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1. WO2017177816 - PROCESS FOR PREPARING AD-35

Publication Number WO/2017/177816
Publication Date 19.10.2017
International Application No. PCT/CN2017/078389
International Filing Date 28.03.2017
IPC
C07D 491/056 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
056with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 491/113 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
113with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
CPC
A61P 25/28
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
25Drugs for disorders of the nervous system
28for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
C07D 491/056
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
056with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
C07D 491/113
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
10Spiro-condensed systems
113with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
Y02P 20/55
YSECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
20Technologies relating to chemical industry
50Improvements relating to the production of bulk chemicals
55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Applicants
  • 浙江海正药业股份有限公司 ZHEJIANG HISUN PHARMACEUTICAL CO., LTD. [CN]/[CN]
Inventors
  • 钟金清 ZHONG, Jinqing
  • 赵旭阳 ZHAO, Xuyang
  • 白骅 BAI, Hua
  • 龚永祥 GONG, Yongxiang
  • 张鑫龙 ZHANG, Xinlong
  • 朱齐凤 ZHU, Qifeng
  • 刘伟伟 LIU, Weiwei
  • 周亚 ZHOU, Ya
Agents
  • 北京邦信阳专利商标代理有限公司 BOSS&YOUNG PATENT AND TRADEMARK LAW OFFICE
Priority Data
201610221284.611.04.2016CN
Publication Language Chinese (ZH)
Filing Language Chinese (ZH)
Designated States
Title
(EN) PROCESS FOR PREPARING AD-35
(FR) PROCÉDÉ DE PRÉPARATION DE AD-35
(ZH) 制备AD-35的工艺
Abstract
(EN)
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.
(FR)
La présente invention concerne un procédé de préparation d'un dérivé de benzodioxole (AD-35) représenté par la formule (I) et un intermédiaire de ce dernier. Le procédé de la présente invention consiste : à utiliser de l'acide pipérique en tant que matière première; et à effectuer une bromation, une estérification, une cyanuration, une lactamisation de cyclopropane, une alkylation de l'azote amide, une déprotection, une alkylation de l'azote de pipéridine et une salification de manière à obtenir le composé de formule (I). Le procédé comporte des matières premières de départ bon marché et facilement disponibles, des voies de synthèse courtes et un fonctionnement simple, et se prête à une production industrielle.
(ZH)
本发明公开了一种式(I)所示的苯并间二氧杂环戊烯衍生物(AD-35)的制备方法及其中间体。本发明方法以胡椒酸为原料,经过溴代、酯化、氰化、环丙烷内酰胺化、酰胺氮烷基化、脱保护、哌啶氮烷基化和成盐,得到式(I)化合物。该方法起始原料廉价易得,合成路线短,操作简单,可适合工业化生产。
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