2-Acetamido-7-methoxy-3,4-dihydronaphthalen-1(2H)-one | 2471-73-0

• 分子结构分类: 有机化合物 - 苯类化合物 - 四氢化萘
• 英文名称: 2-Acetamido-7-methoxy-3,4-dihydronaphthalen-1(2H)-one
• 英文别名: 2-acetamido-7-methoxy-1-tetralone；2-Acetamino-7-methoxy-tetralon-(1)；N-(7-methoxy-1-oxo-3,4-dihydro-2H-naphthalen-2-yl)acetamide
• CAS: 2471-73-0
• 化学式: C₁₃H₁₅NO₃
• 分子量: 233.267
• InChiKey: ROYBTGIGSTVEAD-UHFFFAOYSA-N

物化性质

• 熔点：
  133 °C
• 沸点：
  481.0±45.0 °C(Predicted)
• 密度：
  1.20±0.1 g/cm3(Predicted)

计算性质

• 辛醇/水分配系数(LogP)：
  1.4
• 重原子数：
  17
• 可旋转键数：
  2
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.38
• 拓扑面积：
  55.4
• 氢给体数：
  1
• 氢受体数：
  3

反应信息

• 作为反应物：
  描述：

  2-Acetamido-7-methoxy-3,4-dihydronaphthalen-1(2H)-one 在 sodium tetrahydroborate 、 lithium aluminium tetrahydride 作用下， 以 四氢呋喃 、 乙醇 、 甲醚 、 乙二醇 为溶剂， 反应 1.0h， 生成
  参考文献：
  名称：

  Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists

  摘要：

  A series of tricyclic oxazines, namely, the 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, have been synthesized and assayed for dopamine agonist activity. One of the members of this series, compound (+)VII-15, was found to be a remarkably potent agonist in vivo when tested in the standard 6-hydroxydopamine lesioned rat assay. The absolute configuration of the compound corresponds to that found in the active isomer of apomorphine. Its activity at the alpha 2 receptor (vs. [3H]clonidine) is relatively low. It also failed to stimulate the synthesis of cAMP in the carp retina assay, thus giving the compound a highly selective profile in favor of the D2 receptor.

  DOI：

  10.1021/jm00378a014
• 作为产物：
  描述：

  7-甲氧基-1-萘满酮 在 palladium on activated charcoal potassium tert-butylate 、 氢气 、 亚硝酸异戊酯 作用下， 以 四氢呋喃 、 乙醚 、 正丁醇 为溶剂， 反应 4.0h， 生成 2-Acetamido-7-methoxy-3,4-dihydronaphthalen-1(2H)-one
  参考文献：
  名称：

  Synthesis of 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, a new class of dopamine agonists

  摘要：

  A series of tricyclic oxazines, namely, the 4-substituted 2H-naphth[1,2-b]-1,4-oxazines, have been synthesized and assayed for dopamine agonist activity. One of the members of this series, compound (+)VII-15, was found to be a remarkably potent agonist in vivo when tested in the standard 6-hydroxydopamine lesioned rat assay. The absolute configuration of the compound corresponds to that found in the active isomer of apomorphine. Its activity at the alpha 2 receptor (vs. [3H]clonidine) is relatively low. It also failed to stimulate the synthesis of cAMP in the carp retina assay, thus giving the compound a highly selective profile in favor of the D2 receptor.

  DOI：

  10.1021/jm00378a014

文献信息

• Carbapenem derivatives containing a bicyclic substituent, process for their preparation, and their use
  申请人：ZENECA LIMITED

  公开号：EP0695753A1

  公开（公告）日：1996-02-07

  The present invention relates to carbapenems and provides a compound of the formula (I) wherein R¹is hydroxymethyl, 1-hydroxyethyl or 1-fluoroethyl; Ris hydrogen or C₁₋₄alkyl; X¹is oxygen or sulphur; and Ais of the formula which is optionally substituted on either ring and wherein B is of the formula -CH₂-C(=O)-(CH₂)n-, -C(=O)-(CH₂)n1-, -C(=O)-CH=CH-X-, -C(=O)CH₂CH₂X-, -(CH₂)nC(=0)NH- or -CH=CHC(=O)NH- wherein n is 1 or 2, n¹ is 2 or 3 and X is NH, 0 or S; and a pharmaceutically acceptable salt or an in vivo hydrolysable ester thereof, processes for their preparation, intermediates in their preparation, their use as therapeutic agents and pharmaceutical compositions containing them.

  本发明涉及碳青霉烯，并提供式（I）的化合物，其中R¹是羟甲基，1-羟乙基或1-氟乙基；R是氢或C₁₋₄烷基；X¹是氧或硫；以及A是式的选配取代环上的化合物，其中B是式-CH₂-C（=O）-（CH₂）n-，-C（=O）-（CH₂）n1-，-C（=O）-CH=CH-X-，-C（=O）CH₂CH₂X-，-（CH₂）nC（=0）NH-或-CH=CHC（=O）NH-，其中n为1或2，n¹为2或3，X为NH，0或S；以及其药学上可接受的盐或体内可水解的酯，它们的制备过程，制备中间体，它们作为治疗剂的用途以及含有它们的制药组合物。
• Hexahydronaphth[1,2-b]-1,4-oxazines
  申请人：Merck & Co., Inc.

  公开号：US04420480A1

  公开（公告）日：1983-12-13

  Hexahydronaphth[1,2-b]-1,4-oxazines have dopaminergic activity and display .alpha..sub.2 -adrenergic receptor antagonism. They are useful in the treatment of parkinsonism, depression and hypertension. An important method of preparation is by ring closure of the appropriate 2-chloroacetamidotetrahydronaphthalen-1-ol and reduction of the resulting cyclic amide carbonyl group.

  六氢萘并[1,2-b]-1,4-噁唑具有多巴胺能活性，并表现出.alpha..sub.2-肾上腺素受体拮抗作用。它们在帕金森病、抑郁症和高血压的治疗中很有用。一种重要的制备方法是通过环合成适当的2-氯乙酰胺四氢萘酚-1-醇，并还原所得的环状酰胺羰基团。
• Hexahydronaphth(1,2-b)-1,4-oxazines, process for their preparation and pharmaceutical formulation containing them
  申请人：Merck & Co., Inc.

  公开号：EP0080115A2

  公开（公告）日：1983-06-01

  Hexahydronaphth[1,2-b]-1,4-oxazines have dopaminergic activity and display α2-adrenergic receptor antagonism. They are useful in the treatment of parkinsonism, depression and hypertension. An important method of preparation is by ring closure of the appropriate 2-chloroacetamido- tetrahydronaphthalen-1-ol and reduction of the resulting cyclic amide carbonyl group.

  六氢萘并[1,2-b]-1,4-噁嗪具有多巴胺能活性，并显示出α2-肾上腺素能受体拮抗作用。 它们可用于治疗帕金森病、抑郁症和高血压。 一种重要的制备方法是将适当的 2-氯乙酰胺基四氢萘-1-醇闭环，并还原由此产生的环状酰胺羰基。
• JONES, J. H.;ANDERSON, P. S.;BALDWIN, J. J.;CLINESCHMIDT, B. V.;MCCLURE, +, J. MED. CHEM., 1985, 27, N 12, 1607-1613
  作者：JONES, J. H.、ANDERSON, P. S.、BALDWIN, J. J.、CLINESCHMIDT, B. V.、MCCLURE, +

  DOI：——

  日期：——
• US4420480A
  申请人：——

  公开号：US4420480A

  公开（公告）日：1983-12-13