(+)-(2S)-2-tert-butylpiperidine

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 哌啶类
• 英文名称: (+)-(2S)-2-tert-butylpiperidine
• 英文别名: (2S)-2-tert-butylpiperidine
• 化学式: C₉H₁₉N
• mdl: MFCD02663555
• 分子量: 141.257
• InChiKey: XVHXKRXHTZYTDU-QMMMGPOBSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.4
• 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：
  12
• 氢给体数：
  1
• 氢受体数：
  1

反应信息

• 作为产物：
  描述：

  (5S,2E)-5-benzyloxycarbonylamino-6,6-dimethylhept-2-enal 在 palladium on activated charcoal 氢气 作用下， 以 乙醇 为溶剂， 20.0 ℃ 、448.17 kPa 条件下， 反应 15.0h， 生成 (+)-(2S)-2-tert-butylpiperidine
  参考文献：
  名称：

  哌啶生物碱不对称合成的一般和对映异构方法：（R）-胡椒碱，（S）-可宁和其他2-烷基哌啶的简明合成

  摘要：

  已经建立了用于制备高度对映体富集的2-烷基哌啶的简单且非常有效的方案，其允许以相同的起始材料在立体发生中心制备具有任何所需构型的最终杂环。合成的关键步骤依赖于非对映的aza-Michael反应方案，使用容易获得且便宜的试剂（+）-（S，S）-伪麻黄碱作为手性助剂。

  DOI：

  10.1016/j.tet.2007.08.067

文献信息

• CATALYST FOR ASYMMETRIC HYDROGENATION
  申请人：MAEDA Hironori

  公开号：US20100324338A1

  公开（公告）日：2010-12-23

  This invention aims at providing a catalyst for producing an optically active aldehyde or an optically active ketone, which is an optically active carbonyl compound, by carrying out selective asymmetric hydrogenation of an α,β-unsaturated carbonyl compound, particularly a catalyst which is insoluble in a reaction mixture for obtaining optically active citronellal which is useful as a flavor or fragrance, by carrying out selective asymmetric hydrogenation of citral, geranial or neral; and a method for producing a corresponding optically active carbonyl compound. The invention relates to a catalyst for asymmetric hydrogenation of an α,β-unsaturated carbonyl compound, which comprises a powder of at least one metal selected from metals belonging to Group 8 to Group 10 of the Periodic Table, or a metal-supported substance in which at least one metal selected from metals belonging to Group 8 to Group 10 of the Periodic Table is supported on a support, an optically active cyclic nitrogen-containing compound and an acid.

  这项发明旨在通过对α，β-不饱和羰基化合物进行选择性不对称加氢，特别是通过对柠檬醛、香叶醛或柠檬醛进行选择性不对称加氢，从而提供用作香料或香精的有用的光学活性香茅醛的催化剂，该香茅醛是一种光学活性羰基化合物；以及生产相应的光学活性羰基化合物的方法。该发明涉及一种用于不对称加氢α，β-不饱和羰基化合物的催化剂，其包括来自周期表第8至第10族金属中至少一种金属的粉末，或者至少一种来自周期表第8至第10族金属的金属负载物质，该金属负载在一种支撑物上，还包括光学活性的含氮环化合物和酸。
• Pro-drugs of riluzole and their method of use for the treatment of amyotrophic lateral sclerosis
  申请人：Biohaven Pharmaceutical Holding Company Limited

  公开号：US10357497B2

  公开（公告）日：2019-07-23

  Pharmaceutical compositions of the invention include substituted riluzole pro drugs useful for the treatment of amyotrophic lateral sclerosis (ALS) and related disorders through the release of riluzole, especially to avoid patient to patient variability in first pass, hepatic metabolism promoted by Cyp 1A2. Pro-drugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process. The invention further includes pro-drugs of riluzole useful for the treatment of disease states that can be treated with riluzole through the release of riluzole from a pro-drug agent.

  本发明的药物组合物包括通过释放利鲁唑治疗肌萎缩性脊髓侧索硬化症（ALS）和相关疾病的取代利鲁唑原药，特别是避免了由Cyp 1A2促进的肝脏代谢中患者与患者之间的首过差异。利鲁唑原药对肝脏代谢的稳定性增强，通过口服进入全身循环，然后通过酶或一般生物物理释放过程裂解，在血浆中释放利鲁唑。本发明还包括可用于治疗疾病的利鲁唑原药，这些疾病可以通过利鲁唑原药释放利鲁唑来治疗。
• Prodrugs of riluzole and their method of use
  申请人：Biohaven Pharmaceutical Holding Company Ltd.

  公开号：US10844026B2

  公开（公告）日：2020-11-24

  Pharmaceutical compositions of the invention include substituted riluzole prodrugs useful for the treatment of cancers including melanoma, breast cancer, brain cancer, and prostate cancer through the release of riluzole. Prodrugs of riluzole have enhanced stability to hepatic metabolism and are delivered into systemic circulation by oral administration, and then cleaved to release riluzole in the plasma via either an enzymatic or general biophysical release process.

  本发明的药物组合物包括取代的利鲁唑原药，可通过释放利鲁唑治疗癌症，包括黑色素瘤、乳腺癌、脑癌和前列腺癌。利鲁唑原药对肝脏代谢的稳定性增强，通过口服进入全身循环，然后通过酶或一般生物物理释放过程裂解，在血浆中释放利鲁唑。
• Macrocyclic compounds for treatment of medical disorders
  申请人：Achillion Pharmaceuticals, Inc.

  公开号：US11053253B2

  公开（公告）日：2021-07-06

  Macrocyclic Complement Factor D inhibitors, pharmaceutical compositions, and uses thereof, as well as processes for their manufacture are provided. The compounds provided include Formula I, Formula II, Formula III, Formula IV, Formula V, Formula VI, Formula VII, and Formula VIII or a pharmaceutically acceptable salt, prodrug, isotopic analog, N-oxide, or isolated isomer thereof, optionally in a pharmaceutically acceptable composition. The inhibitors described herein target Factor D and inhibit or regulate the complement cascade.

  本发明提供了大环补体因子 D 抑制剂、药物组合物及其用途以及制造工艺。所提供的化合物包括式I、式II、式III、式IV、式V、式VI、式VII和式VIII或其药学上可接受的盐、原药、同位素类似物、N-氧化物或分离异构体，可选药学上可接受的组合物。本文所述的抑制剂以因子 D 为靶点，抑制或调节补体级联。
• 7-OXO-1,6-DIAZABICYCLO[3.2.1 ]OCTANE DERIVATIVES AND THEIR USE AS ANTIBACTERIAL AGENTS
  申请人：WOCKHARDT LIMITED

  公开号：US20170044159A1

  公开（公告）日：2017-02-16

  Compounds of Formula (I), their preparation, and use in preventing or treating a bacterial infection are disclosed.