5-(4-(bromomethyl)-[1,1'-biphenyl]-2-yl]-1-(triphenylmethyl)-1H-tetrazole | 159532-62-4

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 英文名称: 5-(4-(bromomethyl)-[1,1'-biphenyl]-2-yl]-1-(triphenylmethyl)-1H-tetrazole
• 英文别名: N-triphenylmethyl-5-[4-(bromomethyl)-biphenyl-2-yl]tetrazole；4,-bromomethyl-2-(N-triphenylmethyltetrazol-5-yl)biphenyl；5-(4-(bromomethyl)-biphenyl-2-yl)-1-(triphenylmethyl)tetrazole；5-(4-(Bromomethyl)-[1,1'-biphenyl]-2-yl)-1-trityl-1H-tetrazole；5-[5-(bromomethyl)-2-phenylphenyl]-1-trityltetrazole
• CAS: 159532-62-4
• 化学式: C₃₃H₂₅BrN₄
• 分子量: 557.492
• InChiKey: BIMWFHVLFZYVIE-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  8.2
• 重原子数：
  38
• 可旋转键数：
  7
• 环数：
  6.0
• sp3杂化的碳原子比例：
  0.06
• 拓扑面积：
  43.6
• 氢给体数：
  0
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  5-(4-(bromomethyl)-[1,1'-biphenyl]-2-yl]-1-(triphenylmethyl)-1H-tetrazole 、 2-丁基-1,3-二氮杂螺环-[4,4]壬-1-烯-4酮 在 氢氧化钾 、 四丁基溴化铵 作用下， 以 乙腈 为溶剂， 反应 2.5h， 生成 三苯甲基厄贝沙坦
  参考文献：
  名称：

  WO2006/73376

  摘要：

  公开号：

文献信息

• A process for the synthesis of valsartan
  申请人：KRKA, D.D., Novo Mesto

  公开号：EP1661891A1

  公开（公告）日：2006-05-31

  This invention relates to an improved process for preparing a valsartan, or a pharmaceutically acceptable salt thereof, or pharmaceutical preparation containing either entity wherein a compound of formula (II) or a salt thereof, is reacted with valine or an ester or a salt thereof in a solvent selected from the group consisting of methylene chloride, chloroform, butyl chloride, isopropyl acetate and tert-butyl methyl ether to form a compound of formula (IV) which is then acylated to form a compound of formula (VI) wherein R is hydrogen, alkyl, alkenyl or benzyl; which is then deprotected to give valsartan, and may be converted to a pharmaceutically acceptable salt and/or a pharmaceutical formulation. The invention also covers intermediates of formula (IV) and (VI) wherein R=H.

  这项发明涉及一种改进的制备缬沙坦、其药用可接受盐或含有任一实体的制药制剂的过程，其中式（II）的化合物或其盐在甲烷氯化物、氯仿、丁基氯化物、丙酸异丙酯和叔丁基甲基醚等溶剂中与缬氨酸或其酯或盐反应，形成式（IV）的化合物，然后酰化形成式（VI）的化合物，其中R为氢、烷基、烯基或苄基；然后去保护得到缬沙坦，并可转化为药用可接受的盐和/或制药配方。该发明还涵盖了中间体式（IV）和（VI），其中R=H。
• [EN] A NEW PROCESS FOR THE PREPARATION OF OLMESARTAN MEDOXOMIL<br/>[FR] NOUVEAU PROCÉDÉ DE PRÉPARATION D'OLMÉSARTAN MÉDOXOMIL
  申请人：INOGENT LAB PRIVATE LTD

  公开号：WO2011036674A1

  公开（公告）日：2011-03-31

  This invention provides a new process for producing (5-methyl-2-oxo-1,3- dioxolen-4-yl)methyl-4-(1-hydroxy-1-methylethyl)-2-propyl-1-[4-[2-(tetrazol-5- yl)phenyl] phenyl] methylimidaozle-5-carboxylate (olmesartan medoxomil) from alkaline salts of trityl olmesartan more preferably calcium salts of trityl olmesartan.

  本发明提供了一种从三苯甲酸奥美沙坦的碱性盐，更优选为三苯甲酸奥美沙坦的钙盐，生产(5-甲基-2-氧代-1,3-二氧杂环戊-4-基)甲基-4-(1-羟基-1-甲基乙基)-2-丙基-1-[4-[2-(四唑-5-基)苯基]苯基]甲基咪唑-5-羧酸酯(奥美沙坦酯)的新工艺。
• 4-pyrimidinone derivatives their preparation and their application in
  申请人：Synthelabo

  公开号：US05472967A1

  公开（公告）日：1995-12-05

  Compounds which can be expressed as tautomeric forms and having the formulas (I), (I') and (I") ##STR1## wherein R.sub.1 =a straight or branched (C.sub.1-7) alkyl group or a straight or branched (C.sub.3-9) alkenyl group or a cyclo(C.sub.3-7)alkyl(C.sub.1-6) alkyl group, R.sub.2 =an atom of hydrogen, or a straight or branched (C.sub.1-7)alkyl group, or a cyclo(C.sub.3-7)alkyl(C.sub.1-3)alkyl group, or an aryl(C.sub.1-3)alkyl group optionally substituted on the ring, or an aryloxy(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylthio(C.sub.1-3)alkyl group optionally substituted on the ring, or an arylsulfonyl(C.sub.1-3)alkyl group optionally substituted on the ring, or a heteroaryl(C.sub.1-3)alkyl group optionally substituted on the ring, R.sub.3 =CO.sub.2 H, 1H-tetrazol-5-yl, NHCOR.sub.11, NHSO.sub.2 R.sub.11, CONHSO.sub.2 R.sub.11 or CONHOR.sub.12 group where R.sub.11 =a methyl, trifluoromethyl, or phenyl group optionally substituted, R.sub.12 =a hydrogen atom, or a methyl or a phenyl group optionally substituted. The compounds are useful for antagonizing angiotensin II.

  可以表达为互变异构体的化合物，其化学式为(I)、(I')和(I")##STR1## 其中，R.sub.1 = 直链或支链(C.sub.1-7)烷基或直链或支链(C.sub.3-9)烯基或环(C.sub.3-7)烷基(C.sub.1-6)烷基，R.sub.2 = 氢原子或直链或支链(C.sub.1-7)烷基或环(C.sub.3-7)烷基(C.sub.1-3)烷基或取代环上的苯基(C.sub.1-3)烷基或取代环上的苯氧基(C.sub.1-3)烷基或取代环上的苯硫基(C.sub.1-3)烷基或取代环上的苯磺酰基(C.sub.1-3)烷基或取代环上的杂环基(C.sub.1-3)烷基，R.sub.3 = CO.sub.2 H、1H-四唑-5-基、NHCOR.sub.11、NHSO.sub.2 R.sub.11、CONHSO.sub.2 R.sub.11或CONHOR.sub.12基，其中R.sub.11 = 可选取代的甲基、三氟甲基或苯基，R.sub.12 = 氢原子或可选取代的甲基或苯基。这些化合物可用于拮抗血管紧张素II。
• Process for Preparing Valsartan
  申请人：Kankan Rajendra Narayanrao

  公开号：US20110105763A1

  公开（公告）日：2011-05-05

  An N-[(2′-(1-triphenyl methyl tetrazole-5-yl)biphenyl]-4-yl]methyl]-L-valine benzyl ester organic salt of formula (IVA) wherein A represents an organic carboxylic acid, a process for its preparation and its use in the synthesis of valsartan or salts thereof.

  一种化学式为(IVA)的有机盐，其化合物为N-[(2′-(1-三苯甲基四唑-5-基)联苯)-4-基]甲基]-L-缬氨酸苄酯，其中A代表有机羧酸，本发明还提供了其制备方法以及在缬沙坦或其盐的合成中的应用。
• PROCESS FOR THE PREPARATION OF 4-BROMOMETHYL-[1,1'-BIPHENYL]-2'-CARBONITRILE
  申请人：SANOFI

  公开号：EP2513046B1

  公开（公告）日：2015-07-08