CAS: 763105-70-0; 2,2,2-Trifluoro-N'-(1,2,3,6-Tetrahydropyrazin-5-yl)Acetohydrazide

该化合物是一种化学化合物,其独特的结构特征是三氟乙酸碱和与管子环相连的氢氮功能组,该化合物通常具有与氢氮化物和氟化碳箱酸有关的特性,例如三氟丙基酸组的存在导致酸性增加,三氟甲基组有助于其亲脂性,能够加强生物活动,使其对药物研究感兴趣.管状子环可能带来更多的药理特性,包括与生物目标的潜在相互作用.该化合物可能由于存在碳酸组而溶解于极地溶剂,而氟化部分可能会影响其再活性和稳定性.总体而言,2,22-2-三氟酸(2Z)-2-(2-丙基基)氢氮酸是一种多用途结构,可能被用于医药化学和材料科学.

结构式图片

物理性质

MSDS等安全信息

    上下游产品

    2-trifluoromethyl-1,3,4-oxadiazol-5-ylmethyl chloride ethylenediamine ethyl trifluoroacetate,3-(trifluoromethyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazine hydr°Chloride sitagliptin phosphate (Z)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]pyrazin-7(8H)-yl)-4-(2,4,5-trifluorophenyl)but-2-en-1-one sitagliptin

    合成工艺路线路线简述

      📜三氟乙酸乙酯,N-Methylpiperazin-2-Imine 以 乙腈 作为反应溶剂,以96%的收率获得产物n-[(2Z)-哌嗪-2-亚基]-2,2,2-三氟乙酰肼
      参考文献:一种西他列汀中间体的制备方法
      标题:一种西他列汀中间体的制备方法
      摘要:本发明涉及一种西他列汀中间体的制备方法,属于药物中间体合成技术领域.为了解决现有的产物收率低和环保性差的问题,提供一种西他列汀中间体的合成方法,该方法包括在醇溶剂中将2‑哌嗪酮与水合肼进行反应反应生成哌嗪腙;在乙腈或醚类溶剂中,将哌嗪腙与三氟乙酸乙酯进行反应得到相应的中间体n‑[(2Z)‑哌嗪‑2‑亚基]三氟乙酰肼;在醇溶剂中,在盐酸的作用下使n‑[(2Z)‑哌嗪‑2‑亚基]三氟乙酰肼进行成环成盐反应,得到相应的西他列汀中间体3‑三氟甲基‑5,6,7,8‑四氢‑1,2,4‑三唑[4,3‑a]吡嗪盐酸盐,本发明能够使反应具有高选择性和产物收率高的效果.

      海关参考信息

      专利信息


      专利号:US-7468459-B2
      优先权日:2003-03-19
      标题:Process for the preparation of chiral beta amino acid derivatives by asymmetric hydrogenation
      发明人：XIAO YI; ARMSTRONG III JOSEPH D; KRSKA SHANE W; NJOLITO EUGENIA; RIVERA NELO R; SUN YONGKUI; ROSNER THORSTEN
      权利人:MERCK & CO INC
      摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives which are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of a prochiral beta amino acrylic acid derivative substrate in the presence of a transition metal precursor complexed with a chiral ferrocenyl diphosphine ligand.

      专利号:US-7495123-B2
      优先权日:2004-04-05
      标 题:Process for the preparation of enantiomerically enriched beta amino acid derivatives
      发明人：XIAO YI; SUN YONGKUI; ROSNER THORSTEN; RIVERA NELO R; KRSKA SHANE W; CLAUSEN ANDREW M; ARMSTRONG III JOSEPH D; SPINDLER FELIX; MALAN CHRISTOPHE
      权利人:SOLVIAS AG; MERCK & CO INC
      摘要:The present invention relates to a process for the efficient preparation of enantiomerically enriched beta amino acid derivatives wherein the amino group is unprotected. The product chiral beta amino acid derivatives are useful in the asymmetric synthesis of biologically active molecules. The process comprises an enantioselective hydrogenation of an amine-unprotected prochiral beta-amino acrylic acid or derivative thereof in the presence of a rhodium metal precursor complexed with a chiral mono- or bisphosphine ligand.

      专利号:WO-2004083212-A1
      优先权日:2003-03-18
      标 题:Process to beta-ketoamide intermediates to dipeptidyl peptidase inhibitors
      发明人：IKEMOTO NORIHIRO; SIMMONS BRYON L; WILLIAMS J MICHAEL; XU FENG; YANG CHUNHUA
      权利人:MERCK & CO INC; IKEMOTO NORIHIRO; SIMMONS BRYON L; WILLIAMS J MICHAEL; XU FENG; YANG CHUNHUA
      摘要:A novel process is provided for the preparation of beta-ketoamide intermediates which are useful in the synthesis of dipeptidyl peptidase-IV inhibitors for the treatment of type 2 diabetes. Also provided are useful intermediates obtained from the process.

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      合成参考文献


      摘要:Ye, Z.-S., Science of Synthesis Knowledge Updates, (2021) 2, 364.
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