4-Chlor-1-(1-naphthyloxy)-2-butanol | 59747-97-6

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 4-Chlor-1-(1-naphthyloxy)-2-butanol
• 英文别名: 4-Chloro-1-(naphthyloxy)-2-butanol；4-chloro-1-naphthalen-1-yloxybutan-2-ol
• CAS: 59747-97-6
• 化学式: C₁₄H₁₅ClO₂
• 分子量: 250.725
• InChiKey: IWNOYNQILKRDHU-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  3.6
• 重原子数：
  17
• 可旋转键数：
  5
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.29
• 拓扑面积：
  29.5
• 氢给体数：
  1
• 氢受体数：
  2

反应信息

• 作为反应物：
  描述：

  4-Chlor-1-(1-naphthyloxy)-2-butanol 生成 4-Isopropylamino-1-(1-naphthyloxy)-2-butanol Hydrochloride
  参考文献：
  名称：

  LUNSFORD, C. D.;CHEN, YING-HO

  摘要：

  DOI：
• 作为产物：
  描述：

  1,4-二氯-2-丁醇 、 萘酚 在 sodium hydroxide 作用下， 生成 4-Chlor-1-(1-naphthyloxy)-2-butanol
  参考文献：
  名称：

  The synthesis and antiallergy activity of 1-(aryloxy)-4-(4-arylpiperazinyl)-2-butanol derivatives

  摘要：

  A series of 1-(aryloxy)-4-(4-arylpiperazinyl)-2-butanol derivatives were prepared and evaluated for antiallergy activity in the passive foot anaphylaxis (PFA) assay in rats. Twenty-seven derivatives had activity equal to or greater than the parent, alpha-(phenoxymethyl)-4-phenyl-1-piperazinepropanol. Six derivatives that possessed greater activity in the PFA than the parent compound were then tested in the guinea pig anaphylaxis (GPA) assay. Five of the derivatives were more potent than the parent (PD50 = 40 mg/kg) in the GPA with alpha-[(4-fluorophenoxy)methyl]-4-(4-fluorophenyl)-1-piperazinepropan ol (PD50 = 3 mg/kg) having the greatest potency.

  DOI：

  10.1021/jm00168a044

文献信息

• 1-Aryloxy-4-amino-2-butanols
  申请人：A. H. Robins Company, Inc.

  公开号：US04463190A1

  公开（公告）日：1984-07-31

  Novel 1-aryloxy-4-amino-2-butanols of the formula ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2 wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen form a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.

  公开了一种化合物及其药物学上可接受的酸加成盐，其化学式为ArO-CH2-CHOH-CH2-CH2-NR1R2，其中Ar为1-萘基，2-萘基，4-或5-吲哚基，3-或5-氯-2-吡啶基，苯基，单取代苯基或双取代苯基，R1为较低烷基，苯基，苯基烷基，2-羟甲基-2-丙基，金刚烷基或较低环烷基，R2为氢或较低烷基，其中R1和R2与相邻的氮一起形成杂环残基，具有局部麻醉，β-肾上腺素受体阻滞，降压和抗心律失常作用。该化合物通过将新型1-芳氧基-4-氯-2-丁醇与胺反应制备而成。还公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。
• 1-aryloxy-4-amino-2-butanols
  申请人：A. H. Robins Company, Incorporated

  公开号：US04806555A1

  公开（公告）日：1989-02-21

  Novel 1-aryloxy-4-amino-2-butanols of the formula ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2 wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen from a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.

  化合物的名称为Novel 1-aryloxy-4-amino-2-butanols，化学式为ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2，其中Ar可以是1-萘基、2-萘基、茚-4（或5-）基、3-（或5-）氯基-2-吡啶基、苯基、单取代苯基或二取代苯基，R.sup.1可以是较低的烷基、苯基、苯基烷基、2-羟甲基-2-丙基、金刚烷基或较低的环烷基，R.sup.2可以是氢或较低的烷基。这些化合物与相邻氮原子组成杂环残基，并且它们的药物可接受的酸盐具有局部麻醉、β-肾上腺素受体阻滞、降压和抗心律失常的性质。这些化合物是通过将新型的1-芳氧基-4-氯-2-丁醇与胺反应制备而成的。此外，还公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。
• Certain aryloxy-4-chloro-2-butanol intermediates
  申请人：A. H. Robins Company, Inc.

  公开号：US04609735A1

  公开（公告）日：1986-09-02

  Novel 1-aryloxy-4-amino-2-butanols of the formula ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2 wherein AR is 1-naphythyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen form a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.

  公开了化学式为ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2的新型1-芳氧基-4-氨基-2-丁醇，其中AR是1-萘基、2-萘基、茚-4（或5-）基、3-（或5-）氯-2-吡啶基、苯基、单取代苯基或双取代苯基，R.sup.1是较低的烷基、苯基、苯基烷基、2-羟甲基-2-丙基、金刚烷基或较低的环烷基，R.sup.2是氢或较低的烷基，其中R.sup.1和R.sup.2与相邻的氮一起形成杂环残基，其药物可接受的酸盐具有局部麻醉、β-肾上腺素受体阻滞、降压和抗心律失常的性质。该化合物是通过将新型的1-芳氧基-4-氯-2-丁醇与胺反应制备而成。公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。
• 1-Aryloxy-4-amino-2-butanols and the pharmaceutical use thereof
  申请人：A. H. Robins Company, Inc.

  公开号：US04379167A1

  公开（公告）日：1983-04-05

  Novel 1-aryloxy-4-amino-2-butanols of the formula ArO--CH.sub.2 --CHOH--CH.sub.2 --CH.sub.2 --NR.sup.1 R.sup.2 wherein Ar is 1-naphthyl, 2-naphthyl, indene-4(or 5-)yl, 3-(or 5-)chloro-2-pyridyl, phenyl, monosubstituted phenyl or di-substituted phenyl, R.sup.1 is lower alkyl, phenyl, phenylalkyl, 2-hydroxymethyl-2-propyl, adamantyl or lower-cycloalkyl, R.sup.2 is hydrogen or lower alkyl, wherein R.sup.1 and R.sup.2 together with the adjacent nitrogen form a heterocyclic residue and the pharmaceutically acceptable acid addition salts thereof having local anesthetic, beta-adrenergic blocking, antihypertensive and antiarrhythmic properties are disclosed. The compounds are prepared by reacting novel 1-aryloxy-4-chloro-2-butanols with amines. Methods for the preparation of the novel 1-aryloxy-4-chloro-2-butanol intermediates are also disclosed.

  公开了一种新型的化合物及其药物可接受的酸盐，其化学式为ArO-CH2-CHOH-CH2-CH2-NR1R2，其中Ar为1-萘基，2-萘基，吲哚-4（或5-）基，3-（或5-）氯-2-吡啶基，苯基，单取代苯基或双取代苯基，R1为低碳基，苯基，苯基烷基，2-羟甲基-2-丙基，金刚烷基或低环烷基，R2为氢或低碳基，其中R1和R2与相邻的氮一起形成杂环残基。该化合物具有局部麻醉，β-肾上腺素阻滞，降压和抗心律失常性质。该化合物是通过将新型的1-芳氧基-4-氯-2-丁醇与胺反应制备而成。还公开了制备新型1-芳氧基-4-氯-2-丁醇中间体的方法。
• CH612907
  申请人：——

  公开号：——

  公开（公告）日：——