trans-1-(3,4-difluorophenyl)-1-propene

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: trans-1-(3,4-difluorophenyl)-1-propene
• 英文别名: 1,2-difluoro-4-[(E)-prop-1-enyl]benzene
• 化学式: C₉H₈F₂
• 分子量: 154.159
• InChiKey: SZZSOKKIWGZRQJ-NSCUHMNNSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.1
• 重原子数：
  11
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.11
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  氨基甲酸乙酯 、 trans-1-(3,4-difluorophenyl)-1-propene 在 Hydroquinone 1,4-phthalazinediyl diether 、 potassium dioxotetrahydroxoosmate(VI) 、 1,3-二氯-5,5-二甲基海因 作用下， 以 丙醇 、 水 为溶剂， 生成 (4S,5S)-4-(3,4-difluorophenyl)-5-methyloxazolidin-2-one 、 (4R,5R)-4-(3,4-difluorophenyl)-5-methyloxazolidin-2-one
  参考文献：
  名称：

  一锅法制备手性恶唑烷丁-2-酮中无尖锐不对称氨基羟基化反应的实际应用和应用。

  摘要：

  [反应：见正文]手性恶唑烷-2-酮在手性助剂方面具有合成价值，并且许多具有药学上令人关注的生物学活性。该交流侧重于方便，实用的一锅法制备高收率，高对映选择性的手性4,5-二取代的oxazolidan-2-ones，方法是使用改良的Sharpless不对称氨基羟基化β-取代的苯乙烯衍生物，然后进行碱介导的闭环。已经使用1，3-二氯-5，5-二甲基乙内酰脲作为次氯酸叔丁酯的易于处理的市售替代品在小规模和大规模上证明了该方法。

  DOI：

  10.1021/ol006255z

文献信息

• Process for preparing &bgr;-hydroxycarbamates and their conversion to oxazolidinones
  申请人：Merck & Co., Inc.

  公开号：US06372911B1

  公开（公告）日：2002-04-16

  A process for preparing a &bgr;-hydroxy carbamate product is disclosed. The process comprises reacting an olefin compound containing at least one carbon-carbon double bond with a carbamate in an aqueous solvent and in the presence of a base, an osmium catalyst, a co-oxidant selected from a halohydantoin, a haloisocyanuric acid, and an alkali metal salt of a haloisocyanuric acid, and optionally an asymmetric ligand, to form a reaction mixture containing the &bgr;-hydroxy carbamate product. The process optionally further comprises treating the &bgr;-hydroxy carbamate product with additional base to form an oxazolidinone. The oxazolidinones are useful as chiral auxiliary agents and as intermediates for the formation of pharmaceutically active substances such as alpha 1 a adrenergic receptor antagonists. A process for preparing nitrogen-functionalized derivatives of the oxazolidinones is also disclosed.

  公开了一种制备&bgr;-羟基氨基甲酸酯产品的方法。该方法包括在水溶剂和碱的存在下，将至少含有一个碳-碳双键的烯烃化合物与氨基甲酸酯反应，并与一种卤代烷二酮、一种卤代异氰尿酸或一种卤代异氰尿酸的碱金属盐等共氧化剂以及可选的不对称配体反应，形成含有&bgr;-羟基氨基甲酸酯产品的反应混合物。该方法还可选地包括使用额外的碱处理&bgr;-羟基氨基甲酸酯产品，以形成噁唑烷酮。噁唑烷酮可用作手性辅助剂和制药活性物质的中间体，例如α1a肾上腺素受体拮抗剂。公开了一种制备噁唑烷酮的氮功能化衍生物的方法。
• Novel inhibitors of chymase
  申请人：Hawkins Michael J.

  公开号：US20090036409A1

  公开（公告）日：2009-02-05

  The present invention is directed to a compound of formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof, and methods for treating inflammatory and serine protease mediated disorders.

  本发明涉及化合物(I)的配方、制备这些化合物的方法、组合物、中间体和其衍生物，以及治疗炎症和丝氨酸蛋白酶介导的疾病的方法。
• Copper-catalyzed carbonylative multi-component borylamidation of alkenes for synthesizing γ-boryl amides with CO as both methylene and carbonyl sources
  作者：Hui-Qing Geng、Yan-Hua Zhao、Peng Yang、Xiao-Feng Wu

  DOI：10.1039/d4sc00156g

  日期：——

  A multi-component carbonylation reaction is an efficient strategy for the synthesis of valuable carbonyl compounds from simple and readily available substrates. However, there remain challenges in carbonylation reactions where two CO molecules are converted to different groups in the target product. Considering the merit of complex amides, we reported here a copper-catalyzed multi-component borylamidation

  多组分羰基化反应是从简单且易于获得的底物合成有价值的羰基化合物的有效策略。然而，羰基化反应仍然存在挑战，其中两个CO分子转化为目标产物中的不同基团。考虑到复杂酰胺的优点，我们在此报道了用于合成γ-硼基酰胺的铜催化多组分硼酰胺化。该方法可以从烯烃、胺、B 2 pin 2和 CO 中获得多种功能性 γ-硼基酰胺，并且具有良好的产率和优异的非对映异构体比例。值得注意的是，两个 CO 分子转化为目标酰胺中的亚甲基和羰基。一系列胺被成功参与转化，包括芳胺、脂肪胺、脂肪仲胺盐酸盐。
• CAMPTOTHECIN DERIVATIVE, PREPARATION METHOD THEREFOR AND APPLICATION THEREOF
  申请人：MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD.

  公开号：US20220177485A1

  公开（公告）日：2022-06-09

  The present invention is directed to compounds according to Formula I as well as to stereoisomer, tautomer or pharmaceutically acceptable salts of such compounds. The invention also is directed to pharmaceutically acceptable compositions containing such compounds and associated methods for preparing and effect dose in treatment as well as the application in preparing medicine for preventing and/or treating cancers. The invention provides the novel derivatives which introduce methylenedioxy in the position of 10,11 and different groups in the position of 7. The derivatives of novel structure, and the raw materials are easily to obtain. In addition, the compounds in this invention have good cytotoxic activity in vitro and anti-tumor activity in vivo. Therefore, this kind of compounds have broad application foreground. The structure of derivatives are as follows:
• US6372911B1
  申请人：——

  公开号：US6372911B1

  公开（公告）日：2002-04-16