(S)-2-氨基戊酰胺盐酸盐 | 101925-47-7

• 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: (S)-2-氨基戊酰胺盐酸盐
• 英文名称: L-norvalinamide hydrochloride
• 英文别名: (S)-2-Aminopentanamide hydrochloride；(2S)-2-aminopentanamide;hydrochloride
• CAS: 101925-47-7
• 化学式: C₅H₁₂N₂O*ClH
• mdl: MFCD00237404
• 分子量: 152.624
• InChiKey: BKHOLEXUVFOVRH-WCCKRBBISA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.42
• 重原子数：
  9
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.8
• 拓扑面积：
  69.1
• 氢给体数：
  3
• 氢受体数：
  2

安全信息

• 海关编码：
  2924199090

反应信息

• 作为反应物：
  描述：

  (S)-2-氨基戊酰胺盐酸盐 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 反应 12.0h， 生成 (2S)-pentane-1,2-diamine
  参考文献：
  名称：

  Asymmetric trimethylsilylcyanation of aldehydes catalyzed by chiral salen TiIV complexes with theC 1 symmetry

  摘要：

  Asymmetric trimethylsilylcyanation of a number of aromatic and aliphatic aldehydes catalyzed by chiral Ti-IV complexes prepared in situ from Ti(OPri)(4) and (1S)-[N,N'-bis(2'-hydroxy-3'-tert-butylbenzylidene)]-1,2-diaminoalkanes gives products with (S)-absolute configurations.

  DOI：

  10.1007/bf02503790
• 作为产物：
  描述：

  (S)-2-Amino-pentanimidic acid isopropyl ester; hydrochloride 反应 2.0h， 生成 (S)-2-氨基戊酰胺盐酸盐
  参考文献：
  名称：

  A convenient synthesis of (S)-2-Azidonitriles, (S)-2-aminonitriles and (S)-1,2-diamines

  摘要：

  (S)-2-Azidonitriles (S)-4 are easily accessible from (R)-2-(sulfonyloxy)nitriles (R)-2 by nucleophilic substitution with alkali azides 3 under complete inversion of configuration. The azidonitriles (S)-4 can be converted by catalytic hydrogenation into (S)-2-aminonitriles (S)-8 and by hydrogenation using LiAlH4 into (S)-1, 2-diaminoalkanes (S)-9, respectively, both, (S)-8 and (S)-9, isolated as hydrochlorides. Hydrolysis of the aminonitrile hydrochlorides (S)-8 HCl in a saturated solution of HC1 in alcohol gives (S)-2-amino carboxamide hydrochlorides(S)-10 . HCl with enantiomeric excesses >99% after recrystallization.

  DOI：

  10.1016/0957-4166(96)00044-4

文献信息

• [EN] METHODS OF TREATING ALZHEIMER'S DISEASE USING ARYL ALKANOIC ACID AMIDES<br/>[FR] METHODES DE TRAITEMENT DE LA MALADIE D'ALZHEIMER PAR DES AMIDES D'ACIDE ARYL ALCANOIQUE
  申请人：ELAN PHARM INC

  公开号：WO2003103653A1

  公开（公告）日：2003-12-18

  Disclosed are methods for treating Alzheimer’s disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula 1 (1) wherein the variables R1-R8 and X are defined herein.

  揭示了一种治疗阿尔茨海默病和其他疾病，和/或抑制β-分泌酶，和/或通过使用式1（1）中定义的化合物在哺乳动物体内抑制Aβ肽的沉积的方法。其中变量R1-R8和X在此处定义。
• Tritiation of Peptides to High Specific Radioactivity. Part 1. Synthesis and Biological Properties of [13-(3H4)Norvaline]-?-MSH and of [2,23-Bis((3H2)tyrosine)]ACTH(1-24)
  作者：Alex N. Eberle、Albert Zeller

  DOI：10.1002/hlca.19850680711

  日期：1985.11.13

  radioactivity (> 100 Ci/mmol) using a new tritiation apparatus with which the tritiation reaction can be performed at slightly elevated pressure. This allows short reaction times with the least possible damage to the molecule. The starting compounds for the tritiation were [13-propargylglycine]α-MSH and [2,23-Bis(3′,5′-diiodotyrosine)]ACTH(1–24). Both tritiations were quantitative and yielded products

  使用新型tri化装置将α-MSH和ACTH（1-24）tri化至高比放射性（> 100 Ci / mmol），可以在稍高的压力下进行tri化反应。这样可以缩短反应时间，并尽可能减少对分子的损害。ti化反应的起始化合物为[13-炔丙基甘氨酸]α-MSH和[2,23-Bis（3'，5'-二碘酪氨酸）] ACTH（1-24）。两种tri化都是定量的，并产生高纯度，完整的生物活性以及比放射性分别为115 Ci / mmol和100 Ci / mmol的产物。
• [EN] 3,5-DIAMINO-6-CHLORO-PYRAZINE-2-CARBOXYLIC ACID DERIVATIVES AND THEIR USE AS EPITHELIAL SODIUM CHANNEL BLOCKERS FOR THE TREATMENT OF ARWAY DISEASES<br/>[FR] DÉRIVÉS D'ACIDE 3,5-DIAMINO-6-CHLOROPYRAZINE-2-CARBOXYLIQUE ET LEUR UTILISATION COMME BLOQUEUR DU CANAL SODIQUE ÉPITHÉLIAL POUR LE TRAITEMENT DE MALADIES DES VOIES AÉRIENNES
  申请人：NOVARTIS AG

  公开号：WO2009138378A1

  公开（公告）日：2009-11-19

  A compound of Formula (I) in free or salt or solvate form, where R1, R2, R3, R4, R5, R6, R7, R8 and R9 have the meanings as indicated in the specification, is useful for treating diseases which respond to the blockade of the epithelial sodium channel. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.

  公式（I）的化合物以自由或盐或溶剂形式存在，其中R1、R2、R3、R4、R5、R6、R7、R8和R9的含义如规范中所示，对于治疗对上皮钠通道阻滞有响应的疾病是有用的。还描述了含有这些化合物的药物组合物以及制备这些化合物的方法。
• Methods of treating alzheimer's disease using aryl alkanoic acid amides
  申请人：John Varghese

  公开号：US20060154926A1

  公开（公告）日：2006-07-13

  Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of compounds of formula (1) wherein the variables R 1 -R 8 and X are defined herein.

  本发明涉及使用式（1）中所述的化合物治疗阿尔茨海默病和其他疾病，抑制β-分泌酶酶活性和/或抑制Aβ肽在哺乳动物体内的沉积的方法，其中变量R1-R8和X在此定义。
• 1-substituted alkyl-1,2-dihydro-2-pyrazinone derivatives
  申请人：Toyo Jozo Kabushiki Kaisha

  公开号：US04837319A1

  公开（公告）日：1989-06-06

  1-Substituted alkyl-1,2-dihydro-2-pyrazinone derivatives of the formula ##STR1## wherein A is lower alkyl; R.sub.1 is selected from the group consisting of alkyl, phenyl-lower alkyl, and substituted phenyl-lower alkyl; R.sub.2 and R.sub.3 are each lower alkyl, or together form tetramethylene and R is selected from the group consisting of hydroxyl, hologen, lower alkanoyloxy R.sub.4 -carbamoyloxy, arylthio, 1-methyltetrazole-5-yl-thio, 1-imidazole, morpholino, ##STR2## in which R.sub.4 is lower alkyl or aryl, R.sub.5 is lhydrogen, lower alkyl or aryl, R.sub.6 is hydrogen, lower alkyl, hydroxy-lower alkyl, aryl, aryl-lower alkanoyl, arylcarbonyl, arylsulfonyl or thienyl-lower alkanoyl, Ar is phenyl or phenyl substituted with C.sub.1-3 alkyl, halogen, nitro, or lower alkoxy, A, R.sub.1, R.sub.2 and R.sub.3 are as defined above, m is an integer from 4-6, and n is 2 or 3; and pharmaceutically acceptable salts thereof. The compounds are useful as agents for platelet aggregation inhibition, vasodilation and anti-lipoperoxide generation.

  式子如下：##STR1## 其中A是低碳基；R.sub.1选自烷基、苯基-低碳基、取代苯基-低碳基；R.sub.2和R.sub.3分别是低碳基，或者一起形成四亚甲基，R选自羟基、卤素、低碳酰氧基、R.sub.4-氨基甲酰氧基、芳基硫醇、1-甲基四唑-5-基硫醇、1-咪唑、吗啉基、##STR2## 其中R.sub.4是低碳基或芳基，R.sub.5是氢、低碳基或芳基，R.sub.6是氢、低碳基、羟基-低碳基、芳基、芳基-低碳酰基、芳基羰基、芳基磺酰基或噻吩基-低碳酰基，Ar是苯基或取代了C.sub.1-3烷基、卤素、硝基或低碳氧基的苯基，其中A、R.sub.1、R.sub.2和R.sub.3如上所定义，m是4-6的整数，n为2或3；以及其药学上可接受的盐。这些化合物可用作抑制血小板聚集、扩张血管和抗脂质过氧化物生成的药物。