以邻苯二甲酰亚胺钾盐为起始原料,与环氧氯丙烷缩合制得N-(2,3-环氧丙基)邻苯二甲酰胺,再和二甲胺在密闭环境中加热发生亲核加成开环反应,得到N-[3-(二甲氨基)-2-羟丙基]邻苯二甲酰胺,最后再用水合肼脱去邻苯二甲酰基得到1-氨基-3-(二甲氨基)丙-2-醇,1-氨基-3-(二甲氨基)丙-2-醇成盐得目标产物.经过正交优化,关键步骤开环反应在温度为75℃、反应时间为6.0h、物料比为1∶2.5时收率可达75％.所有化合物经MS、1H NMR、13C NMR等确证结构.该合成方法简单易行,反应条件温和,总收率可达55％,能有效合成出氨基不对称取代的1,3-二氨基-2-丙醇这类重要的中间体.%2-(oxiran-2-ylmethyl)isoindoline-1,3-dione was prepared by condensation reaction,with epichloroh-ydrin and phthalimide potassium salt which as its-starting material.2-(3-(di-methylamino)-2-hydroxypropyl) isoindoline-1,3-dione was synthesized by 2-(oxiran-2-ylme-thyl)isoindoline-1,3-dione and dimethylamine which react in a high temperature sealed environment to open the epoxy ring and nucleophilic addition.At last,2-(3-(dimethylamino)-2--hydroxypropyl)isoindoline1,3-dione take off the protective group to obtain the products.After orthogonal test,when the reaction temperature was 75℃,reaction time was 6.0h,the feed ratio was 1∶ 2.5,ring opening reaction yield was 75％,All the compounds were characterized by MS,1H NMR and 13C NMR.The synthesis process is simple and reaction conditions are mild,the total yield was 55％,therefore,an import-ant intermediate such as 1,3-diamin opropan-2-ol,which is asymmetrically substituted by amino groups can be efficiently synthesized.
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