6-(2-Piperidin-4-ylethyl)spiro[[1,3]dioxolo[4,5-f]isoindole-7,1'-cyclopropane]-5-one

• 分子结构分类: 有机化合物 - 有机杂环化合物 - 异吲哚及其衍生物
• 英文名称: 6-(2-Piperidin-4-ylethyl)spiro[[1,3]dioxolo[4,5-f]isoindole-7,1'-cyclopropane]-5-one
• 英文别名: 6-(2-piperidin-4-ylethyl)spiro[[1,3]dioxolo[4,5-f]isoindole-7,1'-cyclopropane]-5-one
• 化学式: C₁₈H₂₂N₂O₃
• 分子量: 314.4
• InChiKey: HHVJIQBBOZBJPS-UHFFFAOYSA-N

计算性质

• 辛醇/水分配系数(LogP)：
  1.8
• 重原子数：
  23
• 可旋转键数：
  3
• 环数：
  5.0
• sp3杂化的碳原子比例：
  0.61
• 拓扑面积：
  50.8
• 氢给体数：
  1
• 氢受体数：
  4

文献信息

• Process for preparing AD-35
  申请人：Zhejiang Hisun Pharmaceutical Co., Ltd.

  公开号：US10399992B2

  公开（公告）日：2019-09-03

  Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.

  本发明公开了一种制备式（I）所示苯并二恶茂衍生物（AD-35）及其中间体的方法。本发明的方法包括：以哌啶酸为原料，进行溴化、酯化、氰化、环丙烷内酰胺化、酰胺氮烷基化、脱保护、哌啶氮烷基化和盐析，得到式（I）化合物。该方法起始原料便宜易得，合成路线短，操作简单，适合工业化生产。
• [EN] BENZODIOXOLE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF<br/>[FR] DÉRIVÉ DE BENZODIOXOLE ET SON PROCÉDÉ DE PRÉPARATION ET SON UTILISATION
  申请人：ZHEJIANG HISUN PHARM CO LTD

  公开号：WO2014005421A1

  公开（公告）日：2014-01-09

  本发明提供一类新的苯并间二氧杂环戊烯衍生物以及这类化合物的制备方法。这类由式（I）所表示的化合物或其药学上可接受的盐具有乙酰胆碱酯酶抑制活性，可以用于治疗或者预防阿尔茨海默氏症（Alzheimer's disease）。式（I）中的R1、R2和A的定义见说明书。
• BENZODIOXOLE DERIVATIVE AND PREPARATION METHOD AND USE THEREOF
  申请人：Zhejiang Hisun Pharmaceutical Co. Ltd.

  公开号：EP2871184B1

  公开（公告）日：2017-09-06
• Process For Preparing AD-35
  申请人：Zhejiang Hisun Pharmaceutical Co., Ltd.

  公开号：US20190100527A1

  公开（公告）日：2019-04-04

  Disclosed are a method for preparing a benzodioxole derivative (AD-35) shown by Formula (I) and an intermediate thereof. The method of the present invention involves: using piperic acid as a raw material; and performing bromination, esterification, cyanidation, cyclopropane lactamization, amide nitrogen alkylation, deprotection, piperidine nitrogen alkylation and salification to obtain the compound of Formula (I). The method has cheap and easily available start raw materials, short synthesis routes and simple operation, and is suitable for industrial production.
• US9346818B2
  申请人：——

  公开号：US9346818B2

  公开（公告）日：2016-05-24