(R)-(+)-6-(4-biphenylyl)methoxy-2-[2-(N, N-dimethylamino)ethyl]tetralin hydrochloride monohydrate | 365276-12-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 苯和取代衍生物
• 英文名称: (R)-(+)-6-(4-biphenylyl)methoxy-2-[2-(N, N-dimethylamino)ethyl]tetralin hydrochloride monohydrate
• 英文别名: (R)-(+)-6-(4-biphenylyl)methoxy-2-[2-(N,N-dimethylamino)ethyl]tetralin hydrochloride monohydrate；6-((1,1'-Biphenyl)-4-ylmethoxy)-1,2,3,4-tetrahydro-N,N'-dimethyl-2-napthaleneethanamine hydrochloride monohydrate, R-；N,N-dimethyl-2-[(2R)-6-[(4-phenylphenyl)methoxy]-1,2,3,4-tetrahydronaphthalen-2-yl]ethanamine;hydrate;hydrochloride
• CAS: 365276-12-6
• 化学式: C₂₇H₃₁NO*ClH*H₂O
• 分子量: 440.025
• InChiKey: VBMPTAUGUUBFJK-FGJQBABTSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.59
• 重原子数：
  31
• 可旋转键数：
  7
• 环数：
  4.0
• sp3杂化的碳原子比例：
  0.33
• 拓扑面积：
  13.5
• 氢给体数：
  2
• 氢受体数：
  3

反应信息

• 作为产物：
  描述：

  (+)-N,N-dimethyl-(6-(4-biphenylyl)methoxy-2-tetralin)acetamide 、 红铝 在 concentrated hydrochloric acid 作用下， 以 sodium hydroxide 、 甲苯 为溶剂， 生成 (R)-(+)-6-(4-biphenylyl)methoxy-2-[2-(N, N-dimethylamino)ethyl]tetralin hydrochloride monohydrate
  参考文献：
  名称：

  Pharmaceutical preparation containing copolyvidone

  摘要：

  一种稳定的制剂，包括：在聚乙二醇含量制剂中的不稳定药物；以及一种包衣剂，其中药物被包衣的是一种共聚维酮而不是聚乙二醇。

  公开号：

  US20040018239A1

文献信息

• Process for producing amine derivatives
  申请人：——

  公开号：US20030139602A1

  公开（公告）日：2003-07-24

  This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein. 1 In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid &bgr; protein can be obtained in high yield.

  本发明提供了一种方便且具有工业优势的过程，用于生产具有抑制淀粉样蛋白β蛋白分泌和积累作用的胺衍生物。在化合物（I）中，选择性地断裂了醚键，而不断裂同一分子中存在的酰胺键，且三级胺没有转化为季铵盐，因此可以高产得到具有抑制淀粉样蛋白β蛋白分泌和积累作用的良好品质的胺衍生物（V）。
• Beta secretase inhibitors
  申请人：Miyamoto Masaomi

  公开号：US20050228020A1

  公开（公告）日：2005-10-13

  An excellent β secretase inhibitor is provided, which comprises a compound of the general formula: wherein Ar is an aromatic group; X is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO 2 —, —NR 8 —, CONR 8 —, —SO 2 NR 8 —, and —COO— (wherein R 8 is hydrogen, etc.), a divalent C 1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups, or a bond; Y is a divalent group selected from —O—, —S—, —CO—, —SO—, —SO 2 —, —NR 8 —, —CONR 8 —, —SO 2 NR 8 —, and —COO—, or a divalent C 1-6 aliphatic hydrocarbon group which may contain one or two of these divalent groups; R 1 and R 2 are hydrogen, a hydrocarbon group, etc., respectively; and A is a ring which may be further substituted, or a salt thereof.

  提供了一种优秀的β-分泌酶抑制剂，其包括一种具有以下通式的化合物：其中Ar为芳香基团；X为二价基团，选自—O—、—S—、—CO—、—SO—、—SO2—、—NR8—、CONR8—、—SO2NR8—和—COO—（其中R8为氢等），一种C1-6链状脂肪基碳氢基团，可以包含其中一种或两种这些二价基团，或一个键；Y为二价基团，选自—O—、—S—、—CO—、—SO—、—SO2—、—NR8—、—CONR8—、—SO2NR8—和—COO—，或一种C1-6链状脂肪基碳氢基团，可以包含其中一种或两种这些二价基团；R1和R2分别为氢、碳氢基团等；A为环，可以进一步取代，或其盐。
• PROCESS FOR PRODUCING AMINE DERIVATIVES
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1270545A1

  公开（公告）日：2003-01-02

  This invention provides a convenient and industrially advantageous process producing amine derivatives having the action of inhibiting the secretion and accumulation of amyloid β protein. In Compound (I), the ether linkage is selectively cleaved without cleaving the amide linkage present in the same molecule and tertiary amines are not converted into quaternary salts, and thus Amine Derivative (V) with good qualities having the action of inhibiting the secretion and accumulation of amyloid β protein can be obtained in high yield.

  本发明提供了一种生产具有抑制淀粉样β蛋白分泌和积聚作用的胺衍生物的方便且具有工业优势的工艺。 在化合物（I）中，醚键被选择性地裂解，而不会裂解存在于同一分子中的酰胺键，叔胺也不会转化为季盐，因此可以高产率地获得具有抑制淀粉样β蛋白分泌和积累作用的优质胺衍生物（V）。
• REMEDIES FOR MILD RECOGNITION DEFLICT
  申请人：Takeda Chemical Industries, Ltd.

  公开号：EP1459764A1

  公开（公告）日：2004-09-22

  It is intended to provide agents for treating mild cognitive impairment which comprise compounds having an effect of inhibiting the production, secretion, aggregation, and/or accumulation of β-amyloid proteins, prodrugs thereof or salts of the same and inhibit the progress of mild cognitive impairment to Alzheimer's disease using the same.

  本发明旨在提供用于治疗轻度认知障碍的制剂，这些制剂包括具有抑制β-淀粉样蛋白的产生、分泌、聚集和/或积聚作用的化合物、其原药或盐，并利用这些制剂抑制轻度认知障碍向阿尔茨海默病的发展。
• PHARMACEUTICAL PREPARATION OF N-[2-(1,6,7,8-TETRAHYDRO-2H-INDENO[5,4 B]FURAN-8-YL)ETHYL]PROPIONAMIDE COATED WITH A COPOLYVIDONE-CONTAINING COATING FREE OF POLYETHYLENE GLYCOL
  申请人：Takeda Pharmaceutical Company Limited

  公开号：EP1334732B1

  公开（公告）日：2010-06-02