1-(2-hydroxyethyl)pyridin-2-one | 64330-83-2

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 吡啶及其衍生物
• 英文名称: 1-(2-hydroxyethyl)pyridin-2-one
• 英文别名: 1-(2-Hydroxyethyl)-1,2-dihydropyridin-2-one
• CAS: 64330-83-2
• 化学式: C₇H₉NO₂
• mdl: MFCD09865472
• 分子量: 139.154
• InChiKey: OSAKOAYGMSTAKA-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  -0.3
• 重原子数：
  10
• 可旋转键数：
  2
• 环数：
  1.0
• sp3杂化的碳原子比例：
  0.285
• 拓扑面积：
  40.5
• 氢给体数：
  1
• 氢受体数：
  2

安全信息

• 海关编码：
  2933399090

反应信息

• 作为反应物：
  描述：

  1-(2-hydroxyethyl)pyridin-2-one 在 三氯氧磷 作用下， 生成 1-(2-氯乙基)-2(1H)-吡啶酮
  参考文献：
  名称：

  Gautier, Comptes Rendus Hebdomadaires des Seances de l'Academie des Sciences, 1941, vol. 212, p. 164

  摘要：

  DOI：
• 作为产物：
  描述：

  2-(2-亚氨基-1(2H)-吡啶基)乙醇 在 sodium hydroxide 、 水 作用下， 生成 1-(2-hydroxyethyl)pyridin-2-one
  参考文献：
  名称：

  Knunjanz, Doklady Akademii Nauk SSSR, 1935, p. I 501;dtsch.Ref.S.505

  摘要：

  DOI：

文献信息

• [EN] ADENOSINE RECEPTOR BINDING COMPOUNDS<br/>[FR] COMPOSÉS SE LIANT AU RÉCEPTEUR DE L'ADÉNOSINE
  申请人：NIKANG THERAPEUTICS INC

  公开号：WO2020014332A1

  公开（公告）日：2020-01-16

  The present invention relates to pharmaceutical compounds and compositions of Formula (I) and methods of treatment using the compounds and compositions, especially for the treatment and/or prevention of a proliferation disorder, such as cancer. Compounds of Formula (I) as further described herein are shown modulators of the adenosine A2A receptor and exhibit antiproliferative activity. Accordingly, these compounds are useful to treat proliferative disorders such as cancer, and other adenosine receptor-related conditions including an inflammatory disease, renal disease, diabetes, vascular disease, lung disease, or an autoimmune disease.

  本发明涉及化学式（I）的药物化合物和组合物，以及使用这些化合物和组合物进行治疗的方法，特别是用于治疗和/或预防增殖性疾病，如癌症。如本文进一步描述的化合物（I）被显示为腺苷A2A受体的调节剂，并表现出抗增殖活性。因此，这些化合物对于治疗增殖性疾病如癌症以及其他与腺苷受体相关的疾病条件包括炎症性疾病、肾脏疾病、糖尿病、血管疾病、肺部疾病或自身免疫疾病是有用的。
• Synthetic Access to New Pyridone Derivatives through the Alkylation Reactions of Hydroxypyridines with Epoxides
  作者：Ahmet Kocak、Sultan Kurbanli、Sait Malkondu

  DOI：10.1080/00397910701569254

  日期：2007.10.1

  oxiranes in good yields, whereas oxypyridine derivatives (5a–d, 9a,b) were obtained from reactions of 3‐hydroxypyridine and 2‐pyridinemethanol with oxiranes. Chlorohydrines (3d, 5d, 7d) were easily converted to corresponding epoxy derivatives (10, 11, 12) in basic medium; then amino alcohols (13–17) were obtained from the reaction of these epoxy derivatives with amines.

  摘要 描述了制备各种吡啶酮和氧吡啶衍生物的一般方法。在不同的路易斯酸作为催化剂的存在下，2-,3-,4-羟基吡啶和2-吡啶甲醇与乙烯-、丙烯-、苯乙烯-氧化物和环氧氯丙烷发生烷基化反应。在 CdI2/BF3·OEt2 存在下获得了 3a 的最佳产率。相应的吡啶酮衍生物 (3a-d, 7a-d) 由 2-和 4-羟基吡啶与环氧乙烷以良好的收率反应获得，而氧吡啶衍生物 (5a-d, 9a,b) 由 3-羟基吡啶和 2-吡啶甲醇与环氧乙烷。氯醇（3d、5d、7d）在碱性介质中很容易转化为相应的环氧衍生物（10、11、12）；然后从这些环氧衍生物与胺的反应中获得氨基醇（13-17）。
• Heterocyclic Compounds For Preventing And Treating Disorders Associated With Excessive Bone Loss
  申请人：Ono Mitsunori

  公开号：US20080058297A1

  公开（公告）日：2008-03-06

  This invention relates to pyrimidine compounds of formula (I), formula (I′), and formula (I″): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R 1 , R 2 , R 3 , R 4 , R 5 , U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).

  本发明涉及式(I)、式(I′)和式(I″)的嘧啶化合物，以及其药学上可接受的盐、溶剂合物、包合物和前药，其中R1、R2、R3、R4、R5、U、V、W、X、Y、Z和n在此处有定义。本发明还涉及包含这些化合物的组合物和使用它们的方法。本发明的化合物和组合物可用于治疗或预防与骨量过度流失相关的疾病，包括但不限于牙周病、非恶性骨疾病（如骨质疏松症、帕格氏骨病、遗传性骨发育不全、纤维性骨发育不良和原发性甲状旁腺功能亢进症）、雌激素缺乏、炎症性骨流失、骨恶性肿瘤、关节炎、骨质增生症以及某些与癌症相关的疾病（如恶性高钙血症、多发性骨髓瘤的溶骨性骨病变和乳腺癌及其他转移癌的溶骨性骨转移）。
• 2-(4-Pyrimidone alkoxyalkyl) dihydropyridine anti-ischaemic and
  申请人：Pfizer Inc.

  公开号：US04568677A1

  公开（公告）日：1986-02-04

  1,4-Dihydropyridine derivatives of the formula: ##STR1## wherein R is aryl or heteroaryl; R.sup.1 and R.sup.2 are each independently C.sub.1 -C.sub.4 alkyl or 2-methoxyethyl; X is a 5 or 6 membered nitrogen-containing heterocyclic ring which is substituted with one or more hydroxyl or oxo groups and which may optionally be fused to a further 5 or 6 membered nitrogen-containing heterocyclic ring, and which may optionally be further substituted in the heterocyclic ring or further fused heterocyclic ring; Y is --(CH.sub.2).sub.n --, --CH.sub.2 CH(CH.sub.3)-- or --CH.sub.2 C(CH.sub.3).sub.2 --; and n is 1 to 3 when X is linked to Y by a ring carbon atom, or 2 or 3 when X is linked to Y by a ring nitrogen atom; and their pharmaceutically acceptable salts, and pharmacuetical preparation containing such compounds, have utility as anti-ischaemic and antihypertensive agents.

  1,4-二氢吡啶衍生物的化学式为：##STR1## 其中R为芳基或杂环芳基；R.sup.1和R.sup.2分别独立为C.sub.1 -C.sub.4烷基或2-甲氧基乙基；X为含氮的5或6成员杂环环，其上取代有一个或多个羟基或氧代基，且可能选择性地与另一个含氮的5或6成员杂环环融合，在杂环环中或进一步融合的杂环环中可能进一步取代；Y为--(CH.sub.2).sub.n --，--CH.sub.2 CH(CH.sub.3)--或--CH.sub.2 C(CH.sub.3).sub.2 --；当X由环碳原子与Y连接时，n为1至3，或当X由环氮原子与Y连接时，n为2或3；它们的药学上可接受的盐，以及含有这些化合物的药物制剂，具有作为抗缺血和降压药物的用途。
• Substituted vinyl pyridine derivative and drugs containing the same
  申请人：SS Pharmaceutical Co., Ltd.

  公开号：US05935977A1

  公开（公告）日：1999-08-10

  The present invention relates to a substituted vinylpyridine derivative represented by the following formula (1): ##STR1## (wherein R.sup.1 represents a hydrogen atom, an alkyl group, etc., R.sup.2 represents an alkyl group; one of R.sup.3 and R.sup.4, which are different from each other, represents a hydrogen atom and the other represents a nitrile group, R.sup.5 represents an aryl group or a heteroaryl group, X represents an oxygen atom, etc., and one of Q.sup.1, Q.sup.2, and Q.sup.3 represents a nitrogen atom and the other two represent CH); a salt of the derivative; and a drug containing the derivative or salt as the active ingredient. Due to strong PDE inhibitory action and TNF-.alpha. production inhibitory action, the derivative, salt, and drug are useful for the prevention and treatment of a wide variety of inflammatory diseases and autoimmune diseases.

  本发明涉及一种代表如下式（1）的取代乙烯基吡啶衍生物：##STR1## （其中，R.sup.1代表氢原子，烷基等，R.sup.2代表烷基;R.sup.3和R.sup.4中的一个代表氢原子，另一个代表腈基，R.sup.5代表芳基或杂环芳基，X代表氧原子等，Q.sup.1、Q.sup.2和Q.sup.3中的两个代表CH，另一个代表氮原子）；该衍生物的盐；以及包含该衍生物或盐作为活性成分的药物。由于该衍生物具有强烈的PDE抑制作用和TNF-α生成抑制作用，因此该衍生物、盐和药物对于预防和治疗各种炎症性疾病和自身免疫性疾病非常有用。