tert-butyl 1-hydroxyhex-5-en-2-ylcarbamate | 1174400-46-4

• 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
• 英文名称: tert-butyl 1-hydroxyhex-5-en-2-ylcarbamate
• 英文别名: Tert-butyl (1-hydroxyhex-5-en-2-yl)carbamate；tert-butyl N-(1-hydroxyhex-5-en-2-yl)carbamate
• CAS: 1174400-46-4
• 化学式: C₁₁H₂₁NO₃
• 分子量: 215.293
• InChiKey: AVJJIUDUTJDPQD-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  15
• 可旋转键数：
  7
• 环数：
  0.0
• sp3杂化的碳原子比例：
  0.73
• 拓扑面积：
  58.6
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  tert-butyl 1-hydroxyhex-5-en-2-ylcarbamate 在 吡啶-N-氧化物 、 potassium osmate(VI) dihydrate 、 copper(II) bis(trifluoromethanesulfonate) 、 柠檬酸 、 sodium sulfite 作用下， 以 乙腈 为溶剂， 反应 36.5h， 以82%的产率得到(2S,5R)-1-t-butoxycarbonyl-(2,5)-bis(hydroxymethyl)pyrrolidine
  参考文献：
  名称：

  A Lewis Acid Promoted Oxidative Cyclization

  摘要：

  Replacing trifluoroacetic acid with it catalytic amount of Lewis acid in the osmium mediated oxidative cyclization results in higher yielding reactions that can proceed nearly an order of magnitude faster. The osmium loading can also be reduced to as little its 0.2 mol %. Furthermore, these mildly acidic conditions are capable of tolerating a wide range of acid sensitive protecting groups that are incompatible with previous cyclization conditions.

  DOI：

  10.1021/jo901243y
• 作为产物：
  描述：

  methyl 2-[(tert-butoxycarbonyl)amino]hex-5-enoate 在 lithium tri-tert-butoxyaluminum hydride 作用下， 以 四氢呋喃 为溶剂， 以75%的产率得到tert-butyl 1-hydroxyhex-5-en-2-ylcarbamate
  参考文献：
  名称：

  Pd-Catalyzed Carboamination of Oxazolidin-2-ones: A Stereoselective Route to trans-2,5-Disubstituted Pyrrolidines

  摘要：

  Palladium-catalyzed carboamination reactions between aryl bromides and 4-(but-3-enyl)-substituted oxazolidin-2-ones are described. These transformations afford bicyclic oxazolidin-2-one derivatives that can be converted to trans-2,5-disubstituted pyrrolidines in one step. The starting materials are easily prepared from amino acid precursors, and products that contain up to three stereocenters are generated with >20:1 dr.

  DOI：

  10.1021/ol1006828

文献信息

• [EN] MODULATORS OF THE INTEGRATED STRESS RESPONSE PATHWAY<br/>[FR] MODULATEURS DE LA VOIE DE RÉPONSE AU STRESS INTÉGRÉE
  申请人：EVOTEC INT GMBH

  公开号：WO2020216764A1

  公开（公告）日：2020-10-29

  The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R1 to R3, A1 and A2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing one or more diseases or disorders associated with integrated stress response.

  本发明涉及式(I)的化合物或其药学上可接受的盐、溶剂和水合物、互变体或立体异构体，其中R1至R3、A1和A2的含义如描述和索赔中所示。该发明还涉及包含所述化合物的药物组合物，其用作药物以及用于治疗和预防与综合性应激反应相关的一种或多种疾病或障碍的方法。
• [EN] PIM KINASE INHIBITOR<br/>[FR] INHIBITEUR DE PIM KINASE<br/>[ZH] PIM激酶抑制剂
  申请人：HANGZHOU BANGSHUN PHARMACEUTICAL CO LTD

  公开号：WO2022166860A1

  公开（公告）日：2022-08-11

  一种具有通式(I)所示结构的化合物、其氘代物、立体异构体或药学上可接受的盐、包含其的药物组合物以及其用途。该化合物具有良好的PIM激酶抑制效果，是一种新型、高活性、低毒性的理想PIM抑制剂，可用于治疗和/或预防急性髓系白血病、骨髓纤维化、慢性淋巴细胞性白血病等血液瘤、胃癌、前列腺癌等实体瘤等疾病。
• NEW BICYCLIC ANTIBIOTICS
  申请人：Actelion Pharmaceuticals Ltd.

  公开号：EP1799676A2

  公开（公告）日：2007-06-27
• ANTIBIOTIC COMPOUNDS
  申请人：Actelion Pharmaceuticals Ltd.

  公开号：EP1996579A2

  公开（公告）日：2008-12-03
• MODULATORS OF THE INTEGRATED STRESS RESPONSE PATHWAY
  申请人：EVOTEC INTERNATIONAL GMBH

  公开号：US20220213078A1

  公开（公告）日：2022-07-07

  The present invention relates to compounds of formula (I) or pharmaceutically acceptable salts, solvates, hydrates, tautomers or stereoisomers thereof, wherein R 1 to R 3 , A 1 and A 2 have the meaning as indicated in the description and claims. The invention further relates to pharmaceutical compositions comprising said compounds, their use as medicament and in a method for treating and preventing one or more diseases or disorders associated with integrated stress response.