3-(4-联苯基)-2-({[(2-甲基-2-丙基)氧基]羰基}氨基)丙酸 | 119273-61-9

• 分子结构分类: 有机化合物 - 有机酸及其衍生物 - 羧酸及其衍生物
• 中文名称: 3-(4-联苯基)-2-({[(2-甲基-2-丙基)氧基]羰基}氨基)丙酸
• 中文别名: 2-(BOC-氨基)-3-(联苯-4-基)丙酸
• 英文名称: rac-2-{[(tert-butyloxy)carbonyl]amino}-3-(biphenyl-4-yl)propionic acid
• 英文别名: 3-(1,1'-Biphenyl-4-yl)-2-tert-butoxycarbonylaminopropionic acid；N-t-butoxycarbonyl-4-biphenylalanine；2-[(2-methylpropan-2-yl)oxycarbonylamino]-3-(4-phenylphenyl)propanoic Acid
• CAS: 119273-61-9
• 化学式: C₂₀H₂₃NO₄
• mdl: MFCD03425235
• 分子量: 341.407
• InChiKey: NBVVKAUSAGHTSU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.4
• 重原子数：
  25
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.3
• 拓扑面积：
  75.6
• 氢给体数：
  2
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  3-(4-联苯基)-2-({[(2-甲基-2-丙基)氧基]羰基}氨基)丙酸 在 (benzotriazo-1-yloxy)tris(dimethylamino)phosphonium hexafluorophosphate 、 N,N-二异丙基乙胺 、 三氟乙酸 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 0.5h， 生成 2-amino-3-(4-phenylphenyl)-N-(2,2,6,6-tetramethylpiperidin-4-yl)propanamide
  参考文献：
  名称：

  EP4137480

  摘要：

  公开号：
• 作为产物：
  描述：

  对溴苯丙氨酸 在 potassium phosphate 、 bis(η3-allyl-μ-chloropalladium(II)) 、 triethylammonium 2-(dicyclohexylphosphino)-4'-{[(sulfonatomethyl)amino]carbonyl}biphenyl 、 sodium hydroxide 作用下， 以 四氢呋喃 、 二氯甲烷 、 水 为溶剂， 反应 4.0h， 生成 3-(4-联苯基)-2-({[(2-甲基-2-丙基)氧基]羰基}氨基)丙酸
  参考文献：
  名称：

  Synthesis of an amidosulfonate-tagged biphenyl phosphine and its application in the Suzuki–Miyaura reaction affording biphenyl-substituted amino acids in water

  摘要：

  An amidosulfonate-tagged phosphinobiphenyl, viz triethylammonium 2-(dicyclohexylphosphino)-4'-{[(sulfonatomethyl)amino]carbonyl}biphenyl(3), was prepared in two steps from 2-(dicyclohexylphosphino) biphenyl-4'-carboxylic acid and fully characterized including the crystal structure determination. As a highly polar phosphine ligand, compound 3 was employed in the Pd-catalyzed Suzuki-Miyaura cross-coupling of N-Boc protected 4-bromo and 4-chlorophenylalanine with aromatic boronic acids to afford the corresponding biphenyls in aqueous N,N-dimethylformamide or pure water. The coupling was demonstrated to proceed very well and without the loss of the Boc protecting group when the bromo-substituted substrate is reacted in the presence of 1 mol.% of Pd/3 catalyst in water at 40 degrees C. Reactions with boronic acids bearing electron-withdrawing substituents and, mainly, those with the less reactive chlorophenylalanine substrate required slightly higher reaction temperature and more catalyst to achieve similar results. (C) 2015 Elsevier B.V. All rights reserved.

  DOI：

  10.1016/j.jorganchem.2015.01.020

文献信息

• NEPRILYSIN INHIBITORS
  申请人：Fleury Melissa

  公开号：US20150210690A1

  公开（公告）日：2015-07-30

  In one aspect, the invention relates to compounds having the formula I: where R 1 -R 6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising these compounds; methods of using these compounds; and processes and intermediates for preparing these compounds.

  在一个方面，该发明涉及具有以下式I的化合物： 其中R1-R6如规范中定义，或其药学上可接受的盐。这些化合物具有神经肽酶抑制活性。在另一个方面，该发明涉及包含这些化合物的药物组合物；使用这些化合物的方法；以及制备这些化合物的过程和中间体。
• NITRIC OXIDE DONOR NEPRILYSIN INHIBITORS
  申请人：Mammen Mathai

  公开号：US20130323271A1

  公开（公告）日：2013-12-05

  In one aspect, the invention relates to compounds having the formula: where R 1 , R 2 , R 3 , R 7 , R 8 , Z, X, b, and c are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds are nitric oxide donors and have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and processes and intermediates for preparing such compounds.

  在一方面，本发明涉及具有以下公式的化合物：其中R1、R2、R3、R7、R8、Z、X、b和c按说明书定义，或其药用可接受的盐。这些化合物是氧化氮供体并具有中性内肽酶抑制活性。在另一方面，本发明涉及包含此类化合物的药物组合物；使用此类化合物的方法；以及制备此类化合物的过程和中间体。
• SUBSTITUTED CARBAMOYLCYCLOALKYL ACETIC ACID DERIVATIVES AS NEP
  申请人：KARKI Rajeshri Ganesh

  公开号：US20120122764A1

  公开（公告）日：2012-05-17

  The present invention provides a compound of formula I; or a pharmaceutically acceptable salt thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , B, X, m and n are defined herein. The invention also relates to a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides pharmaceutical composition of compounds of the invention, and a combination of pharmacologically active agents and a compound of the invention.

  本发明提供了一种具有化学式I的化合物； 或其药学上可接受的盐，其中R 1 ，R 2 ，R 3 ，R 4 ，R 5 ，B，X，m和n在此处被定义。该发明还涉及制造该发明化合物的方法及其治疗用途。本发明进一步提供了该发明化合物的药物组合物，以及具有药理活性剂和该发明化合物的组合。
• Compounds with growth hormone releasing properties
  申请人：Novo Nordisk A/S

  公开号：US05977178A1

  公开（公告）日：1999-11-02

  Compounds of peptide mimetic nature having the general formula I ##STR1## wherein a and b are independently 1 or 2, R.sup.1 and R.sup.2 are independently H or C.sub.1-6 alkyl, G and J are independently, inter alia, aromats, and D and E are independently several different groups are growth hormone secretagogous with improved bioavailability.

  具有一般式I的肽类模拟化合物##STR1##，其中a和b独立地为1或2，R.sup.1和R.sup.2独立地为H或C.sub.1-6烷基，G和J独立地为芳香族等，D和E独立地为几种不同的基团，具有改善生物利用度的生长激素分泌素。
• Certain thiol inhibitors of endothelin-converting enzyme
  申请人：——

  公开号：US20020082218A1

  公开（公告）日：2002-06-27

  Disclosed as endothelin converting enzyme inhibitors are the compounds of the formula 1 wherein the variables have the meanings as defined hereinbefore.

  披露的内皮素转化酶抑制剂是具有以下公式的化合物，其中变量的含义如前文所定义。