(R,R)-2,2'-亚异丙基双(4-异丙基-2-恶唑啉) | 150529-94-5

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 唑啉类
• 中文名称: (R,R)-2,2'-亚异丙基双(4-异丙基-2-恶唑啉)
• 中文别名: (4R,4'R)-2,2'-异丙亚基双(4-异丙基-2-噁唑啉)
• 英文名称: (R,R)-isopropylbisoxazoline
• 英文别名: (R,R)-(+)-2,2'-isopropylidene bis(4-isopropyl-2-oxazoline)；2,2-bis(4S- isopropyl-2-oxazolinyl)propane；2,2-bis-(4R-i-propyl-1,3-oxazolin-2-yl)propane；2,2-Bis[(4R)-4-isopropyl-2-oxazolin-2-yl]propane；(4R)-4-propan-2-yl-2-[2-[(4R)-4-propan-2-yl-4,5-dihydro-1,3-oxazol-2-yl]propan-2-yl]-4,5-dihydro-1,3-oxazole
• CAS: 150529-94-5
• 化学式: C₁₅H₂₆N₂O₂
• 分子量: 266.384
• InChiKey: XFZUPCITFHSROM-RYUDHWBXSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.2
• 重原子数：
  19
• 可旋转键数：
  4
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.87
• 拓扑面积：
  43.2
• 氢给体数：
  0
• 氢受体数：
  4

反应信息

• 作为反应物：
  描述：

  (R,R)-2,2'-亚异丙基双(4-异丙基-2-恶唑啉) 、 copper(II) bis(trifluoromethanesulfonate) 以 二氯甲烷 为溶剂， 反应 3.0h， 生成
  参考文献：
  名称：

  α-亚烷基β-酮亚胺的催化不对称[4 + 2]环加成反应和Hosomi-Sakurai反应

  摘要：

  描述了合理设计的α-亚烷基β-酮酰亚胺的高度对映选择性催化不对称反应。α-亚烷基β-酮酰亚胺的[4 + 2]环加成反应和Hosomi-Sakurai反应以高对映选择性和高收率进行。酰亚胺与各种二烯的[4 + 2]环加成反应提供的产物在环结处带有全碳四元立体异构中心。α-亚烷基β-酮酰亚胺应用于天然产物的对映选择性全合成和其他催化不对称应用。

  DOI：

  10.1021/ol303381c
• 作为试剂：
  描述：

  吲哚 、 亚苯甲基丙二酸二乙酯 在 (R,R)-2,2'-亚异丙基双(4-异丙基-2-恶唑啉) 、 copper(II) bis(trifluoromethanesulfonate) 作用下， 以 乙醇 为溶剂， 反应 16.0h， 以93%的产率得到(R)-ethyl 2-ethoxycarbonyl-3-(3-indolyl)-3-phenyl Propanoate
  参考文献：
  名称：

  The importance of 1:1 and 1:2 metal–ligand species in chiral copper(II)–bis(oxazoline) complexes for catalytic activity

  摘要：

  The rate ratio of different copper(II)-bis(oxazoline) complexes for catalytic activity was assessed in a simple competitive experiment. The cumulated product enantioselectivity derived from a mixture of catalysts with antipodal chiral induction provided sufficient information to determine the relative rates in the asymmetric Friedel-Crafts alkylations of indoles with benzylidene malonates. The discovery of non-linear effects in the reaction system investigated gave insights into the active and resting states of the catalysts. This approach can serve as a tool to screen the activities of different catalysts when detailed kinetic measurements are not suggestive. (C) 2010 Elsevier Ltd. All rights reserved.

  DOI：

  10.1016/j.tetasy.2010.03.030

文献信息

• [EN] ANTIFUNGAL COMPOUNDS AND PROCESSES FOR MAKING<br/>[FR] COMPOSÉS ANTIFONGIQUES ET PROCÉDÉS DE PRÉPARATION
  申请人：VIAMET PHARMACEUTICALS INC

  公开号：WO2017049196A1

  公开（公告）日：2017-03-23

  Provided are polymorphic forms of compound 5 or 5*, or mixtures thereof, and polymorph forms of compound 14 or 14*, or mixtures thereof. Also provided are methods of preparing compound 5 or 5*, or mixtures thereof, and methods of preparing compound of 14 or 14*, or mixtures thereof, which are useful as antifungal agents. In particular, provided is new methodology for preparing polymorphs of the compounds described and substituted derivatives thereof.

  提供了化合物5或5*的多态形式，或二者的混合物，以及化合物14或14*的多形式，或二者的混合物。还提供了制备化合物5或5*，或二者的混合物的方法，以及制备化合物14或14*，或二者的混合物的方法，这些方法可用作抗真菌剂。特别提供了制备所述化合物及其取代衍生物的多形式的新方法。
• NOVEL PROCESSES FOR THE PREPARATION OF PHENYLCYCLOPROPYLAMINE DERIVATIVES AND USE THEREOF FOR PREPARING TICAGRELOR
  申请人：Khile Anil Shahaji

  公开号：US20130165696A1

  公开（公告）日：2013-06-27

  Provided herein are novel processes for the preparation of phenylcyclopropylamine derivatives, which are useful intermediates in the preparation of triazolo[4,5-d]pyrimidine compounds. Provided particularly herein are novel, commercially viable and industrially advantageous processes for the preparation of a substantially pure ticagrelor intermediate, trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine. Provided further herein are novel acid addition salts of trans-(1R,2S)-2-(3,4-difluorophenyl)-cyclopropylamine, and process for their preparation. The intermediate and its acid addition salts are useful for preparing ticagrelor, or a pharmaceutically acceptable salt thereof, in high yield and purity.

  本文提供了一种制备苯基环丙胺衍生物的新型工艺，这些衍生物在三唑并[4,5-d]嘧啶化合物的制备中是有用的中间体。特别提供了一种新颖、商业可行且在工业上具有优势的工艺，用于制备一种基本纯的替卡格雷中间体，即trans-(1R,2S)-2-(3,4-二氟苯基)-环丙胺。此外，本文还提供了trans-(1R,2S)-2-(3,4-二氟苯基)-环丙胺的新型酸加盐，以及其制备工艺。该中间体及其酸加盐对于高产率和纯度制备替卡格雷或其药用可接受盐是有用的。
• Aliphatic C–H hydroxylation activity and durability of a nickel complex catalyst according to the molecular structure of the bis(oxazoline) ligands
  作者：Takashi Izumi、Naki Matsuba、Jun Nakazawa、Shiro Hikichi

  DOI：10.1016/j.mcat.2021.111718

  日期：2021.7

  Applicability of the oxazoline-based compounds, bis(2-oxazolynyl)methane (BOX) and 2,6-bis(2-oxazolynyl)pyridine (PyBOX), as supporting ligands of nickel(II) complexes for the catalysis of aliphatic CH hydroxylation with m-CPBA (meta-chloroperoxybenzoic acid) was explored. Substituent groups at the fourth and fifth positions of oxazoline rings and the bridgehead carbon atom of the BOX derivatives affected

  基于恶唑啉的化合物，双（2-恶唑炔基）甲烷（BOX）和 2,6-双（2-恶唑炔基）吡啶（PyBOX）作为镍（II）配合物的支持配体用于脂肪族 C H催化的适用性羟基化米-CPBA（间氯过氧苯甲酸）进行了探讨。恶唑啉环第四位和第五位的取代基和BOX衍生物的桥头碳原子影响了对环己烷羟基化的催化性能。除完全取代的 BOX 配体配合物外，双氧的存在导致镍配合物的催化性能降低。
• Method for producing optically active chrysanthemic acid
  申请人：SUMITOMO CHEMICAL COMPANY, LIMITED

  公开号：US20020123645A1

  公开（公告）日：2002-09-05

  Disclosed is a method for producing an optically active chrysanthemic acid, which method is characterized by optical resolution of a chrysanthemic acid having a trans isomer ratio of not less than 70% and an optical purity of 2% e.e. to less than 10% e.e. with an optically active organic.

  公开了一种生产光学活性菊酯酸的方法，该方法的特征是利用光学活性有机物对具有不低于70%的顺式异构体比率和2% e.e.至少10% e.e.的光学纯度的菊酯酸进行光学分辨。
• 2'-HYDROXYL-PROTECTED RIBONUCLEOSIDE DERIVATIVE AND MANUFACTURING METHOD OF SAME
  申请人：Kaneka Corporation

  公开号：EP2258709A1

  公开（公告）日：2010-12-08

  The present invention relates to a method for producing a 2'-hydroxy-protected nucleoside derivative by reacting a ribonucleoside with an acylating reagent in the presence of a metal complex consisting of a copper compound and an optically active ligand. By the method according to the present invention, a 2'-hydroxy-protected ribonucleoside derivative, which is an important intermediate for producing an oligonucleoside, can be easily produced with good regioselectivity from a nucleoside derivative of which 2',3'-hydroxy groups are not protected.

  本发明涉及一种通过在铜化合物和光学活性配体组成的金属配合物存在下，将核糖核苷与酰化试剂反应以制备2'-羟基保护核苷衍生物的方法。根据本发明的方法，可以从未保护2'、3'-羟基的核苷衍生物中轻松、有良好的区域选择性地制备重要的2'-羟基保护核糖核苷衍生物，该衍生物是合成寡核苷酸的重要中间体。