3-羟基-4-甲氧基吡啶 | 153199-54-3

• 物质功能分类: 医药中间体 - 杂环化合物 - 吡啶类化合物
• 分子结构分类: 有机化合物 - 有机氧化合物
• 中文名称: 3-羟基-4-甲氧基吡啶
• 中文别名: 4-甲氧基-3-羟基吡啶
• 英文名称: 3-hydroxy-4-methoxypyridine
• 英文别名: (3R,4R)-3-hydroxy-4-methoxypyridine；4-Methoxypyridin-3-ol
• CAS: 153199-54-3
• 化学式: C₆H₇NO₂
• mdl: MFCD11044354
• 分子量: 125.127
• InChiKey: JHKBAGPVKNQUOC-UHFFFAOYSA-N

物化性质

• 沸点：
  326.1±22.0 °C(Predicted)
• 密度：
  1.190±0.06 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  0.5
• 重原子数：
  9
• 可旋转键数：
  1
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.166
• 拓扑面积：
  42.4
• 氢给体数：
  1
• 氢受体数：
  3

安全信息

• 危险等级：
  IRRITANT
• 海关编码：
  2933399090
• 危险性防范说明：
  P264,P270,P301+P312+P330,P501
• 危险性描述：
  H302
• 储存条件：
  室温

反应信息

• 作为反应物：
  描述：

  3-羟基-4-甲氧基吡啶 在 吡啶 、 仲丁基锂 、 苯基锂 作用下， 以 四氢呋喃 、 乙醚 、 环己烷 为溶剂， 反应 25.5h， 生成 N,N-diisopropyl-4-methoxy-2,2'-(5-D)bipyridine-3-carbamate
  参考文献：
  名称：

  First Synthesis of Caerulomycin B. A New Synthesis of Caerulomycin C

  摘要：

  Caerulomycins produced by Streptomyces caeruleus are bipyridinic molecules endowed with antibiotic properties. The first synthesis of caerulomycin B (1) as well as a new synthesis of caerulomycin C (2) are reported. Starting from 3-hydroxypyridine, the same methodology was used to prepare both compounds 1 and 2. Efficiently controlled reactions such as metalation to allow the synthesis of 2,6-diiodo-3,4-dialkoxypyridines, which are key intermediates, and further halogen lithium exchange and cross-coupling to reach the targets molecules 1 and 2 have been developed.

  DOI：

  10.1021/jo010913r
• 作为产物：
  描述：

  4-甲氧基吡啶-N-氧化物 在 palladium on activated charcoal 过氧乙酸 、 硼酸三甲酯 、 氢气 、 苯基锂 作用下， 生成 3-羟基-4-甲氧基吡啶
  参考文献：
  名称：

  Total synthesis of the antifungal dilactones UK-2A and UK-3A: The determination of their relative and absolute configurations, analog synthesis and antifungal activities

  摘要：

  The synthesis of the antifungal dilactones, UK-2A and UK-3A, is described. In addition to providing a workable synthetic route to these potent antifungal antibiotics, this has allowed us to determine the assignment of the relative and absolute configurations in the nine-membered ring. Furthermore, UK-2A analogs were also synthesized and evaluated their antifungal activities and cytotoxic activities along with UK-2A, (2R, 3R, 4S, 7R)-UK-2A, UK-3A, (2R, 3R, 4S, 7R)-UK-3A, and antimycin A. The structural requirements for the selective cytotoxicity against yeasts and filamentous fungi will also be suggested. (C) 1998 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0040-4020(98)00777-7

文献信息

• Process for producing stereoisomer of pyrrolidine derivative
  申请人：——

  公开号：US20030004208A1

  公开（公告）日：2003-01-02

  The present invention provides a process for producing optically active 3-hydroxy-4-methoxypyrrolidine, which is an intermediate for synthesizing a quinuclidine derivative useful as a squalene synthetase inhibitor, a salt thereof, or a hydrate thereof by subjecting a pyrrolidine derivative represented by the following formula (1-4): 1 wherein R 3a and R 3b are different and each of R 3a and R 3b represents a hydrogen atom or a methyl group, to optical division purification by using an optically active dibenzoyltartaric acid derivative or the like.

  本发明提供了一种用于生产光学活性的3-羟基-4-甲氧基吡咯烷的方法，这是一种合成作为角鲨烯合酶抑制剂有用的喹努啉衍生物的中间体，其盐类，或者其水合物，通过使用光学活性的二苯甲酰酒石酸衍生物等，对以下式子(1-4)所表示的吡咯烷衍生物进行光学分离纯化： 1 式中，R 3a 和R 3b 不同，R 3a 和R 3b 各自代表一个氢原子或甲基基团。
• [EN] SUBSTITUTED ISOXAZOLE AMIDE COMPOUNDS AS INHIBITORS OF STEAROYL-COA DESATURASE 1 (SCD1)<br/>[FR] COMPOSÉS D'AMIDE D'ISOXAZOLE SUBSTITUÉS EN TANT QU'INHIBITEURS DE STÉAROYL-COA DÉSATURASE 1 (SCD1)
  申请人：HOFFMANN LA ROCHE

  公开号：WO2014086704A1

  公开（公告）日：2014-06-12

  The invention is concerned with a compound of formula (I) and pharmaceutically acceptable salts thereof. In addition, the present invention relates to methods of manufacturing and using the compound of formula (I) as well as pharmaceutical compositions containing such compounds. The compound of formula (I) are SCD1 inhibitors and may be useful in treating cancer.

  该发明涉及一种具有化学式(I)及其药学上可接受的盐的化合物。此外，本发明涉及制造和使用化学式(I)化合物的方法，以及含有这种化合物的药物组合物。化学式(I)的化合物是SCD1抑制剂，可能在治疗癌症方面有用。
• A concise approach towards the synthesis of WS75624 A and WS75624 B via the cross-metathesis of vinyl-functionalized thiazoles
  作者：Jyotirmayee Dash、Bruno Melillo、Stellios Arseniyadis、Janine Cossy

  DOI：10.1016/j.tetlet.2011.01.027

  日期：2011.4

  converting enzyme (ECE) inhibitors and potential antihypertensive agents, is reported featuring a key cross-metathesis between a vinyl-functionalized thiazole and a terminal olefin. As the two natural products only differ by the nature of their hydroxyalkyl side-chain, our convergent strategy enable the synthesis of key intermediates of both molecules in a limited amount of steps.

  据报道，合成方法是针对WS75624 A和WS75624 B的前体，两种有效的内皮素转化酶（ECE）抑制剂和潜在的降压药，其在乙烯基官能化的噻唑和末端烯烃之间具有关键的交叉复分解。由于两种天然产物的区别仅在于其羟烷基侧链的性质，因此我们的聚合策略可在有限的步骤中合成两种分子的关键中间体。
• Indole, azaindole and related heterocyclic amidopiperazine derivatives
  申请人：——

  公开号：US20030096825A1

  公开（公告）日：2003-05-22

  This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with amido piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.

  本发明提供具有药物和生物影响性质的化合物，它们的制药组合物和使用方法。具体而言，本发明涉及酰胺哌嗪衍生物。这些化合物具有独特的抗病毒活性，无论是单独使用还是与其他抗病毒药物、抗感染药物、免疫调节剂或HIV进入抑制剂联合使用。更具体地，本发明涉及治疗HIV和艾滋病。
• ANTIVIRAL AGENT
  申请人：SHIONOGI & CO., LTD.

  公开号：US20150202208A1

  公开（公告）日：2015-07-23

  The present invention provides an integrase inhibitor. The inventors have found the following compound of formula (I) possessing an integrase inhibitory activity. (wherein, R C and R D taken together with the neighboring carbon atoms form a ring which may be a condensed ring, Y is hydroxyl, mercapto or amino; Z is O, S or NH; R A is a group shown by (wherein, C ring is N-containing aromatic heterocycle) or the like).

  本发明提供了一种整合酶抑制剂。发明人发现以下式(I)的化合物具有整合酶抑制活性。（其中，RC和RD与相邻的碳原子一起形成一个环，该环可以是一个缩合环，Y是羟基，巯基或氨基; Z是O，S或NH; RA是由（其中，C环是含N的芳香杂环）或类似物所示的基团）。