2-(azetidin-3-yl)propan-2-ol | 1257293-78-9

• 分子结构分类: 有机化合物 - 有机氮化合物
• 英文名称: 2-(azetidin-3-yl)propan-2-ol
• CAS: 1257293-78-9
• 化学式: C₆H₁₃NO
• mdl: MFCD22581534
• 分子量: 115.175
• InChiKey: ALDIUUDTUYLMIV-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.2
• 重原子数：
  8
• 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：
  32.3
• 氢给体数：
  2
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-(azetidin-3-yl)propan-2-ol 在 palladium 10% on activated carbon 、 氢气 、 caesium carbonate 作用下， 以 甲醇 、 乙腈 为溶剂， 生成 2-(1-(4-aminopyridin-2-yl)azetidin-3-yl)propan-2-ol
  参考文献：
  名称：

  Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors

  摘要：

  DOI：

  10.1016/j.bmcl.2022.128552
• 作为产物：
  描述：

  1-(叔丁氧基羰基)氮杂环丁烷-3-甲酸甲酯 在 三氟乙酸 作用下， 以 四氢呋喃 、 二氯甲烷 为溶剂， 反应 4.0h， 生成 2-(azetidin-3-yl)propan-2-ol
  参考文献：
  名称：

  Synthesis and biological evaluation of 4-(pyridine-4-oxy)-3-(tetrahydro-2H-pyran-4-yl)-pyrazole derivatives as novel, potent of ALK5 receptor inhibitors

  摘要：

  DOI：

  10.1016/j.bmcl.2022.128552

文献信息

• [EN] AZAINDAZOLE COMPOUNDS AS INHIBITORS OF T790M CONTAINING EGFR MUTANTS<br/>[FR] COMPOSÉS D'AZAINDAZOLE EN TANT QU'INHIBITEURS DE LA T790M CONTENANT DES MUTANTS DE L'EGFR
  申请人：GENENTECH INC

  公开号：WO2014210354A1

  公开（公告）日：2014-12-31

  This invention relates to novel compounds of formula (I), which are inhibitors of T790M containing EGFR mutants, to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the prevention or treatment of cancer.

  这项发明涉及公式（I）的新化合物，这些化合物是T790M含有EGFR突变体的抑制剂，涉及含有它们的药物组合物，它们的制备过程，以及它们在预防或治疗癌症中的应用。
• KDM1A INHIBITORS FOR THE TREATMENT OF DISEASE
  申请人：Imago Biosciences, Inc.

  公开号：US20160237043A1

  公开（公告）日：2016-08-18

  Disclosed herein are new compounds and compositions and their application as pharmaceuticals for the treatment of diseases. Methods of inhibition of KDM1A, methods of increasing gamma globin gene expression, and methods to induce differentiation of cancer cells in a human or animal subject are also provided for the treatment of diseases such as acute myelogenous leukemia.

  本文披露了新化合物和组合物，以及它们作为药物治疗疾病的应用。还提供了抑制KDM1A的方法，增加γ球蛋白基因表达的方法，以及诱导人类或动物主体中癌细胞分化的方法，用于治疗急性髓性白血病等疾病。
• [EN] SUBSTITUTED 1,1'-BIPHENYL COMPOUNDS AND METHODS USING SAME<br/>[FR] COMPOSÉS 1,1'-BIPHÉNYLE SUBSTITUÉS ET LEURS PROCÉDÉS D'UTILISATION
  申请人：ARBUTUS BIOPHARMA INC

  公开号：WO2021158481A1

  公开（公告）日：2021-08-12

  The present invention includes substituted 1,1'-biphenyl compounds, analogues thereof, and compositions comprising the same. In one aspect, the compounds contemplated in the invention can be used to treat, ameliorate, or prevent hepatitis B virus (HBV) and/or hepatitis D virus (HDV) infections in a patient. In another aspect, the compounds contemplated in the invention can be used to treat, ameliorate, and/or prevent cancer in a patient.

  本发明包括取代的1,1'-联苯化合物，其类似物，以及包含它们的组合物。在一个方面，本发明中考虑的化合物可用于治疗、改善或预防患者体内的乙型肝炎病毒（HBV）和/或丙型肝炎病毒（HDV）感染。在另一个方面，本发明中考虑的化合物可用于治疗、改善和/或预防患者体内的癌症。
• FUSED PYRIMIDINE COMPOUND, INTERMEDIATE, PREPARATION METHOD THEREFOR, AND COMPOSITION AND APPLICATION THEREOF
  申请人：SHANGHAI YINGLI PHARMACEUTICAL CO., LTD

  公开号：US20160214994A1

  公开（公告）日：2016-07-28

  Disclosed are a fused pyrimidine compound, an intermediate, a preparation method therefor, and a composition and an application thereof. The present invention provides a fused pyrimidine compound shown in formula I, pharmaceutically acceptable salt, hydrate, solvate, and an optical isomer or prodrug of the compound. The present invention further provides applications of the fused pyrimidine compound shown in formula I, the pharmaceutically acceptable salt, the hydrate, solvate, and the optical isomer or the prodrug of the compound in the preparing drugs for curing and/or preventing a kinase-related disease. The fused pyrimidine compound I of the present invention is an efficient PI3 kinase depressor, and can be used to prepare drugs for preventing and/or curing cell-proliferation diseases such as cancer, infection, inflammation, and an autoimmune disease.

  揭示了一种融合嘧啶化合物，其中间体，制备方法以及其组成和应用。本发明提供了一种如式I所示的融合嘧啶化合物，该化合物的药用可接受盐，水合物，溶剂合物，以及光学异构体或前药。本发明还提供了应用式I所示的融合嘧啶化合物，药用可接受盐，水合物，溶剂合物，以及该化合物的光学异构体或前药在制备用于治疗和/或预防激酶相关疾病的药物中。本发明的融合嘧啶化合物I是一种高效的PI3激酶抑制剂，可用于制备用于预防和/或治疗细胞增殖性疾病，如癌症，感染，炎症和自身免疫疾病的药物。
• FUSED HETEROCYCLIC COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTCIAL COMPOSITION, AND USES THEREOF
  申请人：SHANGHAI YINGLI PHARMACEUTICAL CO., LTD

  公开号：US20160244432A1

  公开（公告）日：2016-08-25

  Disclosed are a fused heterocyclic compound, a preparation method therefor, a pharmaceutical composition, and uses thereof. The fused heterocyclic compound is shown in formula I, formula II, or formula III. The preparation method of the fused heterocyclic compound and/or the pharmaceutically acceptable salt thereof in the present invention comprises three synthesizing routes. The present invention also provides a pharmaceutical composition of the fused heterocyclic compound, the pharmaceutical composition containing one or more of the fused heterocyclic compound shown in formula I, formula II, or formula III, the pharmaceutically acceptable salt thereof, hydrates, solvent compounds, polymorphs and prodrugs thereof, and a pharmaceutically acceptable carrier. The present invention also relates to an application of the fused heterocyclic compound and/or the pharmaceutical composition in preparing kinase inhibitors and in preparing drugs for preventing and treating diseases related to kinase. The fused heterocyclic compound of the present invention has selective inhibition function on PI3Kδ, and can be used for preparing drugs for preventing and treating cell proliferation diseases such as cancers, infections, inflammations, or autoimmune diseases.

  揭示了一种融合杂环化合物，其制备方法，药物组合物及其用途。所述融合杂环化合物如公式I、公式II或公式III所示。本发明的所述融合杂环化合物和/或其药用可接受盐的制备方法包括三种合成途径。本发明还提供了一种包含融合杂环化合物的药物组合物，所述药物组合物含有公式I、公式II或公式III所示的一个或多个融合杂环化合物，其药用可接受盐、水合物、溶剂化合物、多型体和前药，以及药用可接受载体。本发明还涉及应用所述融合杂环化合物和/或药物组合物制备激酶抑制剂以及制备用于预防和治疗与激酶相关疾病的药物。本发明的融合杂环化合物对PI3Kδ具有选择性抑制功能，可用于制备用于预防和治疗细胞增殖性疾病如癌症、感染、炎症或自身免疫疾病的药物。