N-tert-butoxycarbonyl-2-hydroxypyrrolidine | 347189-17-7

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡咯烷类
• 英文名称: N-tert-butoxycarbonyl-2-hydroxypyrrolidine
• 英文别名: (R)-tert-butyl 2-hydroxypyrrolidine-1-carboxylate；(3R)-hydroxypyrrolidine-1-carboxylic acid tert-butyl ester；N-tert-butyloxycarbonyl-(R)-(-)-pyrrolidinol；tert-butyl (2R)-2-hydroxypyrrolidine-1-carboxylate
• CAS: 347189-17-7
• 化学式: C₉H₁₇NO₃
• 分子量: 187.239
• InChiKey: NUYWPLSBEHXOHO-SSDOTTSWSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.6
• 重原子数：
  13
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.89
• 拓扑面积：
  49.8
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  N-tert-butoxycarbonyl-2-hydroxypyrrolidine 在 二乙胺基三氟化硫 作用下， 以 二氯甲烷 为溶剂， 反应 1.17h， 以26%的产率得到(3S)-fluoropyrrolidine-1-carboxylic acid tert-butyl ester
  参考文献：
  名称：

  PYRAZOLE DERIVATIVES

  摘要：

  由式(I)表示的化合物： （其中Ar1代表可能具有1到3个取代基的苯基，或者是非取代的5-或6-成员芳香杂环基团；Ar2代表（i）非取代的苯基团，（ii）已被1到3个来自羰胺基、氨基、羟基、低烷氧基和卤原子的群或原子取代的较低烷基基团取代的苯基团，或者（iii）已被1到3个来自低烷基基团、低炔基基团、低烷酰基团、羰胺基、氰基、氨基、羟基、低烷氧基和卤原子的群或原子取代的5-或6-成员含氮芳香杂环基团；X代表由式(II)表示的基团： （其中环结构表示可能具有除了式(II)中显示的氮原子之外，从氮、氧和硫中选择的一个杂原子的4-到7-成员杂环基团，并且可能被1到4个来自低烷基基团、羰胺基、氨基、羟基、低烷氧基、氧基、低烷酰基团、低烷基磺酰基团和卤原子的群或原子取代）），其盐，该化合物或其盐的溶剂化合物，以及药物。

  公开号：

  EP1762568A1
• 作为产物：
  描述：

  BOC-L-脯氨酸 在 ammonium cerium(IV) nitrate 、 水 作用下， 以 乙腈 为溶剂， 反应 0.5h， 以65%的产率得到N-tert-butoxycarbonyl-2-hydroxypyrrolidine
  参考文献：
  名称：

  Cerium ammonium nitrate (CAN) for mild and efficient reagent to remove hydroxyethyl units from 2-hydroxyethyl ethers and 2-hydroxyethyl amines

  摘要：

  Cerium ammonium nitrate (CAN) removed hydroxyethyl units from 2-hydroxyethyl ethers and 2-hydroxyethyl amines to produce alcohols and amines in good yields. Especially, removal of the 2-hydroxyethyl ethers from C-2-symmetric diols, chiral 2,3-butanediol and chiral hydrobenzoin, was very useful for asymmetric syntheses using C-2-symmetric diols. The reactions using dual abilities of CAN, i.e., the ability for removal of the 2-hydroxyethyl unit and the ability for acetal hydrolysis by a single electron transfer, were also achieved Successfully. The reaction conditions were very mild and efficient, and many functional groups, which can be affected under normal conditions, were unaffected during the reaction. (c) 2006 Published by Elsevier Ltd.

  DOI：

  10.1016/j.tet.2006.11.004

文献信息

• Naphthostyrils
  申请人：——

  公开号：US20020147343A1

  公开（公告）日：2002-10-10

  Disclosed are novel naphthostyrils of formula 1 These compounds inhibit cyclin-dependent kinases (CDKs), in particular CDK2. These compounds and their pharmaceutically acceptable salts and esters are anti-proliferative agents useful in the treatment or control of cell proliferative disorders, in particular cancer. Also disclosed are pharmaceutical compositions containing such compounds, methods for the treatment and/or prevention of cancer using such compositions, and intermediates useful in the preparation of the compounds of formula I.

  本发明涉及一种新型萘基苯基丙酮类化合物，其化学式为1。这些化合物抑制细胞周期依赖性激酶（CDKs），尤其是CDK2。这些化合物及其药学上可接受的盐和酯是抗增殖剂，可用于治疗或控制细胞增殖性疾病，尤其是癌症。本发明还涉及含有这些化合物的制药组合物，使用这些组合物治疗和/或预防癌症的方法，以及制备式I化合物的中间体。
• [EN] SYNTHETIC MIMETICS OF HOST DEFENSE AND USES THEREOF<br/>[FR] MIMÉTIQUE SYNTHÉTIQUE DE DÉFENSE D'HÔTE ET SON UTILISATION
  申请人：POLYMEDIX INC

  公开号：WO2010062573A1

  公开（公告）日：2010-06-03

  The present invention provides arylamide compounds and methods of making and using them as antibiotics.

  本发明提供了芳基酰胺化合物及其制备和用作抗生素的方法。
• Compounds Having Activity at Nk3 Receptor and Uses Thereof in Medicine
  申请人：Smith Paul William

  公开号：US20080261945A1

  公开（公告）日：2008-10-23

  The present invention relates to compounds of formula (I), a pharmaceutically acceptable salt, solvate or prodrug thereof: wherein R 1 is phenyl optionally substituted by 1, 2 or 3 halogen atoms which halogen atoms may be the same or different; R 2 is C 1-6 alkyl, C 3-6 cycloalkyl or acetyl; X is oxygen or sulphur; a is 1, 2 or 3; b is 0 or 1; c is 0, 1 or 2; R 3 is hydrogen or C 1-6 alkyl; R 4 is hydrogen, C 1-6 alkyl, haloC 1-6 alkyl, C 1-4 alkoxyC 1-6 alkyl, C 3-6 cycloalkyl or C 3-6 cycloalkylC 1-6 alkyl; R 5 is hydrogen; or R 5 and R 3 , together with the interconnecting atoms, form a 4, 5 or 6 membered ring; R 6 is phenyl or thienyl, either of which is optionally substituted by 1, 2 or 3 halogen atoms, which atoms may be the same or different; and z is 0, 1 or 2; wherein when z is 1 or 2, Z is a halogen atom, and wherein when z is 2 the halogen atoms may be the same or different. Also disclosed are processes for their preparation, pharmaceutical compositions containing them and their use as medicaments particularly in treating disorders of the Central Nervous System (CNS).

  本发明涉及公式(I)的化合物，其可接受的药物盐、溶剂化物或前药：其中，R1是苯基，可选地被1、2或3个卤素原子取代，所述卤素原子可以相同或不同；R2是C1-6烷基、C3-6环烷基或乙酰基；X是氧或硫；a为1、2或3；b为0或1；c为0、1或2；R3是氢或C1-6烷基；R4是氢、C1-6烷基、卤代C1-6烷基、C1-4烷氧基C1-6烷基、C3-6环烷基或C3-6环烷基C1-6烷基；R5是氢；或R5和R3与相互连接的原子一起形成4、5或6元环；R6是苯基或噻吩基，其中任一种均可选择性地被1、2或3个卤素原子取代，所述原子可以相同或不同；z为0、1或2；当z为1或2时，Z为卤素原子，当z为2时，所述卤素原子可以相同或不同。还公开了它们的制备方法、含有它们的药物组合物以及它们作为药物的用途，特别是用于治疗中枢神经系统(CNS)疾病。
• RAF KINASE MODULATOR COMPOUNDS AND METHODS OF USE THEREOF
  申请人：Abraham Sunny

  公开号：US20110118245A1

  公开（公告）日：2011-05-19

  Compounds according to formula (I), compositions and methods are provided for modulating the activity of RAF kinases, including BRAF kinase and for the treatment, prevention, or amelioration of one or more symptoms of disease or disorder mediated by RAF kinases. Formula (I): or a pharmaceutically acceptable salt, solvate, clathrate of hydrate thereof, wherein X is O or S(O) t ; R a is O or S.

  提供了按照公式(I)的化合物、组合物和方法，用于调节RAF激酶的活性，包括BRAF激酶，并用于治疗、预防或缓解由RAF激酶介导的一种或多种疾病或障碍的症状。公式(I)：或其药学上可接受的盐、溶剂化合物、包合物或水合物，其中X为O或S(O)t；R为O或S。
• Red light-induced highly efficient aerobic oxidation of organoboron compounds using spinach as a photocatalyst
  作者：Peng Yan、Rong Zeng、Bo Bao、Xiu-Ming Yang、Lei Zhu、Bin Pan、Sheng-Li Niu、Xiao-Wei Qi、Yu-Long Li、Qin Ouyang

  DOI：10.1039/d2gc03055a

  日期：——

  A simple and general red light-induced oxidation of organoboron compounds to obtain hydroxyl has been developed with spinach as the photocatalyst in alcohol. This mild protocol shows broad substrate scope and provides a wide range of aliphatic alcohols and phenols in moderate to excellent yields. Notably, the robustness of this method is suitable for B(OH)2, Bpin, Bneo and BF3K substrates that respond

  已经开发了一种简单且通用的红光诱导有机硼化合物氧化以获得羟基，菠菜作为醇中的光催化剂。这种温和的协议显示了广泛的底物范围，并以中等至优异的产量提供了广泛的脂肪醇和酚。值得注意的是，该方法的稳健性适用于 B(OH) 2、Bpin、Bneo 和 BF 3对不同光（包括红色、蓝色和阳光）作出反应的 K 底物。更大规模的实验和绿色化学指标分析证明，这是一种稳健且绿色的方法，甚至可以仅使用厨房设备和配料进行。进一步的机理研究表明，该反应可能涉及由光诱导电子转移过程产生的超氧阴离子自由基。