CAS: 144675-97-8; 6,9-Bis((2-Aminoethyl)Amino)Benzo[g]Isoquinoline-5,10-Dione Dimaleate

3,4-吡啶二羧酸置于盐酸,Aluminum (III) Chloride,Palladium On Activated Charcoal,氢气,乙酸酐,溶剂黄146,三乙胺体系中,用 四氢呋喃,水 用作溶剂,20.0~165.0 °C,344.75 Kpa 条件下,反应 28.0H,反应生成匹杉群马来酸盐
参考文献:一种匹杉琼马来酸盐的制备方法
标题:一种匹杉琼马来酸盐的制备方法
摘要:本发明提供了一种收率高,杂质含量低,工艺简单且易于放大生产的匹杉琼马来酸盐合成方法.该方法以吡啶‑3,4‑二羧酸为起始原料,与醋酸酐反应,得到吡啶‑3,4‑二酸酐,再与1,4‑二氟苯进行傅‑克酰基化反应,所得混合物经催化环合,得到关键中间体,该中间体与经氨基保护的乙二胺反应,得含保护基的匹杉琼,然后脱保护,成盐,得到目标产物.该方法在傅‑克酰基化反应中,以硫酸的正己烷溶液作催化剂,不仅使用方便,后处理简单,而且消除了生产安全隐患;采用cbz或fmoc保护的乙二胺与取代蒽醌反应,再经过催化氢化脱去保护基,得到匹杉琼,该过程有效抑制了副反应的发生,降低了杂质含量,同时,后处理的简化,有利于收率的提高.

专利信息

专利号:US-5717099-A
优先权日:1994-03-28
标 题:Method of synthesis for 6,9-bis((2-aminoethyl)amino)benzo g!isoquinoline-5,10-dione and its dimaleate salt
发明人：SPINELLI SILVANO; DIDOMENICO ROBERTO
权利人:BOEHRINGER MANNHEIM ITALIA
摘要:In the search for novel heteroanalogs of anthracendiones, 6,9-bis (2-aminoethyl)amino!benzo g!isoquinoline-5,10-dione dimaleate salt (BBR 2778), was selected as the most promising compound. New methods of synthesis produce the compound in purity greater than 99%.

专利号:DK-0752857-T3
优先权日:1994-03-28
标 题:Improved Process for the Synthesis of 6,9-Bis [(2-Aminoethyl) -amino] Bonzo [g] Isoquinoline-5,10-Dione and its Dimaleate Salt

专利号:RU-2144028-C1
优先权日:1994-03-28
标题:Improved methods of synthesis of 6,9-bis-[(2-aminoethyl)- -amino]benzo[g]isoquinoline-5,10-dione maleate

专利号:CZ-284937-B6
优先权日:1994-03-28
标 题:Improved method for the synthesis of 6,9-bis [(2-aminoethyl) amino] benzo [g] isoquinoline-5,10-dione and its dimaleate salt

专利号:JP-3151462-B2
优先权日:1994-03-28
标 题:Improved synthesis of 6,9-bis [(2-aminomethyl) amino] benzo [g] isoquinoline-5,10-dione and its dimaleate

专利号:JP-H09507674-A
优先权日:1994-03-28
标 题 :Improved synthesis of 6,9-bis [(2-aminomethyl) amino] benzo [g] isoquinoline-5,10-dione and its dimaleate