(R)-1-(4-(trifluoromethoxy)phenyl)ethan-1-ol | 1567738-33-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯酚醚
• 英文名称: (R)-1-(4-(trifluoromethoxy)phenyl)ethan-1-ol
• 英文别名: (1R)-1-[4-(trifluoromethoxy)phenyl]ethan-1-ol；(1R)-1-[4-(trifluoromethoxy)phenyl]ethanol
• CAS: 1567738-33-3
• 化学式: C₉H₉F₃O₂
• mdl: MFCD18339572
• 分子量: 206.164
• InChiKey: RFESEZYNEIOJHS-ZCFIWIBFSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  2.6
• 重原子数：
  14
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.333
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  5

反应信息

• 作为反应物：
  描述：

  (R)-1-(4-(trifluoromethoxy)phenyl)ethan-1-ol 在 吡啶 、 N,N-二异丙基乙胺 作用下， 以 二氯甲烷 、 乙腈 为溶剂， 反应 0.17h， 生成 (1R)-1-[4-(trifluoromethoxy)phenyl]ethyl 4-[6-(1-methyl-1H-pyrazol-4-yl)pyrazolo[1,5-a]pyridin-3-yl]piperazine-1-carboxylate
  参考文献：
  名称：

  [EN] PLATELET-DERIVED GROWTH FACTOR RECEPTOR (PDGFR) ALPHA INHIBITORS AND USES THEREOF
  [FR] INHIBITEURS DU RÉCEPTEUR DU FACTEUR DE CROISSANCE DÉRIVÉ DES PLAQUETTES (PDGFR) ALPHA ET LEURS UTILISATIONS

  摘要：

  The present disclosure provides compounds that can specifically target a PDGFRα, and thereby, reduce and/or inhibit the activation of the receptor ("PDGFRα inhibitor"). The present disclosure also provides methods of treating a demyelinating disease using the disclosed PDGFRα inhibitors.

  公开号：

  WO2023081923A1
• 作为产物：
  描述：

  4-(三氟甲氧基)苯乙酮 在 C₃₇H₄₀MnN₂O₂P₂⁽¹⁺⁾*Br^(1-) 、 sodium t-butanolate 作用下， 以 异丙醇 为溶剂， 反应 3.0h， 以97%的产率得到(R)-1-(4-(trifluoromethoxy)phenyl)ethan-1-ol
  参考文献：
  名称：

  锰（I）催化的酮的不对称转移加氢：揭示大环特权。

  摘要：

  具有手性（NH）2 P2大环配体（1）的双（羰基）锰（I）配合物[Mn（CO）2（1）] Br（2）催化2-丙醇对极性双键的不对称转移加氢反应作为氢源 酮（43种底物）以高收率（高达> 99％）和出色的对映选择性（90-99％ee）被还原为醇。提出了基于有吸引力的CH-π相互作用的立体化学模型。

  DOI：

  10.1002/anie.201912605

文献信息

• Chiral Frustrated Lewis Pairs Catalyzed Highly Enantioselective Hydrosilylations of Ketones
  作者：Xiaoqin Liu、Qiaotian Wang、Caifang Han、Xiangqing Feng、Haifeng Du

  DOI：10.1002/cjoc.201900121

  日期：2019.7

  A highly enantioselective Piers‐type hydrosilylation of simple ketones was successfully realized using a chiral frustrated Lewis pair of tri‐tert‐butylphosphine and chiral diene‐derived borane as catalyst. A wide range of optically active secondary alcohols were furnished in 80%—99% yields with 81%—97% ee's under mild reaction conditions.

  简单酮的对映体选择性高墩型氢化硅烷化，使用手性路易斯沮丧对三- ，成功地实现叔丁基膦和手性二烯衍生的硼烷作为催化剂。在温和的反应条件下，提供了多种旋光性仲醇，收率为80％-99％，ee为81％-97％。
• Observation of hyperpositive non‐linear effect in catalytic asymmetric organozinc additions to aldehydes
  作者：Yannick Geiger、Thierry Achard、Aline Maisse‐François、Stéphane Bellemin‐Laponnaz

  DOI：10.1002/chir.23271

  日期：2020.10

  an understanding of how chiral amplification is possible, in particular based on non‐linear effects. Interestingly, it has been proposed a quarter century ago that chiral catalysts, when not enantiopure might even be more enantioselective than their enantiopure counterparts. We show here that such hyperpositive non‐linear effect in asymmetric catalysis is indeed possible. An in‐depth study into the underlying

  不对称扩增是一种现象，据信在生活中出现手性方面起着关键作用。在不对称催化中，已经研究了理论和实验模型，以了解如何进行手性扩增，尤其是基于非线性效应。有趣的是，四分之一世纪前有人提出，手性催化剂在不对映纯的情况下甚至可能比对映纯对映体具有更高的对映选择性。我们在这里表明，这种在非对称催化中的超正非线性效应确实是可能的。进行了对潜在机制的深入研究，我们得出的方案与先前提出的模型不同。
• Mn(<scp>i</scp>) phosphine-amino-phosphinites: a highly modular class of pincer complexes for enantioselective transfer hydrogenation of aryl-alkyl ketones
  作者：Harikrishnan Jayaprakash

  DOI：10.1039/d1dt02257a

  日期：——

  A series of Mn(I) catalysts with readily accessible and more π-accepting phosphine-amino-phosphinite (P′(O)N(H)P) pincer ligands have been explored for the asymmetric transfer hydrogenation of aryl-alkyl ketones which led to good to high enantioselectivities (up to 98%) compared to other reported Mn-based catalysts for such reactions. The easy tunability of the chiral backbone and the phosphine moieties

  一系列具有易于获得且更多π接受的膦-氨基-次亚膦酸酯(P'(O)N(H)P)钳配体的Mn( I )催化剂已被探索用于芳基烷基酮的不对称转移氢化，从而导致与其他报道的用于此类反应的锰基催化剂相比，该催化剂具有良好到高的对映选择性（高达 98%）。手性主链和膦部分的简单可调性使 P'(O)N(H)P 成为众所周知的 PNP 型钳子的替代配体框架。
• 6-alkyl dihydropyrazolopyrimidinone compounds as PDE2 inhibitors
  申请人：Merck Sharp & Dohme Corp.

  公开号：US10160762B2

  公开（公告）日：2018-12-25

  The present invention is directed to 6-alkyl dihydropyrazolopyrimidinone compounds of formula (I) which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 2 (PDE2). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis, Parkinson's disease, Parkinson's disease dementia (PDD), or Huntington's disease, and those associated with striatal hypo-function or basal ganglia dysfunction.

  本发明涉及式（I）的6-烷基二氢吡唑嘧啶酮化合物，该化合物可作为治疗剂用于治疗与磷酸二酯酶2（PDE2）相关的中枢神经系统疾病。本发明还涉及使用此类化合物治疗神经和精神疾病，如精神分裂症、精神病、帕金森病、帕金森病痴呆（PDD）或亨廷顿病，以及与纹状体功能低下或基底节功能障碍相关的疾病。
• A Green approach towards the synthesis of chiral alcohols using functionalized alginate immobilized Saccharomyces cerevisiae cells
  作者：Narmada Muthineni、Manikanta Swamy Arnipally、Sridhar Bojja、Harshadas Mitaram Meshram、Ajay Kumar Srivastava、Bhaskar Rao Adari

  DOI：10.1016/j.molcatb.2016.10.016

  日期：2016.12

  The stereochemistry of the drug molecule is gaining greater therapeutic importance and thus much attention was drawn in synthesis of chiral compounds by the pharmaceutical industry. In this study Saccharomyces cerevisiae cells immobilized on functionalized alginate beads, catalyze the bio-reduction of prochiral ketones 1a-12a to their corresponding chiral alcohols 1b-12b in higher yields of 60-99% and.excellent optical purity 75-97%. The synthesized chiral azido alcohols 10b-12b were further subjected to hydrogenation using Palladium(Pd) nanoparticles (<= 5 nm), to obtain chiral amino alcohols 10c-12c of therapeutic importance. Thus, a simple, green and inexpensive continuous chemo-enzymatic process has been developed in the synthesis of chiral alcohols/amino alcohols to enhance the scope of the methodology towards industrial application. (C) 2016 Elsevier B.V. All rights reserved.