(2S)-2-(ethylamino)propan-1-ol | 112150-26-2

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: (2S)-2-(ethylamino)propan-1-ol
• CAS: 112150-26-2
• 化学式: C₅H₁₃NO
• mdl: MFCD11053920
• 分子量: 103.164
• InChiKey: SGBGCXQCQVUHNE-YFKPBYRVSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.1
• 重原子数：
  7
• 可旋转键数：
  3
• 环数：
  0.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  (2S)-2-(ethylamino)propan-1-ol 在 偶氮二甲酸二异丙酯 、 N,N-二异丙基乙胺 、 三苯基膦 、 甲胺 作用下， 以 四氢呋喃 、 N-甲基吡咯烷酮 、 乙醇 为溶剂， 反应 39.5h， 生成 tert-butyl N-ethyl-N-[(2S)-1-[[5-(trifluoromethyl)pyrimidin-2-yl]amino]propan-2-yl]carbamate
  参考文献：
  名称：

  [EN] NOVEL N-[(PYRIMIDINYLAMINO)PROPANYL]-, N-[(PYRIDYLAMINO)PROPANYL] - AND N-[(PYRAZINYLAMINO)PROPANYL]ARYLCARBOXAMIDES
  [FR] NOUVEAUX N-[(PYRIMIDINYLAMINO)PROPANYL]-, N-[(PYRIDYLAMINO)PROPANYL] - ET N-[(PYRAZINYLAMINO)PROPANYL]ARYLCARBOXAMIDES

  摘要：

  本发明涉及新颖的N-[(嘧啶基氨基)丙基]-、N-[(吡啶基氨基)丙基]-和N-[(吡嗪基氨基)丙基]芳基羧酰胺衍生物，其制备方法，含有它们的药物组合物以及它们在治疗中的应用，特别是用于治疗或预防与促觉醒素亚型1受体相关的疾病。

  公开号：

  WO2019025275A1
• 作为产物：
  描述：

  (S)-N-ethanoylalanine ethyl ester 在 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 为溶剂， 以70%的产率得到(2S)-2-(ethylamino)propan-1-ol
  参考文献：
  名称：

  合成d'氨基膦次膦酸酯。利用还原非对称催化

  摘要：

  由天然氨基醇或通过还原α-氨基酸和PPh 2 Cl的甲酸酯直接合成手性氨基膦次膦酸酯配体（AMPP）。已经发现它们的阳离子铑配合物是脱氢氨基酸的对映选择性加氢的优良催化剂（ee〜86％，收率〜100％）。酮的不对称还原也可以用新型烷基AMPP *改性铑催化剂（ee 50％）进行。

  DOI：

  10.1016/s0022-328x(00)99348-3

文献信息

• New indazole and indolone derivatives and their use pharmaceuticals
  申请人：Allerton Norfor Charlotte Moira

  公开号：US20050267096A1

  公开（公告）日：2005-12-01

  The present invention provides for compounds of formula (I), which are a class of dopamine agonists, more particularly a class of agonists that are selective for D3 over D2. These compounds are useful for the treatment and/or prevention of sexual dysfunction, for example female sexual dysfunction (FSD), in particular female sexual arousal disorder (FSAD), hypoactive sexual desire disorder (HSDD; lack of interest in sex), female orgasmic disorder (FOD; inability to achieve orgasm); and male sexual dysfunction, in particular male erectile dysfunction (MED). Male sexual dysfunction as referred to herein is meant to include ejaculatory disorders such as premature ejaculation, anorgasmia (inability to achieve orgasm) or desire disorders such as hypoactive sexual desire disorder (HSDD; lack of interest in sex). These compounds are also useful in treating neuropsychiatric disorders and neurodegenerative disorders.

  本发明提供了一类多巴胺激动剂的化合物，具体来说是一类选择性作用于D3而非D2的激动剂。这些化合物可用于治疗和/或预防性功能障碍，例如女性性功能障碍（FSD），特别是女性性唤醒障碍（FSAD），性欲不振障碍（HSDD；对性欲缺乏兴趣），女性性高潮障碍（FOD；无法达到高潮）；以及男性性功能障碍，特别是男性勃起功能障碍（MED）。本文提到的男性性功能障碍包括射精障碍，如早泄，无法达到高潮的无性感（无法达到高潮）或性欲障碍，如性欲不振（HSDD；对性欲缺乏兴趣）。这些化合物还可用于治疗神经精神障碍和神经退行性疾病。
• [EN] NOVEL N-[(PYRIMIDINYLAMINO)PROPANYL]-AND N [(PYRAZINYLAMINO)PROPANYL]ARYLCARBOXAMIDES<br/>[FR] NOUVEAUX N-[(PYRIMIDINYLAMINO)PROPANYL]- ET N [(PYRAZINYLAMINO)PROPANYL]ARYLCARBOXAMIDES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2017178341A1

  公开（公告）日：2017-10-19

  The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyrazinylamino)-propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.

  本发明涉及新颖的N-[(嘧啶基氨基)丙基]-和N-[(吡嗪基氨基)丙基]芳基甲酰胺衍生物，其制备方法，含有它们的药物组合物以及它们在治疗中的应用，特别是在与促觉醒素亚型1受体有关的疾病的治疗或预防中的应用。
• BRANCHED CHAIN ALKYL HETEROAROMATIC RING DERIVATIVE
  申请人：Taisho Pharmaceutical Co., Ltd.

  公开号：EP2862855A1

  公开（公告）日：2015-04-22

  A branched chain alkyl heteroaromatic ring derivative represented by formula (Ia) or a pharmaceutically acceptable salt thereof is useful for treatment or prophylaxis of diseases such as sleep disorder, depression, anxiety disorder, panic disorder, schizophrenia, drug dependence, Alzheimer's disease, Parkinson's disease, Huntington's disease, eating disorder, cephalalgia, hemicrania, pain, digestive diseases, epilepsy, inflammation, immune-related diseases, endocrine-related diseases and hypertension, on the basis of the orexin (OX) receptor antagonist activity.

  由公式（Ia）表示的支链烷基杂芳环衍生物或其药用可接受盐，可用于治疗或预防睡眠障碍、抑郁症、焦虑症、恐慌症、精神分裂症、药物依赖、阿尔茨海默病、帕金森病、亨廷顿病、进食障碍、头痛、偏头痛、疼痛、消化系统疾病、癫痫、炎症、免疫相关疾病、内分泌相关疾病和高血压等疾病，基于促觉醒素（OX）受体拮抗活性。
• New process for the preparation of pristinamycin II.sub.B derivatives
  申请人：Rhone-Poulenc Sante

  公开号：US04775753A1

  公开（公告）日：1988-10-04

  Pristinamycin II.sub.B derivatives of formula I in which R represents: ##STR1## either a 4- to 7-membered nitrogen-containing heterocyclic radical, optionally containing 1 or more other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl, or alkyl of 2 to 4 carbon atoms, substituted by 1 or 2 radicals chosen from phenyl, cycloalkylamino or N-alkyl-N-cycloalkylamino having 3 to 6 ring carbon atoms, alkylamino, dialkylamino or dialkylcarbamoyloxy (the alkyl parts of these last 2 radicals being optionally joined to form, with the nitrogen atom to which they are attached, a 4- to 7-membered saturated or unsaturated heterocycle optionally containing another hetero atom chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form, and unsubstituted or substituted by alkyl) or a said alkyl substituted by one or more 4- or 7-membered nitrogen-containing heterocycles optionally containing 1 or 2 other hetero atoms chosen from nitrogen, oxygen and sulphur in the sulphoxide or sulphone form and unsubstituted or substituted by an alkyl radical, the said heterocycles being attached to the alkyl via a carbon atom, at least one of the substituents carried by the alkyl being a nitrogen-containing substituent capable of forming salts, or a [(S)-1-methyl-2-pyrrolidinyl]methyl radical, the aforesaid alkyl radicals being straight-chain or branched and containing, unless otherwise stated, 1 to 10 carbon atoms each, including isomeric forms thereof and mixtures thereof, and the salts thereof, are made by oxidizing a pristinamycin II.sub.B derivative of formula II ##STR2## with potassium peroxymonosulphate.

  在这个公式中，R代表：##STR1## 要么是一个含氮的4至7元杂环基团，可选地包含1个或多个其他异原子，选择自氮、氧和硫的硫氧化物或砜形式，并且未取代或被烷基取代，或者是含有1或2个苯基、环烷基氨基或N-烷基-N-环烷基氨基，具有3至6个环碳原子的基团的2至4个碳原子的烷基，烷基氨基，二烷基氨基或二烷基氨基羰氧基（这些最后两个基团的烷基部分可选择地与它们附着的氮原子形成，具有4至7个饱和或不饱和的杂环基团，可选地包含另一个异原子，选择自氮、氧和硫的硫氧化物或砜形式，并且未取代或被烷基取代），或者是一个被1个或多个含氮的4-或7-元杂环基团取代的上述烷基，可选地包含1个或2个其他异原子，选择自氮、氧和硫的硫氧化物或砜形式，并且未取代或被烷基取代，这些杂环基团通过一个碳原子连接到烷基上，烷基携带的取代基之一至少是能够形成盐的含氮取代基，或者是[(S)-1-甲基-2-吡咯基]甲基基团，上述烷基基团为直链或支链，并且每个基团包含1至10个碳原子，包括其同分异构体和混合物，以及其盐，通过将公式II的pristinamycin II.sub.B衍生物氧化为钾过氧单硫酸盐而制备。
• [EN] NOVEL N-[(PYRIMIDINYLAMINO)PROPANYL]-AND N-[(PYRIDINYLAMINO)PROPANYL]ARYLCARBOXAMIDES<br/>[FR] NOUVEAUX N-[(PYRIMIDINYLAMINO)PROPANYL]- ET N-[(PYRIDINYLAMINO)PROPANYL]ARYLCARBOXAMIDES
  申请人：BOEHRINGER INGELHEIM INT

  公开号：WO2017178343A1

  公开（公告）日：2017-10-19

  The present invention relates to novel N-[(Pyrimidinylamino)propanyl]- and N-[(Pyridinylamino)propanyl]arylcarboxamide derivatives, processes for their preparation, pharmaceutical compositions containing them and their use in therapy, particularly in the treatment or prevention of conditions having an association with the orexin sub-type 1 receptor.

  本发明涉及新型N-[(嘧啶基氨基)丙基]-和N-[(吡啶基氨基)丙基]芳基甲酰胺衍生物，其制备方法，含有它们的药物组合物以及它们在治疗中的应用，特别是在治疗或预防与促醒素亚型1受体相关的疾病方面。