苯甲基N-[(2(三苯代甲基四唑-5-基-1,1联苯基-4-基]-甲基-2-氨基-3-甲基丁酸酯 | 137864-45-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 三苯基化合物
• 中文名称: 苯甲基N-[(2(三苯代甲基四唑-5-基-1,1联苯基-4-基]-甲基-2-氨基-3-甲基丁酸酯
• 中文别名: 苄基N-{[2'-(1-三苯甲基-1H-四唑-5-基)-4-联苯基]甲基}-L-缬氨酸酯
• 英文名称: Benzyl N-[(2'-(Trityltetrazol-5-yl-1,1'-biphenyl-4-yl]-methyl-2-amino-3-methylbutanoate
• 英文别名: benzyl 3-methyl-2-[[4-[2-(1-trityltetrazol-5-yl)phenyl]phenyl]methylamino]butanoate
• CAS: 137864-45-0
• 化学式: C₄₅H₄₁N₅O₂
• 分子量: 683.8
• InChiKey: MGBJPNDAJWSIAT-UHFFFAOYSA-N

物化性质

• 沸点：
  825.6±75.0 °C(Predicted)
• 密度：
  1.15±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  9.8
• 重原子数：
  52
• 可旋转键数：
  14
• 环数：
  7.0
• sp3杂化的碳原子比例：
  0.16
• 拓扑面积：
  81.9
• 氢给体数：
  1
• 氢受体数：
  6

文献信息

• Process For the Preparation of Angiotensin II Antagonist
  申请人：Budidet Sankar Reddy

  公开号：US20090281326A1

  公开（公告）日：2009-11-12

  The present invention provides a method for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetra-zol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine (Valsartan) which comprises; treating N-[[2′-(1-triphenylmethyl-tetra-zol-5-yl)biphenyl-4-yl]methyl]-L-valine methyl ester (X) with oxalic acid or its hydrates in a solvent to produce N-[[2′-(1-triph-enylmethyl-tetrazol-5-yl)biphenyl-4-yl]methy]-L-valine methyl ester oxalate (Xa) and treating the compound (Xa) with a base in a solvent followed by reacting with valeryl chloride in presence of base in a solvent to produce N-[[2′-(1-triphenylmethyl-tetra-=zol-5-yl)[1,1′biphenyl]-4-yl]methyl]-N-valeryl-L-valine methyl ester (XI), de-protecting the compound (XI) using anhydrous acidic conditions to produce N-(1-oxopentyl)-N-[[2′-(1-H-tetrazol-5-yl)[1,1′biphenyl]-4-yl]methyl-L-valine methyl ester (V) followed by

  本发明提供了一种制备缬沙坦（Valsartan）的方法，包括以下步骤：将N-[[2'-(1-三苯甲基-四唑-5-基)[1,1'-联苯]-4-基]甲基]-L-缬氨酸甲酯（X）与草酸或其水合物在溶剂中反应，生成N-[[2'-(1-三苯甲基-四唑-5-基)联苯-4-基]甲基]-L-缬氨酸甲酯草酸酯（Xa），然后将化合物（Xa）与溶剂中的碱反应，随后在溶剂中的碱存在下与戊酰氯反应，生成N-[[2'-(1-三苯甲基-四唑-5-基)[1,1'联苯]-4-基]甲基]-N-戊酰-L-缬氨酸甲酯（XI），用无水酸性条件去保护化合物（XI），生成N-(1-氧代戊基)-N-[[2'-(1-H-四唑-5-基)[1,1'联苯]-4-基]甲基]-L-缬氨酸甲酯（V），最后在溶剂中用碱处理，生成缬沙坦。
• PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS AND INTERMEDIATES THEREOF
  申请人：ALKEM LABORATORIES LTD.

  公开号：US20140316142A1

  公开（公告）日：2014-10-23

  The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(1-oxopentyl)-N-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-L-valine of Formula 1 via a phosphite salt of Formula-4.H 3 PO 3 preferably a phosphite salt of Formula-4′.H 3 PO 3

  本发明涉及一种改进的制备肾素受体拮抗剂及其中间体的方法。特别是本发明涉及一种改进的制备Formula 1中N-(1-oxopentyl)-N-[[2′-(1H-噻唑-5-基)[1,1′-联苯]-4-基]甲基]-L-缬氨酸的方法，通过Formula-4.H3PO3的亚磷酸盐，最好是Formula-4′.H3PO3的亚磷酸盐。
• [EN] AN IMPROVED PROCESS FOR THE PREPARATION OF ANGIOTENSIN II ANTAGONISTS AND INTERMEDIATES THEREOF.<br/>[FR] PROCÉDÉ AMÉLIORÉ DE PRÉPARATION D'ANTAGONISTES DE L'ANGIOTENSINE II ET D'INTERMÉDIAIRES DE SYNTHÈSE DE CEUX-CI
  申请人：ALKEM LAB LTD

  公开号：WO2013072924A1

  公开（公告）日：2013-05-23

  The present invention relates to an improved process for the preparation of angiotensin receptor antagonists and intermediates thereof. Particularly the present invention relates to an improved process for the preparation of N-(l-oxopentyl)-N-[[2'-(lH-tetrazoI-5-yl) [1, 1 '-biphenyl]-4-yl] methyl]-L- valine of Formula (1) Formula-1 Formula-4.H3P03 via a phosphite salt of Formula-4.H3P03 preferably a phosphite salt of Formula-4'.H3P03 Ph3C N-[2'-1 -triphenylmethyl-tetra zol-5-yl)biphenyl-4-yl)methyl ]-(L)-Valine Benzyl ester H3P03 salt Formula-4'.H3P03 salt.

  本发明涉及一种改进的制备肾素受体拮抗剂及其中间体的方法。特别是本发明涉及一种改进的制备N-(l-氧代戊基)-N-[[2'-(1H-四氮唑-5-基)[1,1'-联苯]-4-基] 甲基]-L-缬氨酸的方法，其化学式为（1）Formula-1 Formula-4.H3P03，通过一种磷酸酯盐，优选为一种Formula-4.H3P03的磷酸酯盐，Ph3C N-[2'-1-三苯甲基-四氮唑-5-基)联苯-4-基)甲基]-(L)-缬氨酸苄酯H3P03盐Formula-4'.H3P03盐。
• US7880015B2
  申请人：——

  公开号：US7880015B2

  公开（公告）日：2011-02-01