NI201200177A - Intermedios de agomelatina y método de preparación de estos - Google Patents

Intermedios de agomelatina y método de preparación de estos

Info

Publication number
NI201200177A
NI201200177A NI201200177A NI201200177A NI201200177A NI 201200177 A NI201200177 A NI 201200177A NI 201200177 A NI201200177 A NI 201200177A NI 201200177 A NI201200177 A NI 201200177A NI 201200177 A NI201200177 A NI 201200177A
Authority
NI
Nicaragua
Prior art keywords
intermediates
agomelatine
preparation
yield
present
Prior art date
Application number
NI201200177A
Other languages
English (en)
Inventor
Zhang Peng
Huang Yu
Yuan Zhedong
Shan Hanbin
Yu Xiong
Original Assignee
Servier Lab
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45097542&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=NI201200177(A) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Servier Lab filed Critical Servier Lab
Publication of NI201200177A publication Critical patent/NI201200177A/es

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/06Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/16Amides, e.g. hydroxamic acids
    • A61K31/165Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/06Antimigraine agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/20Hypnotics; Sedatives
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/22Anxiolytics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/12Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/18Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of an acyclic saturated carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00Carboxylic acid amides
    • C07C233/01Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms
    • C07C233/17Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom
    • C07C233/22Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by singly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by an acyclic carbon atom having the carbon atom of the carboxamide group bound to an acyclic carbon atom of a carbon skeleton containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00Systems containing two condensed rings
    • C07C2602/02Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Anesthesiology (AREA)
  • Epidemiology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Inorganic Compounds Of Heavy Metals (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Battery Electrode And Active Subsutance (AREA)

Abstract

La presente invención se refiere a los compuestos intermedios para la preparación de agomelatina, así como a los métodos de preparación de éstos. El intermedio de la presente invención para la preparación de agomelatina es el compuesto A como se muestra en la fórmula siguiente. También se proporcionan dos compuestos intermedios nuevos. Cuando se usan estos compuestos intermedios nuevos para preparar agomelatina, es sencillo de manipular, bien controlado y con alta pureza, sin operaciones complicadas tales como rectificación y separación por cromatografía en columna, y adecuado para la producción industrial. Por otro lado, los métodos de preparación de los dos intermedios nuevos en sí mismo son sencillos y con alto rendimiento, usando sólo la usada muy comúnmente 7 - metoxi - tetralona como material de partida original y que experimenta una etapa de reacción para obtener los intermedios, seguido de una etapa más para convertir los compuesto intermedios en el producto deseado agomelatina. Dichos procesos de reacción están muy simplificados, mejorándose el rendimiento de la reacción y superando la dificultad de purificación del método previo, comparado con la técnica anterior para la preparación de agomelatina. Típicamente, el rendimiento de la presente invención es mayor del 70%.
NI201200177A 2010-06-08 2012-11-30 Intermedios de agomelatina y método de preparación de estos NI201200177A (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CN2010101973700A CN102276492B (zh) 2010-06-08 2010-06-08 阿戈美拉汀中间体及其制备方法

Publications (1)

Publication Number Publication Date
NI201200177A true NI201200177A (es) 2013-02-06

Family

ID=45097542

Family Applications (1)

Application Number Title Priority Date Filing Date
NI201200177A NI201200177A (es) 2010-06-08 2012-11-30 Intermedios de agomelatina y método de preparación de estos

Country Status (40)

Country Link
US (1) US8779199B2 (es)
EP (1) EP2580189B1 (es)
JP (1) JP5519863B2 (es)
KR (1) KR101470874B1 (es)
CN (1) CN102276492B (es)
AP (1) AP3205A (es)
AU (1) AU2011264206B2 (es)
BR (1) BR112012031086B1 (es)
CA (1) CA2801822C (es)
CL (1) CL2012003371A1 (es)
CR (1) CR20120592A (es)
CU (1) CU24148B1 (es)
CY (1) CY1119857T1 (es)
DK (1) DK2580189T3 (es)
EA (1) EA020271B1 (es)
EC (1) ECSP12012328A (es)
ES (1) ES2656968T3 (es)
GE (1) GEP20156234B (es)
GT (1) GT201200328A (es)
HR (1) HRP20171751T1 (es)
HU (1) HUE035850T2 (es)
IL (1) IL223180A (es)
LT (1) LT2580189T (es)
MA (1) MA34292B1 (es)
ME (1) ME02992B (es)
MX (1) MX2012013870A (es)
MY (1) MY160954A (es)
NI (1) NI201200177A (es)
NO (1) NO2580189T3 (es)
NZ (1) NZ604081A (es)
PE (1) PE20130252A1 (es)
PL (1) PL2580189T3 (es)
PT (1) PT2580189T (es)
RS (1) RS56659B1 (es)
SG (1) SG185667A1 (es)
SI (1) SI2580189T1 (es)
TN (1) TN2012000542A1 (es)
UA (1) UA104684C2 (es)
WO (1) WO2011153939A1 (es)
ZA (1) ZA201208764B (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012046253A2 (en) * 2010-10-08 2012-04-12 Msn Laboratories Limited Process for the preparation of n-[2- (7-methoxy-l-naphthyl) ethyl] acetamide and its novel crystalline forms
CN102452951B (zh) * 2010-10-25 2014-02-19 天津泰普药品科技发展有限公司 阿戈美拉汀及其药物组合物
ITMI20121444A1 (it) 2012-08-27 2014-02-28 Procos Spa Processo per la produzione di agomelatine
EP2921473B1 (en) * 2012-10-09 2017-09-27 Jiangxi Synergy Pharmaceutical Co. Ltd. 1-cyan-1-(7-methoxyl-1-naphtyl) methanol ester compound and preparation method and use thereof
CN112574066A (zh) * 2019-09-27 2021-03-30 江苏豪森药业集团有限公司 一种阿戈美拉汀中间体的制备方法
WO2021130057A1 (en) * 2019-12-23 2021-07-01 Dsm Ip Assets B.V. Dehydrogenation process

Family Cites Families (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2658818B1 (fr) * 1990-02-27 1993-12-31 Adir Cie Nouveaux derives a structure naphtalenique, leur procede de preparation et les compositions pharmaceutiques qui les contiennent.
DE10229842A1 (de) 2002-07-03 2004-02-05 Helmut Prof. Dr. Schmidhammer Morphinanderivate und deren quartäre Ammoniumsalze substituiert in Position 14, Herstellungsverfahren und Verwendung
FR2866335B1 (fr) 2004-02-13 2006-05-26 Servier Lab Nouveau procede de synthese de l'agomelatine
FR2866334B1 (fr) * 2004-02-13 2006-05-26 Servier Lab Nouveau procede de synthese du (7-methoxy-1-naphtyl) acetonitrile et application a la synthese de l'agomelatine
FR2866336B1 (fr) * 2004-02-13 2006-03-24 Servier Lab Nouveau procede de synthese du (7-methoxy-3,4-dihydro-1-naphtalenyl) acetonitrile et application a la synthese de l'agomelatine
WO2007147771A2 (en) * 2006-06-20 2007-12-27 F. Hoffmann-La Roche Ag Tetralin and indane derivatives and uses thereof
CN101486665B (zh) * 2009-03-03 2013-04-17 上海医药工业研究院 阿戈美拉汀中间体2-(7-甲氧基-1-萘基)乙酰胺的制备方法
WO2012093402A1 (en) * 2011-01-04 2012-07-12 Symed Labs Limited Processes for the preparation of n-[2-(7-methoxy-1-naphthyl)ethyl]acetamide

Also Published As

Publication number Publication date
CN102276492A (zh) 2011-12-14
GT201200328A (es) 2014-06-09
MX2012013870A (es) 2013-01-24
AU2011264206B2 (en) 2013-08-15
JP5519863B2 (ja) 2014-06-11
NO2580189T3 (es) 2018-03-24
PT2580189T (pt) 2017-12-06
US20130267738A1 (en) 2013-10-10
TN2012000542A1 (en) 2014-04-01
GEP20156234B (en) 2015-01-26
PL2580189T3 (pl) 2018-04-30
BR112012031086B1 (pt) 2020-12-08
ECSP12012328A (es) 2012-12-28
CN102276492B (zh) 2013-04-10
EP2580189A1 (en) 2013-04-17
ZA201208764B (en) 2014-01-29
ME02992B (me) 2018-10-20
DK2580189T3 (da) 2018-01-29
ES2656968T3 (es) 2018-03-01
JP2013531639A (ja) 2013-08-08
EP2580189B1 (en) 2017-10-25
UA104684C2 (ru) 2014-02-25
SG185667A1 (en) 2012-12-28
US8779199B2 (en) 2014-07-15
MY160954A (en) 2017-03-31
RS56659B1 (sr) 2018-03-30
KR101470874B1 (ko) 2014-12-09
IL223180A (en) 2014-06-30
WO2011153939A1 (en) 2011-12-15
PE20130252A1 (es) 2013-03-16
HUE035850T2 (en) 2018-05-28
CR20120592A (es) 2013-03-04
MA34292B1 (fr) 2013-06-01
NZ604081A (en) 2014-01-31
SI2580189T1 (en) 2018-01-31
LT2580189T (lt) 2017-12-11
EP2580189A4 (en) 2016-01-06
AP2013006659A0 (en) 2013-01-31
CA2801822A1 (en) 2011-12-15
CU24148B1 (es) 2016-02-29
KR20130028134A (ko) 2013-03-18
CU20120163A7 (es) 2013-01-30
CA2801822C (en) 2015-03-24
AP3205A (en) 2015-03-31
EA020271B1 (ru) 2014-09-30
EA201201666A1 (ru) 2013-05-30
HRP20171751T1 (hr) 2017-12-29
BR112012031086A2 (pt) 2017-06-20
AU2011264206A1 (en) 2012-12-13
CY1119857T1 (el) 2018-06-27
CL2012003371A1 (es) 2013-03-22
IL223180A0 (en) 2013-02-03

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