2,4-二甲基-2,3-二氢-1-苯并呋喃 | 153782-72-0

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 香豆素
• 中文名称: 2,4-二甲基-2,3-二氢-1-苯并呋喃
• 英文名称: 2,3-dihydro-2,4-dimethylbenzofuran
• 英文别名: 2,4-Dimethyl-2,3-dihydro-1-benzofuran
• CAS: 153782-72-0
• 化学式: C₁₀H₁₂O
• 分子量: 148.205
• InChiKey: YOIIMWIPUXHZLB-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.7
• 重原子数：
  11
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.4
• 拓扑面积：
  9.2
• 氢给体数：
  0
• 氢受体数：
  1

反应信息

• 作为反应物：
  描述：

  2,4-二甲基-2,3-二氢-1-苯并呋喃 在 盐酸 、 titanium(III) chloride 、 硝酸 作用下， 以 四氯化碳 、 溶剂黄146 为溶剂， 反应 5.0h， 生成 5-amino-2,3-dihydro-2,4-dimethylbenzofuran hydrochloride
  参考文献：
  名称：

  The fischer indolisation reaction and the synthesis of dihydroindenoindoles

  摘要：

  The Fischer reaction between indanones and certain alkoxyarylhydrazines fails; the indanones are returned unreacted and the arylhydrazines are converted into the corresponding alkoxy-2-chloroarylamines and other products. A new N-amination route to arylhydrazines from the arylamines has been developed and it has been demonstrated that problems with the indolisation of alkoxyarylhydrazones can be circumvented by ring closures of their O-tosylated analogues. Some results using the Lepke synthesis of indoles are recorded.

  DOI：

  10.1016/s0040-4020(01)81911-6
• 作为产物：
  描述：

  2,4-dimethyl-5-nitro-2,3-dihydrobenzo<2,3>furan 在 盐酸 、 sodium dithionate 、 titanium(III) chloride 、 sodium nitrite 作用下， 以 盐酸 、 溶剂黄146 为溶剂， 反应 3.17h， 生成 2,4-二甲基-2,3-二氢-1-苯并呋喃
  参考文献：
  名称：

  The fischer indolisation reaction and the synthesis of dihydroindenoindoles

  摘要：

  The Fischer reaction between indanones and certain alkoxyarylhydrazines fails; the indanones are returned unreacted and the arylhydrazines are converted into the corresponding alkoxy-2-chloroarylamines and other products. A new N-amination route to arylhydrazines from the arylamines has been developed and it has been demonstrated that problems with the indolisation of alkoxyarylhydrazones can be circumvented by ring closures of their O-tosylated analogues. Some results using the Lepke synthesis of indoles are recorded.

  DOI：

  10.1016/s0040-4020(01)81911-6

文献信息

• C- ARYL GLYCOSID DERIVATIVES, PHARMACEUTICAL COMPOSITION, PREPARATION PROCESS AND USES THEREOF
  申请人：SHANGHAI DE NOVO PHARMATECH CO. LTD.

  公开号：US20170037038A1

  公开（公告）日：2017-02-09

  This invention relates to a kind of C-aryl glycoside derivatives, its pharmaceutical compositions, preparation methods, and uses thereof. The preparation method comprises: method 1: in a solvent, deprotecting the acetyl protecting groups of compound 1-f in the presence of a base; method 2: 1) compound 2-g reacts with via Mitsunobu reaction; 2) deprotecting the acetyl protecting groups of compound 2-f obtained from step 1; method 3: 1) compound 2-g reacts with via nucleophilic substitution reaction; 2) deprotecting the acetyl protecting groups of compound 3-f obtained from step 1. The pharmaceutical composition comprises a kind of C-aryl glycoside derivatives; it's pharmaceutically acceptable salts and/or prodrugs thereof and excipient thereof. This invention further relates to a kind of C-aryl glycoside derivatives, it's pharmaceutically acceptable salts or pharmaceutical compositions thereof for the use in preparation of a SGLT inhibitor. The C-aryl glycoside derivatives of this invention provides a new direction for the study of SGLT inhibitors.

  这项发明涉及一种C-芳基糖苷衍生物，其药物组合物、制备方法及其用途。制备方法包括：方法1：在溶剂中，在碱的存在下去保护化合物1-f的乙酰保护基；方法2：1）化合物2-g通过Mitsunobu反应发生反应；2）去除从步骤1得到的化合物2-f的乙酰保护基；方法3：1）化合物2-g通过亲核取代反应发生反应；2）去除从步骤1得到的化合物3-f的乙酰保护基。药物组合物包括一种C-芳基糖苷衍生物；其药学上可接受的盐和/或前药以及赋形剂。这项发明还涉及一种C-芳基糖苷衍生物，其药学上可接受的盐或其药物组合物，用于制备SGLT抑制剂。这项发明的C-芳基糖苷衍生物为SGLT抑制剂的研究提供了新的方向。
• AMIDE COMPOUND
  申请人：Setoh Masaki

  公开号：US20100041891A1

  公开（公告）日：2010-02-18

  A compound having GPR52 agonist activity or a salt thereof is provided. The compound can be provided as a preventive/therapeutic agent for schizophrenia or the like. The compound is represented by the following formula: wherein A represents —CONR a — or —NR a CO—, R a represents a hydrogen atom or the like, B represents a hydrogen atom or the like, a ring Cy1 represents a six-membered aromatic ring which may have one or more substituents in addition to a group represented by -A-B, a ring Cy2 represents a six-membered ring which may be substituted with a halogen atom or the like, a ring Cy3 represents a five- or six-membered ring which may have one or more substituents; X represents C 1-2 alkylene or the like, m represents an integer of 0 to 2, and a ring Cy4 represents a six-membered aromatic ring which may have one or more substituents.

  提供具有GPR52激动剂活性或其盐的化合物。该化合物可作为预防/治疗精神分裂症等疾病的药物。该化合物由以下公式表示：其中A代表—CONRa—或—NRaCO—，Ra代表氢原子或类似物质，B代表氢原子或类似物质，环Cy1代表一个六元芳香环，除了由-A-B表示的基团外，可能有一个或多个取代基，环Cy2代表一个六元环，可能被卤素原子或类似物质取代，环Cy3代表一个有一个或多个取代基的五元或六元环；X代表C1-2烷基或类似物质，m代表0到2之间的整数，环Cy4代表一个六元芳香环，可能有一个或多个取代基。
• METHOD FOR THE SYNTHESIS OF 4-BENZOFURAN-CARBOXYLIC ACID
  申请人：Burgos Alain

  公开号：US20090131688A1

  公开（公告）日：2009-05-21

  The invention concerns a novel method for synthesis of 4-benzofuran-carboxylic acid or alkyl ester thereof. This method is characterized in that a reaction for aromatization of a compound of formula (II) is performed for the synthesis of the compound of formula (I), according to the scheme A2 below: wherein R independently represents hydrogen or a linear or branched C 1 - 15 alkyl group. With the invention, it is possible to industrially synthesize 4-benzofuran-carboxylic acid or alkyl ester thereof with good yield and very good purity.

  该发明涉及一种合成4-苯并呋喃羧酸或其烷基酯的新方法。该方法的特点在于，根据下面的方案A2，对式（II）化合物进行芳香化反应以合成式（I）的化合物：其中R独立表示氢或直链或支链的C1-15烷基基团。通过这项发明，可以以良好的产率和非常高的纯度工业化合成4-苯并呋喃羧酸或其烷基酯。
• Dihydrobenzofuran production from catalytic tandem Claisen rearrangement–intramolecular hydroaryloxylation of allyl phenyl ethers in subcritical water
  作者：Ligang Luo、Chunze Liu、Zhiqiang Hou、Yuanyuan Wang、Liyi Dai

  DOI：10.1039/c4ra04689g

  日期：——

  mild method for the preparation of dihydrobenzofurans through hydrothermal catalytic tandem Claisen rearrangement–intramolecular hydroaryloxylation of allyl phenyl ethers. This reaction provides a new method for constructing dihydrobenzofurans, a process that is potentially applicable to natural product synthesis. SBA-15, TS-1, HZSM-5 were chosen as catalysts in a hydrothermal reaction medium between 200

  我们在此报告了一种温和的方法，该方法通过水热催化串联Claisen重排-烯丙基苯基醚的分子内氢芳氧基化来制备二氢苯并呋喃。该反应提供了构建二氢苯并呋喃的新方法，该方法可能适用于天然产物的合成。选择SBA-15，TS-1，HZSM-5作为200-320°C水热反应介质中的催化剂。HZSM-5催化剂表现出最高的催化活性，研究了烯丙基苯基醚-水的摩尔比，时间，压力，温度和催化剂对水热条件下克莱森加氢芳氧基化反应的影响。后两个过程变量对产品的产量和分布影响最大。
• 3-AZA-BICYCLO[3.3.0]OCTANE COMPOUNDS
  申请人：Aissaoui Hamed

  公开号：US20100184808A1

  公开（公告）日：2010-07-22

  The invention relates to 3-aza-bicyclo[3.3.0]octane derivatives of the formula (I) wherein R 1 , R 2 , R 3 , and A are as described in the description and their use as orexin receptor antagonists.

  本发明涉及3-aza-bicyclo [3.3.0]辛烷衍生物，其化学式为(I)，其中R1，R2，R3和A如说明书所述，并将其用作促进醒觉素受体拮抗剂。