1H NMR and IR.
出处
《精细化工中间体》
CAS
2010年第4期38-40,共3页
Fine Chemical Intermediates