2,6-二甲基-D-苯丙氨酸 | 128502-64-7

• 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: 2,6-二甲基-D-苯丙氨酸
• 英文名称: D-2',6'-dimethylphenylalanine
• 英文别名: (2R)-2-azaniumyl-3-(2,6-dimethylphenyl)propanoate
• CAS: 128502-64-7
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: VEQOZHOWFAVBOO-SNVBAGLBSA-N

物化性质

• 沸点：
  343.3±30.0 °C(Predicted)
• 密度：
  1.136±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.7
• 重原子数：
  14
• 可旋转键数：
  3
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  63.3
• 氢给体数：
  2
• 氢受体数：
  3

安全信息

• 海关编码：
  2922499990

反应信息

• 作为反应物：
  描述：

  9-芴甲基-N-琥珀酰亚胺基碳酸酯 、 2,6-二甲基-D-苯丙氨酸 在 sodium carbonate 作用下， 以 乙腈 为溶剂， 生成 Fmoc-D-2',6'-dimethylphenylalanine
  参考文献：
  名称：

  Enkephalin analogues with 2′,6′-dimethylphenylalanine replacing phenylalanine in position 4

  摘要：

  Four Leu-enkephalin (Enk) analogues containing 2'.6'-dimethyphenylalanine (Dmp) in position 4 were prepared and tested for their receptor binding and biological activities. Among the analogues prepared, [2', 6'-dimethvltyrosine(1), D-Dmp(4)]Enk was found to be an antagonist toward mu and delta opioid receptors with pA(2) values of 6.90 and 5.57, respectively. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00665-x
• 作为产物：
  描述：

  1,3-二甲基-2-碘苯 在 palladium on activated charcoal 盐酸 、 palladium diacetate 、 sodium hydroxide 、 氢气 、 1-羟基苯并三唑 、 三乙胺 、 N,N'-二环己基碳二亚胺 、 三(邻甲基苯基)磷 作用下， 以 1,4-二氧六环 、 乙酸乙酯 、 N,N-二甲基甲酰胺 、 乙腈 为溶剂， 70.0 ℃ 、405.3 kPa 条件下， 反应 45.0h， 生成 2,6-二甲基-D-苯丙氨酸
  参考文献：
  名称：

  Enkephalin analogues with 2′,6′-dimethylphenylalanine replacing phenylalanine in position 4

  摘要：

  Four Leu-enkephalin (Enk) analogues containing 2'.6'-dimethyphenylalanine (Dmp) in position 4 were prepared and tested for their receptor binding and biological activities. Among the analogues prepared, [2', 6'-dimethvltyrosine(1), D-Dmp(4)]Enk was found to be an antagonist toward mu and delta opioid receptors with pA(2) values of 6.90 and 5.57, respectively. (C) 2001 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(00)00665-x

文献信息

• Angiotensin-1-Receptor Antagonists
  申请人：Ferring B.V.

  公开号：US20170349629A1

  公开（公告）日：2017-12-07

  In one aspect, this disclosure features compounds of formula (I) or a pharmaceutically acceptable salt thereof: AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH   (I), in which AA1, AA4, AA5, and AA8 are defined in the specification. The compounds of formula (I) can be used to treat hypertension (e.g., hypertension induced by pregnancy), preeclampsia, or a renal disease induced by pregnancy.

  在一个方面，这个披露涉及到式(I)的化合物或其药用盐： AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH (I)， 其中AA1，AA4，AA5和AA8在规范中有定义。式(I)的化合物可用于治疗高血压（例如，妊娠引起的高血压），子痫前期，或妊娠引起的肾脏疾病。
• Angiotensin-1-receptor antagonists
  申请人：Ferring B.V.

  公开号：US10344054B2

  公开（公告）日：2019-07-09

  Compounds of formula (I) and pharmaceutically acceptable salts thereof are described: AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH  (I), in which AA1, AA4, AA5, and AA8 are defined in the specification. The compounds of formula (I) can be used to treat hypertension (e.g., hypertension induced by pregnancy), preeclampsia, or a renal disease induced by pregnancy.

  描述了式 (I) 化合物及其药学上可接受的盐类： AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH (I)、 其中 AA1、AA4、AA5 和 AA8 的定义见说明书。式（I）化合物可用于治疗高血压（如妊娠诱发的高血压）、子痫前期或妊娠诱发的肾脏疾病。
• ANGIOTENSIN-1-RECEPTOR ANTAGONISTS
  申请人：Ferring B.V.

  公开号：EP3464324A1

  公开（公告）日：2019-04-10
• [EN] ANGIOTENSIN-1-RECEPTOR ANTAGONISTS<br/>[FR] ANTAGONISTES DU RÉCEPTEUR DE L'ANGIOTENSINE 1
  申请人：FERRING BV

  公开号：WO2017207760A1

  公开（公告）日：2017-12-07

  In one aspect, this disclosure features compounds of formula (I)or a pharmaceutically acceptable salt thereof: AA1-Arg-Val-AA4-AA5-His-Pro-AA8-OH(I), in which AA1, AA4, AA5, and AA8 are defined in the specification. The compounds of formula (I) can be used to treat hypertension(e.g., hypertension induced by pregnancy), preeclampsia,or a renal disease induced bypregnancy.
• Enkephalin analogues with 2′,6′-dimethylphenylalanine replacing phenylalanine in position 4
  作者：Yusuke Sasaki、Mariko Hirabuki、Akihiro Ambo、Hidekazu Ouchi、Yutaka Yamamoto

  DOI：10.1016/s0960-894x(00)00665-x

  日期：2001.2

  Four Leu-enkephalin (Enk) analogues containing 2'.6'-dimethyphenylalanine (Dmp) in position 4 were prepared and tested for their receptor binding and biological activities. Among the analogues prepared, [2', 6'-dimethvltyrosine(1), D-Dmp(4)]Enk was found to be an antagonist toward mu and delta opioid receptors with pA(2) values of 6.90 and 5.57, respectively. (C) 2001 Elsevier Science Ltd. All rights reserved.