2-Methoxy-naphthoesaeure-(1)-amid | 876483-32-8

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 2-Methoxy-naphthoesaeure-(1)-amid
• 英文别名: 2-methoxy-[1]naphthoic acid amide；2-Methoxy-[1]naphthoesaeure-amid；2-Methoxy-1-naphthamide；2-methoxynaphthalene-1-carboxamide
• CAS: 876483-32-8
• 化学式: C₁₂H₁₁NO₂
• 分子量: 201.225
• InChiKey: GZWGJJRNCLYUIL-UHFFFAOYSA-N

物化性质

• 熔点：
  189 °C
• 沸点：
  398.0±25.0 °C(Predicted)
• 密度：
  1.210±0.06 g/cm3(Temp: 20 °C; Press: 760 Torr)(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  2
• 重原子数：
  15
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.08
• 拓扑面积：
  52.3
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-Methoxy-naphthoesaeure-(1)-amid 在 1,2-diaminoethane dihydrochloride 作用下， 生成 2-(2-methoxy-[1]naphthyl)-4,5-dihydro-1H-imidazole
  参考文献：
  名称：

  DE687196

  摘要：

  公开号：
• 作为产物：
  描述：

  2-Methoxy-naphthoyl-(1)-cyanid 在 ammonium hydroxide 作用下， 以 1,4-二氧六环 为溶剂， 生成 2-Methoxy-naphthoesaeure-(1)-amid
  参考文献：
  名称：

  Achmatowicz,O.; Achmatowicz,O., Roczniki Chemii, 1961, vol. 35, p. 813 - 820

  摘要：

  DOI：

文献信息

• Compounds and Methods for Catalytic Directed ortho Substitution of Aromatic Amides and Esters
  申请人：Zhao Yigang

  公开号：US20120302752A1

  公开（公告）日：2012-11-29

  Methods are described for efficient and regioselective reactions that are Ru-catalyzed and either (i) amide-directed C—H, C—N, C—O activation/C—C bond forming reactions, (ii) ester-directed C—O and C—N activation/C—C bond forming reactions, or (iii) amide-directed C—O activation/hydrodemethoxylation reactions. All of these reactions of directed C—H, C—N, C—O activation/coupling reactions establish a catalytic base-free DoM-cross coupling process at non-cryogenic temperature. High regioselectivity, yields, operational simplicity, low cost, and convenient scale-up make these reactions suitable for industrial applications. Many previously unknown amide-substituted or ester-substituted aryl and heteroaryl compounds are presented with synthetic details also provided.

  描述了一种高效和区域选择性反应的方法，这些反应是以钌为催化剂的，可以是（i）酰胺导向的C—H、C—N、C—O活化/C—C键形成反应，（ii）酯导向的C—O和C—N活化/C—C键形成反应，或者（iii）酰胺导向的C—O活化/脱甲氧基反应。所有这些导向C—H、C—N、C—O活化/偶联反应在非低温下建立了一个无催化剂碱的DoM-交叉偶联过程。高区域选择性、产率、操作简便、低成本和便于放大规模使得这些反应适用于工业应用。还提供了许多以前未知的酰胺取代或酯取代的芳基和杂环芳基化合物，同时提供了合成细节。
• Nuclear receptor binding agents
  申请人：Dalton T. James

  公开号：US20070265296A1

  公开（公告）日：2007-11-15

  The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

  本发明涉及一种新型选择性雌激素受体调节剂（SERMs）类。该SERM化合物适用于预防和/或治疗各种疾病和情况，包括预防和治疗癌症，如前列腺癌和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管运动症状，神经系统疾病，心血管疾病和肥胖症。
• NUCLEAR RECEPTOR BINDING AGENTS
  申请人：DALTON James T.

  公开号：US20120157539A1

  公开（公告）日：2012-06-21

  The present invention relates to a novel class of selective estrogen receptor modulators (SERMs). The SERM compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including prevention and treatment of cancers such as prostate and breast cancer, osteoporosis, hormone-related diseases, hot flashes or vasomotor symptoms, neurological disorders, cardiovascular disease and obesity.

  本发明涉及一种新型选择性雌激素受体调节剂（SERMs）类。这些SERM化合物适用于预防和/或治疗各种疾病和病况，包括预防和治疗癌症，如前列腺癌和乳腺癌，骨质疏松症，激素相关疾病，潮热或血管运动症状，神经疾病，心血管疾病和肥胖症。
• ESTROGEN RECEPTOR LIGANDS AND METHODS OF USE THEREOF
  申请人：GTx, Inc.

  公开号：US20160031797A1

  公开（公告）日：2016-02-04

  The present invention relates to a novel class of nuclear receptor binding agents (NRBAs). The NRBA compounds are applicable for use in the prevention and/or treatment of a variety of diseases and conditions including, inter alia, prevention and treatment of hormone-related diseases, cancers, inflammation, osteoporosis, peripheral vascular disease, reducing circulating lipid levels, and cardiovascular disease.

  本发明涉及一种新型的核受体结合剂（NRBAs）。NRBA化合物可用于预防和/或治疗各种疾病和病症，包括但不限于预防和治疗激素相关疾病、癌症、炎症、骨质疏松症、外周血管疾病、降低循环脂质水平和心血管疾病。
• Process for the preparation of 2-thio penem derivatives and intermediates therefor
  申请人：BEECHAM GROUP PLC

  公开号：EP0046363A1

  公开（公告）日：1982-02-24

  The present invention provides a process for the preparation of a compound of the formula (IV): or salt or ester thereof wherein R1 and R2 are independently hydrogen; an organic radical bonded via a carbon atom to the ring carbon atom; a free, etherified or esterified hydroxy or mercapto group; an amino or acylamino group; or together R1 and R2 represent a group = CR5R6 wherein R5 and R6 are the same or different and each represent hydrogen or a hydrocarbon or heterocyclic group optionally substituted with a functional group; and R3 represents an organic radical; which process comprises reacting a compound of the formula (V): wherein Rx is hydrogen or a blocking group and R4 is an organic radical; with a thiol or reactive derivative thereof. The compounds of the formula (IV) are useful as antibiotics and [β-lactamase inhibitors, as are the compounds of the formula (V). This invention also provides the novel compounds of the formula (V) and certain novel compounds within formula (IV). Their preparation and use are described.

  本发明提供了一种制备式(IV)化合物或其盐或酯的工艺： 或其盐或酯 其中 R1 和 R2 独立地为氢；通过碳原子与环碳原子键合的有机基；游离的、醚化的或酯化的羟基或巯基；氨基或酰氨基；或 R1 和 R2 共同代表一个基团＝CR5R6 其中 R5 和 R6 相同或不同，且各自代表氢或任选被官能团取代的烃基或杂环基；以及 R3 代表有机基；该工艺包括使式(V)： 其中 Rx 是氢或封端基团，R4 是有机基团；与硫醇或其反应衍生物反应。式（IV）化合物可用作抗生素和[β-内酰胺酶抑制剂]，式（V）化合物也可用作抗生素和[β-内酰胺酶抑制剂]。本发明还提供了新型的式 (V) 化合物和某些新型的式 (IV) 化合物。对它们的制备和用途进行了描述。