CAS: 14009-24-6; (Z)-1-(3,4-Diethoxybenzylidene)-6,7-Diethoxy-1,2,3,4-Tetrahydroisoquinoline

📜N-[2-(3,4-二乙氧基苯基)乙基]-2-(3,4-二乙氧基苯基)乙酰胺置于硫酸体系中,用 5,5-Dimethyl-1,3-Cyclohexadiene 用作溶剂,化学反应 3.5H,以33 G的收率获得盐酸屈他维林
参考文献:一种盐酸屈他维林降解杂质的制备方法
标题:一种盐酸屈他维林降解杂质的制备方法
摘要:本发明公开了一种盐酸屈他维林降解杂质的制备方法,属于医药合成领域.本发明首次发现,除了盐酸屈他维林的生产过程中的屈他维林酮和乙基罂粟碱这两种杂质外,还会在该药品贮藏过程中产生第三种盐酸屈他维林杂质,本发明公开了该杂质的具体结构,以及制备该杂质的具体方法,包括:将屈他维林缩合物溶于溶剂中,加入酸进行环合反应生成屈他维林;再将屈他维林溶于溶剂中进行催化脱氢反应,生成乙基罂粟碱;最后将乙基罂粟碱溶于溶剂中,加入氧化剂进行氧化,即得所述第三种盐酸屈他维林杂质.由于药品杂质的发现及研究对于提高药品的质控标准及用药的安全性具有重要意义,本发明将在盐酸屈他维林的药品生产中具有重要应用价值.

专利信息

专利号:US-2014255341-A1
优先权日:2011-07-22
标题:Tumor Selective Chemokine Modulation
发明人：KALINSKI PAWEL; MUTHUSWAMY RAVIKUMAR
权利人:KALINSKI PAWEL; MUTHUSWAMY RAVIKUMAR
摘要:Therapies effective for the treatment and prevention of cancer and other diseases are disclosed. These methods include the administration of therapeutically effective amounts of agents that increase the local production of effector cell-attracting chemokines within tumor lesions, with concomitant suppression of local production of undesirable chemokines that attract regulatory T(reg) cells. These methods include administering to the subject therapeutically effective amounts of a Toll-like receptor (TLR) agonist or other activator of NF-KB pathway in combination with a blocker of prostaglandin synthesis or a blocker of prostaglandin signaling, in combination with a type-1 interferon, or in combination with both a blocker of prostaglandin synthesis or signaling and with a type-1 interferon. Alternatively, the methods derived from the same paradigms, but aimed to treat or prevent autoimmune disease, chronic inflammatory disease, transplant rejection or GvR, include the combination of a Toll-like receptor (TLR) agonist in combination with a prostaglandin or other cAMP-activator.