1-Brommethyl-5-methyl-naphthalin | 21674-39-5

• 分子结构分类: 有机化合物 - 苯类化合物 - 萘
• 英文名称: 1-Brommethyl-5-methyl-naphthalin
• 英文别名: 1-(Bromomethyl)-5-methylnaphthalene
• CAS: 21674-39-5
• 化学式: C₁₂H₁₁Br
• 分子量: 235.123
• InChiKey: YECMILBJHVNYLO-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  4.6
• 重原子数：
  13
• 可旋转键数：
  1
• 环数：
  2.0
• sp3杂化的碳原子比例：
  0.17
• 拓扑面积：
  0
• 氢给体数：
  0
• 氢受体数：
  0

反应信息

• 作为反应物：
  描述：

  1-Brommethyl-5-methyl-naphthalin 、 1-氯-6,6-二甲基-2-庚烯-4-炔; 6,6-二甲基-2-烯-4-炔氯代庚烷 在 potassium carbonate 作用下， 以 N,N-二甲基甲酰胺 为溶剂， 以77%的产率得到((E)-6,6-Dimethyl-hept-2-en-4-ynyl)-methyl-(5-methyl-naphthalen-1-ylmethyl)-amine
  参考文献：
  名称：

  Synthesis and structure-activity relationships of naphthalene-substituted derivatives of the allylamine antimycotic terbinafine

  摘要：

  Derivatives of the allylamine antimycotic terbinafine (1) with varied substitution at the naphthalene ring system have been prepared, and their antifungal activity has been evaluated. In general, the potency is strongly dependent on the bulkiness of the substituent. Only hydrogen or in some cases fluorine are tolerated as substituents at positions 2-4 and 6-8 of the naphthalene moiety, whereas 5-substituents may be larger in size (F, Cl, Br, Me). Derivatives with fluorine at positions 3, 5, and 7 or chlorine at position 5 showed enhanced activity against yeasts relative to 1. This increase in sensitivity could be intensified by simultaneous introduction of two fluoro substituents at positions 5 and 7. Compound 7q demonstrated 8-to 16-fold improved potency against Aspergillus fumigatus, Candida albicans, and Candida parapsilosis.

  DOI：

  10.1021/jm00071a011
• 作为产物：
  描述：

  1,5-二甲基萘 在 N-溴代丁二酰亚胺(NBS) 、 过氧化苯甲酰 作用下， 以 四氯化碳 为溶剂， 生成 1-Brommethyl-5-methyl-naphthalin
  参考文献：
  名称：

  Dienol-Benzol-Umlagerung von Penta-2,4-dienyl-benzocyclohexadinolen

  摘要：

  1-羟基-2-甲基-2-（戊-2,4-二烯基）-1,2-二氢萘（2），在乙醚中于0° C用0.75N H 2 SO 4处理，经过[1 s，2 s ]-σ重排，得到2-甲基-1-（戊-2,4-二烯基）-萘（5），参见。方案2。在相同条件下，2-羟基-1-甲基-1-（戊-2,4-二烯基）-1,2-二氢萘（4）产生38％的[1 s，2 s ]产物1-甲基- 2-（戊-2,4-二烯基）萘（6），与26％1-甲基萘，21％1-甲基-4-（戊-2,4-二烯基）萘（7）和1％1-甲基-5-（戊-2,4-二烯基）-萘（8），参见。方案2。后两种萘衍生物很可能至少是分子间过程的产物。

  DOI：

  10.1002/hlca.19730560729

文献信息

• [EN] COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)<br/>[FR] COMPOSÉS SE LIANT À LA PROPROTÉINE CONVERTASE SUBTILISINE/KEXINE DE TYPE 9 (PCSK9)
  申请人：PORTOLA PHARM INC

  公开号：WO2017147328A1

  公开（公告）日：2017-08-31

  The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).

  本公开涉及与PCSK9结合的新化合物、方法和组合物，从而调节PCSK9前蛋白酶酶活性。本公开的化合物包括化合物式（I）。
• COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9 (PCSK9)
  申请人：Portola Pharmaceuticals, Inc.

  公开号：US20190119236A1

  公开（公告）日：2019-04-25

  The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).
• COMPOUNDS FOR BINDING PROPROTEIN CONVERTASE SUBTILISIN/KEXIN TYPE 9
  申请人：SRX Cardio, LLC

  公开号：US20210032214A1

  公开（公告）日：2021-02-04

  The present disclosure relates to novel compounds, methods, and compositions capable of binding to PCSK9, thereby modulating PCSK9 proprotein convertase enzyme activity. The compounds of the disclosure include compounds Formula (I).
• US4152352A
  申请人：——

  公开号：US4152352A

  公开（公告）日：1979-05-01
• US4576809A
  申请人：——

  公开号：US4576809A

  公开（公告）日：1986-03-18