D-2-氨基-5-苯基戊酸 | 36061-08-2

• 物质功能分类: 生物化工 - 氨基酸及其衍生物 - 其他氨基酸衍生物
• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 中文名称: D-2-氨基-5-苯基戊酸
• 中文别名: 2-氨基-5-苯基戊酸
• 英文名称: (2R)-2-amino-5-phenylpentanoic acid
• 英文别名: (R)-2-amino-5-phenylvaleric acid；D-2-amino-5-phenylpentanoic acid；(2R)-2-amino-5-phenyl-pentanoic acid；2-(R)-Amino-5-phenyl-pentanoic acid；(D)-2-amino-5-phenylpentanoic acid；(D)-N-amino-5-phenylpentanoic acid；(R)-2-Amino-5-phenylpentanoic acid
• CAS: 36061-08-2
• 化学式: C₁₁H₁₅NO₂
• 分子量: 193.246
• InChiKey: XOQZTHUXZWQXOK-SNVBAGLBSA-N

物化性质

• 沸点：
  375.2±42.0 °C(Predicted)
• 密度：
  1.133±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.3
• 重原子数：
  14
• 可旋转键数：
  4
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.36
• 拓扑面积：
  67.8
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2922499990
• 危险性防范说明：
  P280,P305+P351+P338
• 危险性描述：
  H302,H312,H315,H319

反应信息

• 作为反应物：
  描述：

  D-2-氨基-5-苯基戊酸 在 palladium 10% on activated carbon benzotriazol-1-yloxyl-tris-(pyrrolidino)-phosphonium hexafluorophosphate 、 氢气 、 N,N-二异丙基乙胺 、 sodium hydroxide 作用下， 以 1,4-二氧六环 、 水 、 溶剂黄146 、 N,N-二甲基甲酰胺 为溶剂， 反应 1.0h， 生成 Bzls-DPpg-hAla(4-Pip)-4-Amba x 2TFA
  参考文献：
  名称：

  [EN] TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE
  [FR] INHIBITEURS DE SÉRINE PROTÉASE DE TYPE TRYPSINE, ET LEUR PRÉPARATION ET UTILISATION

  摘要：

  公开号：

  WO2011094496A3
• 作为产物：
  描述：

  (+/-)-2-Acetamino-5-phenyl-valeriansaeure 在 N-acyl-D-amino acid amidohydrolase 、 zinc(II) chloride 盐酸 、 氢氧化钾 、 水 作用下， 反应 12.0h， 以47.29%的产率得到D-2-氨基-5-苯基戊酸
  参考文献：
  名称：

  [EN] STEREOSELECTIVE PROCESS FOR THE SYNTHESIS OF (D)-2-AMINO-5-PHENYLPENTANOIC OR ALKYL ESTER THEREOF
  [FR] PROCESSUS STEREOSELECTIF POUR LA SYNTHESE DE (D)-2-AMINO-5-PHENYLPENTANOIQUE OU DE L'ESTER ALKYLIQUE DE CELUI-CI

  摘要：

  本发明提供了一种制备式(I)化合物的方法；其中R是C1-C6烷基；或其盐；包括：(c)在D-氨基酰化酶存在下，用适当的碱水解(D,L)-N-乙酰-2-氨基-5-苯基戊酸，得到(D)-2-氨基-5-苯基戊酸；和(d)用烷醇酯化(D)-2-氨基-5-苯基戊酸。在另一实施例中，本发明提供了一种选择性制备(D)-2-氨基-5-苯基戊酸的方法，包括在D-氨基酰化酶存在下，用适当的碱水解(D,L)-N-乙酰-2-氨基-5-苯基戊酸。在另一实施例中，本发明提供了一种改进的制备式(II)生长激素促分泌剂化合物的方法。

  公开号：

  WO2003087036A1

文献信息

• [EN] OXABOROLE ESTERS AND USES THEREOF<br/>[FR] ESTERS D'OXABOROLE ET LEURS UTILISATIONS
  申请人：ANACOR PHARMACEUTICALS INC

  公开号：WO2017195069A1

  公开（公告）日：2017-11-16

  The present invention provides oxaborole ester compounds and compositions thereof which are useful to treat diseases associated with parasites, such as Chagas Disease and African Animal Trypanosomosis.

  本发明提供了氧硼酯酯化合物及其组合物，可用于治疗与寄生虫相关的疾病，如充血性心脏病和非洲动物锥虫病。
• Spiro piperidines and homologs promote release of growth hormone
  申请人：Merck & Co., Inc.

  公开号：US05578593A1

  公开（公告）日：1996-11-26

  There are disclosed certain novel compounds identified as spiro piperidines and homologs which promote the release of growth hormone in humans and animals. This property can be utilized to promote the growth of food animals to render the production of edible meat products more efficient, and in humans, to treat physiological or medical conditions characterized by a deficiency in growth hormone secretion, such as short stature in growth hormone deficient children, and to treat medical conditions which are improved by the anabolic effects of growth hormone. Growth hormone releasing compositions containing such spiro compounds as the active ingredient thereof are also disclosed.

  已披露某些新型化合物，被确定为螺环哌啶和同系物，可以促进人类和动物体内生长激素的释放。这种特性可以用于促进食用动物的生长，使可食用肉制品的生产更加高效，在人类中，可用于治疗生长激素分泌不足所导致的生理或医学状况，如生长激素缺乏儿童的矮小身材，并用于治疗通过生长激素的合成效应得到改善的医学状况。还披露了含有这种螺环化合物作为活性成分的促生长激素组合物。
• Dipeptide derivatives as growth hormone secretagogues
  申请人：Pfizer Inc.

  公开号：US06251902B1

  公开（公告）日：2001-06-26

  This invention is directed to compounds of the formula and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-HT920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

  本发明涉及公式化合物及其药用盐，其中取代基如规范中定义，这些化合物是生长激素分泌素，能增加内源性生长激素水平。本发明的化合物可用于治疗和预防骨质疏松症和/或虚弱、充血性心力衰竭、与衰老有关的虚弱、肥胖；加速骨折修复、减轻重大手术后蛋白质分解反应、减少慢性疾病导致的消瘦和蛋白质丢失、加速伤口愈合，或加速烧伤患者或接受重大手术的患者的康复；改善肌肉力量、运动能力、皮肤厚度的维持、代谢稳态或肾脏稳态。本发明的化合物在与：双膦酸盐类化合物如阿伦膦酸盐；雌激素、前马品、以及可选的孕激素；雌激素拮抗剂或激动剂；或降钙素结合使用时，也可用于治疗骨质疏松症和/或虚弱；及其药用组合物。此外，本发明涉及药用组合物，用于增加人类或其他动物内源性生长激素的产生或释放，包括本发明的化合物和从GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-HT920中选择的生长激素分泌素的有效量。该发明还涉及在制备公式I化合物中有用的中间体。
• TRYPSIN-LIKE SERINE PROTEASE INHIBITORS, AND THEIR PREPARATION AND USE
  申请人：Steinmetzer Torsten

  公开号：US20100022781A1

  公开（公告）日：2010-01-28

  The invention relates to inhibitors of trypsin-like serine proteases of the general formula (I) which, as well as plasmin, also inhibit plasma kallikrien, and to their preparation and use as medicaments, preferably for treatment of blood loss, especially in the case of hyperfibrinolytic states, in organ transplants or heart surgery interventions, in particular with a cardiopulmonary bypass, or as a constituent of a fibrin adhesive.

  该发明涉及一般式（I）的胰蛋白酶样丝氨酸蛋白酶抑制剂，除了抑制纤溶酶外，还抑制血浆激肽原，以及它们的制备和用作药物，优选用于治疗失血，特别是在高纤溶状态、器官移植或心脏手术干预，特别是心肺转流手术中，或作为纤维蛋白粘合剂的组分。
• Dipeptide derivatives
  申请人：——

  公开号：US20010041703A1

  公开（公告）日：2001-11-15

  This invention is directed to compounds of the formula 1 and the pharmaceutically-acceptable salts thereof, where the substituents are as defined in the Specification, which are growth hormone secretogogues and which increase the level of endogenous growth hormone. The compounds of this invention are useful for the treatment and prevention of osteoporosis and/or frailty, congestive heart failure, frailty associated with aging, obesity; accelerating bone fracture repair, attenuating protein catabolic response after a major operation, reducing cachexia and protein loss due to chronic illness, accelerating wound healing, or accelerating the recovery of burn patients or patients having undergone major surgery; improving muscle strength, mobility, maintenance of skin thickness, metabolic homeostasis or renal homeostasis. The compounds of the present invention are also useful in treating osteoporosis and/or frailty when used in combination with: a bisphosphonate compound such as alendronate; estrogen, premarin, and optionally progesterone; an estrogen agonist or antagonist; or calcitonin, and pharmaceutical compositions useful therefor. Further, the present invention is directed to pharmaceutical compositions useful for increasing the endogenous production or release of growth hormone in a human or other animal which comprises an effective amount of a compound of the present invention and a growth hormone secretagogue selected from GHRP-6, Hexarelin, GHRP-1, growth hormone releasing factor (GRF), IGF-1, IGF-2 or B-H-T920. The invention is also directed to intermediates useful in the preparation of compounds of Formula I.

  本发明涉及公式1的化合物及其药学上可接受的盐，其中取代基如规范中所定义，这些化合物是生长激素分泌促进剂，可以增加内源性生长激素的水平。本发明的化合物可用于治疗和预防骨质疏松和/或衰弱、充血性心力衰竭、与衰老有关的衰弱、肥胖症；加速骨折修复、减轻重大手术后的蛋白质分解反应、减少慢性疾病引起的消瘦和蛋白质流失、加速伤口愈合或加速烧伤患者或接受重大手术的患者的恢复；改善肌肉力量、运动能力、皮肤厚度维持、代谢稳态或肾脏稳态。本发明的化合物在与双磷酸盐化合物（如阿伦膦酸）、雌激素、预马林和可选孕激素、雌激素激动剂或拮抗剂或降钙素联合使用时，也可用于治疗骨质疏松和/或衰弱，以及用于该用途的药物组合物。此外，本发明还涉及用于增加人类或其他动物内源性生长激素的产生或释放的药物组合物，该组合物包括本发明化合物的有效量和从GHRP-6、Hexarelin、GHRP-1、生长激素释放因子（GRF）、IGF-1、IGF-2或B-H-T920中选择的生长激素分泌促进剂。本发明还涉及用于制备公式I化合物的中间体。