Dexrazoxane hydrochloride, ADR-529(free base), NSC-169780(free base), ICRF-187, TopoTect, Zinecard, Cardioxane

合成路线:The chiral diamine (II) was obtained by resolution of racemic 1,2-diaminopropane (I) with D-tartaric acid.Condensation of diamine (II) with formaldehyde and NaCN produced the tetranitrile (III).Acidic hydrolysis of tetranitrile (III) produced tetraamide (VI).The cyclization of (VI) upon heating in phenol furnished the title bis-piperazinedione.The cyclization of tetraamide (VI) has also been reported using polyphosphoric acid or sodium (methylsulfinyl)methyde.Alternatively,the synthesis of Dexrazoxane can be performed by by alkylation of diamine (II) with chloroacetic acid (IV) by means of NaOH in water to afford tetraacid (V),which is then subjected to cyclization in hot formamide.

参考文献标题:Process for preparing bis(3,5-dioxopiperazinyl)alkanes or alkenes
文献作者:Tu,C.-Y.J.; Clark,G.W.; Borsotti,G.
参考来源:EP 0330381


合成路线:The chiral diamine (II) was obtained by resolution of racemic 1,2-diaminopropane (I) with D-tartaric acid.Condensation of diamine (II) with formaldehyde and NaCN produced the tetranitrile (III).Acidic hydrolysis of tetranitrile (III) produced tetraamide (VI).The cyclization of (VI) upon heating in phenol furnished the title bis-piperazinedione.The cyclization of tetraamide (VI) has also been reported using polyphosphoric acid or sodium (methylsulfinyl)methyde.Alternatively,the synthesis of Dexrazoxane can be performed by by alkylation of diamine (II) with chloroacetic acid (IV) by means of NaOH in water to afford tetraacid (V),which is then subjected to cyclization in hot formamide.

参考文献标题:Process for preparing (S)(+)-4,4'-(1-methyl-1,2-ethanediyl)-bis(2,6-piperazinedione)
文献作者:Holthuis,J.J.M.; MacDonald,P.L.; Stradi,R.; Rossetto,P.(EuroCetus BV)
参考来源:WO 9308172


合成路线:The chiral diamine (II) was obtained by resolution of racemic 1,2-diaminopropane (I) with D-tartaric acid.Condensation of diamine (II) with formaldehyde and NaCN produced the tetranitrile (III).Acidic hydrolysis of tetranitrile (III) produced tetraamide (VI).The cyclization of (VI) upon heating in phenol furnished the title bis-piperazinedione.The cyclization of tetraamide (VI) has also been reported using polyphosphoric acid or sodium (methylsulfinyl)methyde.Alternatively,the synthesis of Dexrazoxane can be performed by by alkylation of diamine (II) with chloroacetic acid (IV) by means of NaOH in water to afford tetraacid (V),which is then subjected to cyclization in hot formamide.
参考文献标题:(3,5,3',5'-Tetraoxo)-1,2-dipiperazinoalkane cpds.and process for their preparation
文献作者:Creighton,A.M.(National Research Development Corp.)
参考来源:DE 1910283; DE 1967027


产品链接: CAS No. 24584-09-6››