2-chloromethyl-7-(β-trimethyl-silylethoxymethoxy)-naphthalene | 188861-96-3

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 2-chloromethyl-7-(β-trimethyl-silylethoxymethoxy)-naphthalene
• 英文别名: 2-chloromethyl-7-(2-trimethylsilanyl-ethoxymethoxy)-naphthalene；2-[[7-(chloromethyl)naphthalen-2-yl]oxymethoxy]ethyl-trimethylsilane
• CAS: 188861-96-3
• 化学式: C₁₇H₂₃ClO₂Si
• 分子量: 322.907
• InChiKey: HXYBGWGBFDXZOZ-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  5.27
• 重原子数：
  21
• 可旋转键数：
  7
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.41
• 拓扑面积：
  18.5
• 氢给体数：
  0
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  2-chloromethyl-7-(β-trimethyl-silylethoxymethoxy)-naphthalene 在 盐酸 、 sodium hydride 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 反应 1.5h， 生成
  参考文献：
  名称：

  Piperidine-renin inhibitors compounds with improved physicochemical properties

  摘要：

  Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00196-1
• 作为产物：
  描述：

  methyl 7-methoxy-2-naphthoate 在 甲醇 、 四氯化碳 、 lithium aluminium tetrahydride 、 三溴化硼 、 N,N-二异丙基乙胺 、 三苯基膦 作用下， 以 乙醚 、 二氯甲烷 、 乙腈 为溶剂， 反应 12.0h， 生成 2-chloromethyl-7-(β-trimethyl-silylethoxymethoxy)-naphthalene
  参考文献：
  名称：

  Piperidine-renin inhibitors compounds with improved physicochemical properties

  摘要：

  Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets. (C) 1999 Elsevier Science Ltd. All rights reserved.

  DOI：

  10.1016/s0960-894x(99)00196-1

文献信息

• Process and intermediates for preparation of substituted piperidines
  申请人：Hoffmann-La Roche Inc.

  公开号：US06274735B1

  公开（公告）日：2001-08-14

  The present invention concerns intermediates useful in and a process for the preparation of a compound of formula 1 or a salt thereof comprising a) hydroboration of a compound of formula 2 A, R1 and R2 are as herein defined. These compounds are useful in the synthesis of renin inhibitors.

  本发明涉及在制备化合物1或其盐的过程中有用的中间体和方法，包括a) 对化合物2进行氢硼化反应，其中A、R1和R2如本文所定义。这些化合物在合成肾素抑制剂中很有用。
• Methods of treating alzheimer's disease
  申请人：Nieman A. James

  公开号：US20060079533A1

  公开（公告）日：2006-04-13

  Disclosed are methods for treating Alzheimer's disease, and other diseases, and/or inhibiting beta-secretase enzyme, and/or inhibiting deposition of A beta peptide in a mammal, by use of 3,4-disubstituted piperidinyl compounds of formula (I) wherein the variables R 1 , R 2 , R 3 , R 4 , Q, W, X, Z, m, and n are defined herein.

  本发明公开了一种治疗阿尔茨海默病和其他疾病、抑制β-分泌酶酶和/或抑制哺乳动物中A beta肽沉积的方法，使用式(I)的3,4-二取代哌啶基化合物，其中变量R1、R2、R3、R4、Q、W、X、Z、m和n在此定义。
• Piperidine derivatives having renin inhibiting activity
  申请人：Hoffmann-La Roche Inc.

  公开号：US06051712A1

  公开（公告）日：2000-04-18

  Novel piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the novel piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

  本发明涉及新型哌啶衍生物的制备和用作药物。本发明涉及一般式I的新型哌啶衍生物，其中R.sup.1，R.sup.2，R.sup.3，R.sup.4，Q，X，Z，m和n如本文所述。
• Piperidine derivative having renin inhibiting activity
  申请人：Hoffmann-La Roche Inc.

  公开号：US06150526A1

  公开（公告）日：2000-11-21

  Piperidine derivatives, their manufacture and use as medicaments, are disclosed. The invention is concerned with the piperidine derivatives of general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, Q, X, Z, m and n are as described herein.

  本发明涉及哌啶衍生物的制备和用作药物。该发明涉及一般式I的哌啶衍生物，其中R.sup.1，R.sup.2，R.sup.3，R.sup.4，Q，X，Z，m和n如本文所述。
• Piperidine-renin inhibitors compounds with improved physicochemical properties
  作者：Rolf Güller、Alfred Binggeli、Volker Breu、Daniel Bur、Walter Fischli、Georges Hirth、Christian Jenny、Manfred Kansy、François Montavon、Marcel Müller、Christian Oefner、Heinz Stadler、Eric Vieira、Maurice Wilhelm、Wolfgang Wostl、Hans Peter Märki

  DOI：10.1016/s0960-894x(99)00196-1

  日期：1999.5

  Piperidine renin inhibitors with heterocyclic core modifications or hydrophilic attachments show improved physical properties (lower lipophilicity, improved solubility). Tetrahydroquinoline derivative rac-30 with a molecular weight of 517 and a log D(pH 7.4) of 1.9 displays potent and long lasting blood pressure lowering effects after oral administration to sodium depleted conscious marmosets. (C) 1999 Elsevier Science Ltd. All rights reserved.