CAS: 145202-66-0; 2-(5-((1H-1,2,4-Triazol-1-yl)Methyl)-1H-Indol-3-yl)-N,N-Dimethylethan-1-Amine Benzoate

上下游产品

benzoic acid rizatriptan 4-((1H-1,2,4-triazol-1-yl)methyl)-2-iodobenzenamine 2-[5-(1,2,4-triazol-1-ylmethyl)-1H-indol-3-yl]ethyl alcohol

N,N-二甲基色胺置于三乙基硅烷,硫酸,溶剂黄146,三氟乙酸,2,3-二氯-5,6-二氰基-1,4-苯醌,Sodium Hydroxide体系中,用 甲醇,乙醇,甲苯 用作溶剂,化学反应 11.0H,反应生成苯甲酸利扎曲坦
参考文献:一种制备苯甲酸利扎曲坦的方法
标题:一种制备苯甲酸利扎曲坦的方法
摘要:本发明公开了一种新的苯甲酸利扎曲坦的制备方法.该制备方法以色胺为起始原料,经过n,N甲基化,还原,上保护,三氮唑甲基化,脱保护,脱氢,成盐七步反应,得到高纯度的苯甲酸利扎曲坦.该方法的创新之处在于采用了一种全新的方法构建吲哚环,避免了现有路线中使用的fisher吲哚合成法而带来的产品杂质含量高,难于纯化的缺点.该方法的优点为:操作简便,反应条件温和,无昂贵试剂,不需要柱层析纯化,产品纯度高.

专利信息

专利号:US-7786156-B2
优先权日:2004-01-28
标 题 :Synthesis methods and intermediates for the manufacture of Rizatriptan
发明人：MARTIN PIERRE; BERENS ULRICH; BOUDIER ANDREAS; DOSENBACH OLIVER
权利人:RATIOPHARM GMBH
摘要:The invention relates to a process for the manufacture of an 1,2,4-triazol-1-yl compound of the formula [A], n nor a salt thereof, wherein each of R3 and R4 is hydrogen or lower alkyl, said process comprising reacting a hydrazine compound of the formula [B]n n nwherein R is hydrogen or acyl, R2 is hydrogen or a protecting group, are hydrogen or lower alkyl, and R6 is hydrogen or COOR7, or a salt thereof, with a 1,2,4-triazolyl forming reagent.n n In addition, novel intermediates for the synthesis of the anti-migraine agent Rizatriptan and methods for their synthesis are presented.

专利号:US-9359376-B2
优先权日:2011-04-08
标题:Substituted methylformyl reagents and method of using same to modify physicochemical and/or pharmacokinetic properties of compounds
发明人：DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER
权利人:DUGAR SUNDEEP; MAHAJAN DINESH; HOLLINGER FRANK PETER; SPHAERA PHARMA PTE LTD
摘要:The present invention relates to the synthesis and application of novel chiral/achiral substituted methyl formyl reagents to modify pharmaceutical agents and/or biologically active substances to modify the physicochemical, biological and/or pharmacokinetic properties of the resulting compounds from the unmodified original agent.

专利号:CN-115073385-A
优先权日:2022-07-04
标 题 :Application of microchannel continuous flow reaction technology in the synthesis of rizatriptan benzoate

专利号:US-7547436-B2
优先权日:1995-01-17
标 题:Receptor specific transepithelial transport of therapeutics
发明人：BLUMBERG RICHARD S; LENCER WAYNE I; SIMISTER NEIL E
权利人:BRIGHAM & WOMENS HOSPITAL; UNIV BRANDEIS
摘要:The present invention relates in general to methods and products for initiating an immune response against an antigen, and in particular relates to transepithelial delivery of antigens to provoke tolerance and immunity. The present invention further relates to methods and products for the transepithelial delivery of therapeutics. In particular, the invention relates to methods and compositions for the delivery of therapeutics conjugated to a FcRn binding partner to intestinal epithelium, mucosal epithelium and epithelium of the lung. The present invention further relates to the synthesis, preparation and use of the FcRn binding partner conjugates as, or in, pharmaceutical compositions for oral systemic delivery of drugs and vaccines.

专利号:CN-115353492-A
优先权日:2022-08-26
标 题:A method for continuous synthesis of 1-(4-hydrazinophenyl)methyl-1,2,4-triazole

专利号:US-11285169-B2
优先权日:2013-03-13
标题 :Methods for modulating chemotherapeutic cytotoxicity
发明人：ROBERTS DAVID D; SOTO PANTOJA DAVID R
权利人:US HEALTH
摘要:Methods of reducing cytotoxicity of a chemotherapeutic agent to non-cancer cells by administering to a subject with cancer an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent, such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are provided. Example disclosed methods reduce cardiotoxicity. In one example, the methods include administering to a subject with cancer an effective amount of a CD47 antisense morpholino oligonucleotide and an anthracycline such as doxorubicin. Methods of increasing cytotoxicity of a chemotherapeutic agent in cancer cells by administering to a subject with a tumor an effective amount of an agent that inhibits CD47 signaling and a DNA damaging agent such as an anthracycline, topoisomerase inhibitor, or nucleotide synthesis inhibitor, are also provided. In some embodiments, the inhibitor of CD47 signaling is administered to the subject before, during, or after the administration of the DNA damaging agent.