(2R)-(+)-methylchroman | 320382-27-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 苯并吡喃
• 英文名称: (2R)-(+)-methylchroman
• 英文别名: (2R)-2-methyl-3,4-dihydro-2H-chromene
• CAS: 320382-27-2
• 化学式: C₁₀H₁₂O
• 分子量: 148.205
• InChiKey: KGALVPYTKQIBAA-MRVPVSSYSA-N

物化性质

• 沸点：
  223.8±10.0 °C(Predicted)
• 密度：
  1.006±0.06 g/cm3(Predicted)

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：

  (2R)-(+)-methylchroman 在 dipotassium peroxodisulfate 、 copper(II) sulfate 作用下， 以 水 、 乙腈 为溶剂， 以51%的产率得到(R)-2-methylchroman-4-one
  参考文献：
  名称：

  2-取代的chroman-4-ones的方法：（-）-pinostrobin的合成。

  摘要：

  描述了两种光学活性的2-取代的苯并吡喃-4-酮的方法。第一种利用预先形成的苯并二氢吡喃环的氧化，第二种利用分子内光延环化。该方法被应用于生物活性天然产物（-）-pinostrobin（18）的合成。

  DOI：

  10.1016/s0040-4039(01)00567-6
• 作为产物：
  描述：

  2-溴苯酚 在 正丁基锂 、 三苯基膦 、 偶氮二甲酸二乙酯 作用下， 以 四氢呋喃 为溶剂， 生成 (2R)-(+)-methylchroman
  参考文献：
  名称：

  立体控制的2位取代的苯并二氢吡喃

  摘要：

  描述了两步合成高对映体纯度的2-取代的苯并二氢吡喃。同手性卤代丙醇10与2-溴苯酚（9）的Mitsunobu反应，然后在Parham环烷基化条件下用正丁基锂处理，生成2-取代的苯并吡喃7。该方法学适用于合成天然产物妥罗维他命E（5）和抗病毒BW683C（6）。

  DOI：

  10.1016/s0040-4039(00)01530-6

文献信息

• SUBSTITUTED CHROMAN COMPOUNDS AS CALCIUM SENSING RECEPTOR MODULATORS
  申请人：LUPIN LIMITED

  公开号：US20150038546A1

  公开（公告）日：2015-02-05

  The present invention provides calcium sensing receptor modulators (CaSR). In particular, the compounds described herein are useful for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of calcium sensing receptors (CaSR). The invention also provides herein the pharmaceutical compositions thereof, and methods for treating, managing, and/or lessening the severity of diseases, disorders, syndromes and/or conditions associated with the modulation of CaSR. The invention also relates to process for the preparation of the compounds of the invention.

  本发明提供了钙感应受体调节剂（CaSR）。特别是，本发明的化合物可用于治疗、管理和/或减轻与钙感应受体（CaSR）调节相关的疾病、障碍、综合征和/或症状。本发明还提供了其药物组合物，以及用于治疗、管理和/或减轻与CaSR调节相关的疾病、障碍、综合征和/或症状的方法。本发明还涉及用于制备本发明化合物的过程。
• [EN] FXR RECEPTOR AGONIST<br/>[FR] AGONISTE DU RÉCEPTEUR FXR<br/>[ZH] FXR受体激动剂
  申请人：XUANZHU PHARMA CO LTD

  公开号：WO2017133521A1

  公开（公告）日：2017-08-10

  本发明提供下述通式(1)所示的化合物、其药学上可接受的盐、其酯或其立体异构体，本发明还提供上述化合物的制备方法以及在制备用于预防和/或治疗非酒精性脂肪肝、原发性胆汁性肝硬化、脂质代谢紊乱、糖尿病并发症及恶性肿瘤的药物中的用途。其中，R1、R2、R3、R4、m、n、W、A、Z、E、F、X、Y如说明书中所定义。
• Inter- and intramolecular Mitsunobu reaction based approaches to 2-substituted chromans and chroman-4-ones
  作者：Kevin J. Hodgetts

  DOI：10.1016/j.tet.2005.04.047

  日期：2005.7

  Two approaches to optically active 2-substituted chromans and chrornan-4-ones are described. The first utilized an intermolecular Mitsunobu reaction of a homochiral halopropanol and 2-bromophenol followed by cyclization to the 2-substituted chroman. In addition, a double lithiation procedure was developed to introduce additional functionality to the chroman. The second approach utilized an intramolecular Mitsunobu cyclization to give the 2-substituted chroman-4-one nucleus. The methodologies were applied to the syntheses of several biologically active natural and synthetic products. (c) 2005 Elsevier Ltd. All rights reserved.
• Aryl(sulfonyl)amino Group: A Convenient and Stable Yet Activated Modification of Amino Group for Its Intramolecular Displacement
  作者：Yuzo Kato、Dinh Hoang Yen、Yasuhiro Fukudome、Takeshi Hata、Hirokazu Urabe

  DOI：10.1021/ol101541p

  日期：2010.9.17

  Aryl(sulfonyl)amino groups, readily derived from sulfonyl- or arylamines by standard methods as well as the recently introduced methods of sulfonylation and arylation, proved to be good leaving groups in intramolecular substitution reactions by various nitrogen, oxygen, and carbon nucleophiles.
• NOVEL THERAPEUTIC AGENT FOR ALZHEIMER'S DISEASE
  申请人：NAGASAKI UNIVERSITY

  公开号：US20170252318A1

  公开（公告）日：2017-09-07

  The present invention aims to provide a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease, which has a novel action mechanism and shows less side effects. A polyphenol derivative having liposolubility enhanced by the introduction of at least one kind of a liposoluble group selected from the group consisting of a chain saturated hydrocarbon group, a chain unsaturated hydrocarbon group, a cyclic saturated hydrocarbon group, a cyclic unsaturated hydrocarbon group, an aromatic hydrocarbon group, a liposoluble vitamin residue and a sterol residue has an action to potentiate neprilysin activity, and is useful as a pharmaceutical agent for the prophylaxis and/or treatment of Alzheimer's disease.