7-氨基-1,8-萘啶-2,4-二醇 | 76541-91-8

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 二氮杂萘
• 中文名称: 7-氨基-1,8-萘啶-2,4-二醇
• 英文名称: 7-amino-1,8-naphthyridine-2,4-diol
• 英文别名: 2-amino-5,7-dihydroxy-1,8-naphthyridine；7-amino-4-hydroxy-1H-1,8-naphthyridin-2-one
• CAS: 76541-91-8
• 化学式: C₈H₇N₃O₂
• 分子量: 177.162
• InChiKey: YKWBJEGNZIUWLI-UHFFFAOYSA-N

物化性质

• 熔点：
  278-280 °C(Solv: ethanol (64-17-5))
• 沸点：
  363.1±52.0 °C(Predicted)
• 密度：
  1.68±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  -0.4
• 重原子数：
  13
• 可旋转键数：
  0
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.0
• 拓扑面积：
  88.2
• 氢给体数：
  3
• 氢受体数：
  4

安全信息

• 海关编码：
  2933990090

反应信息

• 作为反应物：
  描述：

  7-氨基-1,8-萘啶-2,4-二醇 在 三氯氧磷 作用下， 反应 3.5h， 生成 7-acetamido-2,4-dichloro-1,8-naphthyridine
  参考文献：
  名称：

  Synthesis of 1,8-naphthyridine derivatives: Potential antihypertensive agents — Part VII

  摘要：

  A series of 2-(carbethoxypiperazinyl)- and 2-piperazinyl-1,8-naphthyridine derivatives, variously substituted, have been synthesized and pharmacologically investigated for their antihypertensive activity. Some of them exhibited a significant and prolonged decrease of the mean arterial pressure (MAP) on spontaneously hypertensive rats. For this series of compounds, on the basis of the pharmacological results obtained, no structure-activity relationship can be deduced at this time. Moreover, the most active and representative compounds 11b, 12a and 16b were investigated by means of in vitro pharmacological functional studies and in vivo, as diuretic agents, to determine a possible mechanism of the antihypertensive activity, which is unknown for the moment. (C) Elsevier, Paris.

  DOI：

  10.1016/s0223-5234(98)80014-7
• 作为产物：
  描述：

  2,6-二氨基吡啶 、 丙二酸二乙酯 在 磷酸 作用下， 以 二苯醚 为溶剂， 以92.40 %的产率得到7-氨基-1,8-萘啶-2,4-二醇
  参考文献：
  名称：

  2-(IMIDAZO[1, 2-A]1,8-NAPHTHYRIDIN-8-YL)-1,3,4-OXADIAZOLE DERIVATIVES AS ENHANCERS OF INNATE IMMUNE RESPONSE FOR THE TREATMENT OF VIRAL INFECTIONS

  摘要：

  本发明涉及式 (I) 的 2-(咪唑并[l,2-a]l,8-萘啶-8-基)-l,3,4-噁二唑衍生物，可作为先天免疫反应的增强剂用于治疗病毒感染。

  公开号：

  WO2023244672A1

文献信息

• [EN] COMPOUNDS AND METHODS FOR INHIBITING mTOR<br/>[FR] COMPOSÉS ET PROCÉDÉS D'INHIBITION DE MTOR
  申请人：3-V BIOSCIENCES INC

  公开号：WO2017031427A1

  公开（公告）日：2017-02-23

  Compounds having activity as mTOR inhibitors are disclosed. The compounds have the following structure (I) including stereoisomers, pharmaceutically acceptable salts and prodrugs thereof, wherein R1, R2, R3, R4, and A are as defined herein. Methods associated with preparation and use of such compounds, as well as pharmaceutical compositions comprising such compounds, are also disclosed.

  揭示了具有作为 mTOR 抑制剂活性的化合物。这些化合物具有以下结构（I），包括立体异构体、药用可接受的盐和前药，其中 R1、R2、R3、R4 和 A 如本文所定义。还公开了与制备和使用这些化合物相关的方法，以及包含这些化合物的药物组合物。
• Substituted 1,8-naphthyridines, their preparation and their use as
  申请人：BASF Aktiengesellschaft

  公开号：US05258356A1

  公开（公告）日：1993-11-02

  A combination of a variety of herbicides with safening agents which are substituted 1,8-naphthyridines of the formula ##STR1## where R.sup.1 is mercapto, hydroxyl, halogen, benzylthio, amino or NR.sup.2 R.sup.3, where R.sup.2 is a group ##STR2## where A is C.sub.1 -C.sub.8 -alkyl, R.sup.3 is hydrogen, XR.sup.4, where X is oxygen or sulfur and R.sup.4 is C.sub.1 -C.sub.12 -alkyl, R.sup.5 and R.sup.7 are each hydrogen, C.sub.1 -C.sub.12 -alkyl, hydroxyl, halogen, mercapto, C.sub.1 -C.sub.4 -alkoxy, C.sub.1 -C.sub.4 -alkylthio, dialkylamino where each alkyl is of 1 to 6 carbon atoms, phenoxy or phenylthio, halo-(C.sub.1 -C.sub.3)-alkyl, C.sub.1 -C.sub.4 -alkoxy-(C.sub.1 -C.sub.3)-alkyl, and R.sup.6 is hydrogen, C.sub.1 -C.sub.12 -alkyl, carboxyl or C.sub.1 -C.sub.4 -alkoxycarbonyl or the plant-tolerated salts thereof.

  一种多种除草剂与安全剂的组合，其中所述安全剂是公式##STR1##中的取代1,8-萘啶的衍生物，其中R.sup.1为巯基，羟基，卤素，苄硫基，氨基或NR.sup.2R.sup.3，其中R.sup.2为##STR2##的基团，其中A为C.sub.1-C.sub.8-烷基，R.sup.3为氢，XR.sup.4，其中X为氧或硫，R.sup.4为C.sub.1-C.sub.12-烷基，R.sup.5和R.sup.7分别为氢，C.sub.1-C.sub.12-烷基，羟基，卤素，巯基，C.sub.1-C.sub.4-烷氧基，C.sub.1-C.sub.4-烷硫基，二烷基氨基，其中每个烷基为1至6个碳原子，苯氧基或苯硫基，卤代（C.sub.1-C.sub.3）-烷基，C.sub.1-C.sub.4-烷氧基-（C.sub.1-C.sub.3）-烷基，R.sup.6为氢，C.sub.1-C.sub.12-烷基，羧基或C.sub.1-C.sub.4-烷氧羰基或其植物耐受的盐。
• Azaquinolone dye lasers
  申请人：The United States of America as represented by the United States

  公开号：US04103257A1

  公开（公告）日：1978-07-25

  A dye laser comprising a laser dye solution of a compound having the general structure: ##STR1## wherein at least one of the 5, 6 and 8 ring positions is occupied by a nitrogen atom in lieu of the corresponding CR group and X is OH, alkoxy, or amino including amino substituted by at least one of the following: alkyl, aryl, acyl, aracyl, a group which taken together with the nitrogen atom of the amino group forms a heterocyclic ring, or part of one or two 5 or 6 membered aliphatic heterocyclic rings attached to ring A at positions 6 or 8 or both depending on where the N in ring A is located. R.sub.1, R.sub.3, R.sub.4, R.sub.5, R.sub.6 and R.sub.8 are hydrogen or other groups as defined below. The compounds lase in the blue to near ultraviolet region.

  一种染料激光器，包括具有以下一般结构的激光染料溶液：##STR1## 其中5、6和8环位置中的至少一个由氮原子代替相应的CR基团，并且X为OH、烷氧基或氨基，包括被至少以下物质取代的氨基：烷基、芳基、酰基、芳酰基、与氨基团的氮原子一起形成杂环环的基团，或附加在环A的6或8位置或两个位置上的5或6成员的脂环杂环，具体取决于环A中的N位于何处。R.sub.1、R.sub.3、R.sub.4、R.sub.5、R.sub.6和R.sub.8为氢或以下定义的其他基团。这些化合物在蓝色到近紫外区域内激光。
• 2-(IMIDAZO[1, 2-A]1,8-NAPHTHYRIDIN-8-YL)-1,3,4-OXADIAZOLE DERIVATIVES AS ENHANCERS OF INNATE IMMUNE RESPONSE FOR THE TREATMENT OF VIRAL INFECTIONS
  申请人：ASSEMBLY BIOSCIENCES, INC.

  公开号：WO2023244672A1

  公开（公告）日：2023-12-21

  The present invention relates to 2-(imidazo[l,2-a]l,8-naphthyridin-8- yl)-l,3,4-oxadiazole derivatives of formula (I) as enhancers of innate immune response for the treatment of viral infections

  本发明涉及式 (I) 的 2-(咪唑并[l,2-a]l,8-萘啶-8-基)-l,3,4-噁二唑衍生物，可作为先天免疫反应的增强剂用于治疗病毒感染。
• CYCLIZATION OF 2-AMINOPYRIDINE DERIVATIVES. II. THE REACTION OF SUBSTITUTED 2-AMINOPYRIDINES WITH ETHYL MALONATE¹
  作者：GERALD R. LAPPIN、QUENTIN R. PETERSEN、CARLTON E. WHEELER

  DOI：10.1021/jo01148a023

  日期：1950.3