(1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethanamine | 112395-73-0

• 分子结构分类: 有机化合物 - 有机氧化合物
• 英文名称: (1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethanamine
• 英文别名: (+)-(4S,1'R)-2,2-dimethyl-4-(1'-aminoethyl)-1,3-dioxolane；(R)-1-[(4S)-2,2-Dimethyl-1,3-dioxolan-4-yl]ethanamine
• CAS: 112395-73-0
• 化学式: C₇H₁₅NO₂
• 分子量: 145.202
• InChiKey: IGVMHZDCIZWZGY-PHDIDXHHSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  0
• 重原子数：
  10
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  1.0
• 拓扑面积：
  44.5
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-(2,3-difluorobenzylmercapto)-4,6-dichloropyrimidine 、 (1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethanamine 在 碳酸氢钠 作用下， 以 乙腈 为溶剂， 反应 12.0h， 生成 6-chloro-2-[(2,3-difluorobenzyl)thio]-N-{(1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethyl}pyrimidin-4-amine
  参考文献：
  名称：

  NOVEL COMPOUND 395

  摘要：

  化合物式（1）及其药学上可接受的盐，用于治疗趋化因子介导的疾病和病症。

  公开号：

  US20100016275A1
• 作为产物：
  描述：

  N-benzyl-2,3-O-isopropylidene-D-glyceraldehyde nitrone 在 palladium dihydroxide 氢气 、 zinc dibromide 作用下， 以 乙醚 为溶剂， -40.0~25.0 ℃ 、482.63 kPa 条件下， 反应 78.0h， 生成 (1R)-1-[(4S)-2,2-dimethyl-1,3-dioxolan-4-yl]ethanamine
  参考文献：
  名称：

  Stereocontrolled addition of Grignard reagents to α-alkoxy nitrones. Synthesis of syn and anti 3-amino-1,2-diols

  摘要：

  The stereoselective addition of Grignard reagents to alpha-alkoxy nitrones has been achieved with excellent stereocontrol using ZnBr2 and Et2AlCl as precomplexing agents to obtain the corresponding syn- and anti- adducts, respectively. The obtained hydroxylamines have been transformed into valuable 3-amino-1,2-diols. (C) 1997 Elsevier Science Ltd.

  DOI：

  10.1016/s0957-4166(97)00175-4

文献信息

• [EN] PIPERIDINYL GPCR AGONISTS<br/>[FR] AGONISTES DES RÉCEPTEURS COUPLÉS AUX PROTÉINES G (GPCR) PIPERIDINYLES
  申请人：PROSIDION LTD

  公开号：WO2010004343A1

  公开（公告）日：2010-01-14

  Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.

  式（I）的化合物或其药用盐是GPCR激动剂，可用于治疗糖尿病和肥胖。
• [EN] ANTAGONISTS OF THE ADENOSINE A2A RECEPTOR<br/>[FR] ANTAGONISTES DU RÉCEPTEUR A2A DE L'ADÉNOSINE
  申请人：ADORX THERAPEUTICS LTD

  公开号：WO2021224636A1

  公开（公告）日：2021-11-11

  The present invention relates to compounds of formula I shown below: wherein R0, R1, R2, R3 and A are each as defined in the application. The present invention also relates to processes for the preparation of these compounds, to pharmaceutical compositions comprising them, and to their use in the treatment of diseases or conditions in which adenosine A2a receptor activity is implicated, such as, for example, cancer.

  本发明涉及如下所示的公式I的化合物：其中R0、R1、R2、R3和A分别如申请中所定义。本发明还涉及制备这些化合物的方法，包括它们的药物组合物，并将其用于治疗涉及腺苷A2a受体活性的疾病或症状，例如癌症。
• Asymmetric Synthesis of Primary Amines by Nucleophilic Addition of Alkyllithium Compounds to Aldehyde SAMP/RAMP Hydrazones
  作者：Dieter Enders、Christoph Nübling、Heinrich Schubert

  DOI：10.1002/jlac.199719970608

  日期：1997.6

  temperature. Cleavage of the NN bond of the resulting hydrazines 3 and 8 with Raney-Ni/H2, or of the N-methoxycarbonylhydrazines 9 with Li/NH3, yield the amines 4 with 61–90% ee, the amines 11 with 45–96% de and 93 99% ee. The absolute configuration of the amines 11 was established by X-ray analysis of an appropriate MTPA derivative.

  醛1或5被转换为SAMP腙2或α -烷基化的SAMP腙7和在低温下用有机锂化合物处理。所得肼的NN键的裂解3和8与阮内镍/ H 2，或的Ñ -methoxycarbonylhydrazines 9与Li / NH 3，得到胺4与61-90％ee的，胺11与45- 96％de和93 99％ee。通过对合适的MTPA衍生物进行X射线分析来确定胺11的绝对构型。
• ACYCLIC AMINE INHIBITORS OF 5-METHYTIOADENOSINE PHOSPHORYLASE AND NUCLEOSIDASE
  申请人：Clinch Keith

  公开号：US20110046167A1

  公开（公告）日：2011-02-24

  The present invention relates to compounds of the general formula (I) which are inhibitors of 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase. The invention also relates to the use of these compounds in the treatment of diseases or conditions in which it is desirable to inhibit 5′-methylthioadenosine phosphorylase or 5′-methylthioadenosine nucleosidase including cancer, and to pharmaceutical compositions containing the compounds.

  本发明涉及一般公式（I）的化合物，它们是5'-甲基硫腺苷磷酸化酶或5'-甲基硫腺苷核苷酸酶的抑制剂。本发明还涉及使用这些化合物治疗希望抑制5'-甲基硫腺苷磷酸化酶或5'-甲基硫腺苷核苷酶的疾病或病况，包括癌症，并且涉及含有这些化合物的药物组合物。
• PIPERIDINYL GPCR AGONISTS
  申请人：Bertram Lisa Sarah

  公开号：US20110269734A1

  公开（公告）日：2011-11-03

  Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.

  公式（I）的化合物或其药学上可接受的盐是GPCR激动剂，并且可用于治疗糖尿病和肥胖症。