CAS: 147084-10-4; 11-(1-Methylpiperidin-4-Ylidene)-6,11-Dihydro-5H-Benzo[d]Imidazo[1,2-A]Azepine-3-Carbaldehyde

上下游产品

6,11-Dihydro-11-(1-Methyl-4-Piperidinylidene)-5H-Imidazo[2,1-B][3]-Benzazepine
5,6-Dihydro-11-(1-Methyl-4-Piperidinylidene)-11H-Imidazo[2,1-B][3]Benzazepine
11-Piperidin-4-Ylidene-6,11-Dihydro-5H-Imidazo[2,1-B]-[3]Benzazepine 142654-73-7

📜1-苯乙腈咪唑置于甲酸,氢溴酸,Potassium Acetate,溶剂黄146,三乙胺,Sodium Hydroxide体系中,用 水,乙腈 用作溶剂,化学反应 15.0H,反应生成阿卡他定
参考文献:Investigation Of Alcaftadine Using A Double Oxidation Process By Eliminating Column Chromatography
标题:Investigation Of Alcaftadine Using A Double Oxidation Process By Eliminating Column Chromatography
摘要:阿尔卡法丁是一种活性药物成分(api),用于眼科溶液,用于预防与过敏性结膜炎相关的瘙痒.最初报道的合成方法使用耗时的柱层析技术来分离羟甲基化产物醇(10).使用氧化级锰矿石的简单而有效的双氧化策略,避免了繁琐的色谱纯化.首先,使用少量mno2对羟甲基化的粗质量(化合物9,10和16的混合物)进行部分氧化,以去除关键的二醇杂质(16)并允许醇(10)粗品结晶,然后使用额外的mno2进行第二次氧化,以通过可扩展的过程提供阿尔卡法丁.这种合成方法已被证明具有成本效益和商业可行性.还确定并消除了过程中形成的各种杂质,以获得符合ich指南的阿尔卡法丁api纯度.该过程已在工厂规模上得到验证,并提交了美国dmf以制造阿尔卡法丁api.
Doi:10.14233/ajchem.2022.23672

专利信息

专利号:WO-2023075715-A1
优先权日:2021-10-26
标题 :A pharmaceutical formulation including leukotriene receptor antagonists and/or leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (nsaids)
发明人：OYTUN FARUK; CAN EFE
权利人:VSY BIYOTEKNOLOJI VE ILAC SANAYI ANONIM SIRKETI
摘要:This invention is related to a pharmaceutical formulation including Leukotriene receptor antagonists and/or Leukotriene synthesis inhibitors combined with non-steroidal anti-inflammatory drugs (NSAIDs) and antihistamines in ocular diseases and in inflammatory and allergic diseases for systemic and topical use. The objective of this invention is to create a novel formulation to be effective as much as steroids while having significantly less side effects for long-term use in treating ocular diseases, inflammatory and allergic diseases. In other words our aim is to achieve the inhibition of pro-inflammatory mediators (prostaglandins, thromboxane, histamine and leukotrienes) as much as steroids do with a safer combination.