CAS: 3543-73-5; Ethyl 4-(5-Amino-1-Methyl-1H-Benzo[d]Imidazol-2-yl)Butanoate

相似化合物

3543-72-4 3543-73-5 914626-62-3

上下游产品

1-甲基-5-硝基-1H-苯并咪唑-2-丁酸乙酯 4‐(1‐methyl‐5‐nitro‐1H‐benzoimidazol‐2‐yl)Butyric Acid Ethyl Ester 3543-72-4
1-甲基-5-硝基-1H-苯并咪唑-2-丁酸 4-(1-Methyl-5-Nitro-1H-Benzimidazol-2-yl)Butanoic Acid 31349-48-1

2-氟-5-硝基苯胺置于盐酸,硫酸,5% Pd/c-Iron,氢气体系中,用 乙醇,甲苯 作为反应溶剂,75.0~85.0 °C,400.01 Kpa 条件下,反应 17.0H,反应生成 5-氨基-1-甲基-1H-苯并咪唑-2-丁酸乙酯
参考文献:Process For The Preparation Of Bendamustine
标题:Process For The Preparation Of Bendamustine
摘要:该发明涉及一种从2-氟-5-硝基苯胺制备烷基4-[5-[双(2-羟乙基)氨基]-1-甲基-1H-苯并咪唑-2-基]丁酸酯(7)的方法,包括以下步骤:(a)将2-氟-5-硝基苯胺转化为5-(2-氟-5-硝基苯胺基)-5-氧代戊酸(1),使用戊二酸酐,将化合物(1)转化为甲胺基5-[2-(甲基氨基)-5-硝基苯胺基]-5-氧代戊酸酯(2),使用甲胺;将化合物(2)转化为5-[2-(甲基氨基)-5-硝基苯胺基]-5-氧代戊酸(3),并将化合物(3)缩合为4-(1-甲基-5-硝基-1H-苯并咪唑-2-基)丁酸(4);(b)酯化步骤a)的产物(4)为烷基4-(1-甲基-5-硝基1H-苯并咪唑-2-基)丁酸酯(5);(c)还原步骤b)的产物为烷基4-(5-氨基-1-甲基-1H-苯并咪唑-2-基)丁酸酯(6),以及(d)将步骤c)的产物转化为烷基4-[5-[双(2-羟乙基)氨基]-1-甲基-1H-苯并咪唑-2-基]丁酸酯(7).

专利信息

专利号:US-9643932-B2
优先权日:2011-09-26
标 题:Process for the preparation of bendamustine hydrochloride
发明人：MISHRA BHUWAN BHASKAR; KACHHADIA NIKUNJ SHAMBHUBHAI; TOMAR VINOD SINGH; LAHIRI SASWATA
权利人:FRESENIUS KABI ONCOLOGY LTD
摘要:The present invention relates to an improved process for the synthesis of bendamustine, in particular, bendamustine hydrochloride of the formula (VI) and its intermediate 1-methyl-5-[bis(2-chloroethyl)amino]-1H-benzimidazol-2-yl]lithium butanoate of formula (V), both having a purity of ≧99%, which is simple, convenient, economical, does not use hazardous chemicals and is industrially viable.