CAS: 76824-16-3; 3-(((2-Guanidinothiazol-4-yl)Methyl)Thio)Propanamide

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上下游产品

-4-thiazolyl>methyl>thio>propionimidatemethyl 3-2-(diaminomethylene)amino-4-thiazolylmethylthiopropionimidate famotidine 3-(2-aminothiazol-4-yl-methylthio)propionitrile N''-[4-[[(2-cyanoethyl)thio]methyl]-2-thiazolyl]-guanidine

合成工艺路线路线简述

  • 合成目标产物 Famotidine Amide Impurity 主要起始原料 3-(2-Guanidino-Thiazol-4-Yl-Methylthio)-Propionitrile
  • 76824-35-6 + 100-52-7 = 76824-16-3 + 106433-44-7 + 129083-44-9 + 1994267-84-3 + 90237-03-9 + 89268-62-2 + 124646-10-2 + 107880-74-0
    反应条件:1.1 Solvents: Water; 4 H,80 °C
    标题:Identification,Synthesis,And Characterization Of Unknown Impurity In The Famotidine Powder For Oral Suspension Due To Excipient Interaction By Uplc-Ms/ms And Nmr
    作者:Hotha,Kishore Kumar; Patel,Tejashkumar; Roychowdhury,Swapan; Subramanian,Veerappan
    参考文献:Journal Of Liquid Chromatography & Related Technologies 日期:2015 卷标:38(9) 页码:977-985
📜3-<<<2-(S-Methylisithioureido)-4-Thiazolyl>Methyl>Thio>Propionitrile Hydroiodide置于盐酸,氨,水,氯化铵体系中,用 甲醇,乙醇,N,N-二甲基甲酰胺 作为反应溶剂,化学反应 83.0H,反应生成 3-[[[2-[(氨基亚胺甲基)氨基]-4-噻唑基]甲基]硫基]丙酰胺
参考文献:组胺h2受体拮抗剂.1. N-氰基和n-氨基甲酰基am衍生物的合成及其生物学活性.
标题:组胺h2受体拮抗剂.1. N-氰基和n-氨基甲酰基am衍生物的合成及其生物学活性.
摘要:制备了大量的n-氰基am衍生物作为潜在的组胺h2受体拮抗剂,并评估了它们对组胺刺激豚鼠离体右心房变时反应的抑制作用.评价了几种选择的化合物作为组胺在麻醉狗中诱导的胃酸分泌的抑制剂.这些化合物中,呋喃(8C)和[(二氨基亚甲基)氨基]噻唑衍生物(16C)在两种测定中均比西咪替丁更有效.与胍系列相反,在氰基am的末端氮上的甲基取代对活性是有害的.此外,氰基am的酸水解得到氨基甲酰基am,其被证明比氰基am具有更高的活性,与胍的情况相反.
DOI:10.1021/jm00373A007

海关参考信息

专利信息


专利号:US-2016376245-A1
优先权日:2015-06-23
标题 :Impurity of famotidine
发明人:HOTHA KISHORE KUMAR
权利人:GAVIS PHARMACEUTICALS
摘要:The present invention is directed to a new impurity of famotidine, process for preparing and isolating it. The invention is further related to analytical methods of its identification, synthesis and characterization.

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主要参考文献


1: Lin SY. An overview of famotidine polymorphs: solid-state characteristics, thermodynamics, polymorphic transformation and quality control. Pharm Res. 2014 Jul;31(7):1619-31. doi: 10.1007/s11095-014-1323-5. Epub 2014 Mar 1. Review. doi: 10.1007/s40261-013-0113-x. Review. 6 mg) gastrointestinal protection in the treatment of the signs and symptoms of rheumatoid arthritis and osteoarthritis. Expert Rev Gastroenterol Hepatol. 2012 Feb;6(1):25-35. doi: 10.1586/egh.11.88. Review.

合成参考文献


参考文献:10.1021/jm00373a007
摘要:Yanagisawa I, Hirata Y, Ishii Y. Histamine H2 receptor antagonists. 1. Synthesis of N-cyano and N-carbamoyl amidine derivatives and their biological activities. J Med Chem. 1984 Jul;27(7):849–57. doi: 10.1021/jm00373a007.
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