EA201201666A1 - Промежуточные соединения агомелатина и способ их получения - Google Patents

Промежуточные соединения агомелатина и способ их получения

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Publication number
EA201201666A1
EA201201666A1 EA201201666A EA201201666A EA201201666A1 EA 201201666 A1 EA201201666 A1 EA 201201666A1 EA 201201666 A EA201201666 A EA 201201666A EA 201201666 A EA201201666 A EA 201201666A EA 201201666 A1 EA201201666 A1 EA 201201666A1
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EA
Eurasian Patent Office
Prior art keywords
agomelatine
preparation
intermediate compounds
present
new intermediates
Prior art date
Application number
EA201201666A
Other languages
English (en)
Other versions
EA020271B1 (ru
Inventor
Пэн Чжан
Ю Хуан
Чжедун Юань
Ханьбинь Шань
Сюй Юй
Original Assignee
Ле Лаборатуар Сервье
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=45097542&utm_source=***_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=EA201201666(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Ле Лаборатуар Сервье filed Critical Ле Лаборатуар Сервье
Publication of EA201201666A1 publication Critical patent/EA201201666A1/ru
Publication of EA020271B1 publication Critical patent/EA020271B1/ru

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Classifications

    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/06—Preparation of carboxylic acid amides from nitriles by transformation of cyano groups into carboxamide groups
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/16—Amides, e.g. hydroxamic acids
    • A61K31/165—Amides, e.g. hydroxamic acids having aromatic rings, e.g. colchicine, atenolol, progabide
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic 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
    • C07C233/17—Carboxylic 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
    • C07C233/18—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/16—Carboxylic 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
    • C07C233/17—Carboxylic 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
    • C07C233/22—Carboxylic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2602/00—Systems containing two condensed rings
    • C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
    • C07C2602/04—One of the condensed rings being a six-membered aromatic ring
    • C07C2602/10—One of the condensed rings being a six-membered aromatic ring the other ring being six-membered, e.g. tetraline

Abstract

Настоящее изобретение относится к промежуточным соединениям для получения агомелатина, так же, как и к способам их получения. Промежуточное соединение настоящего изобретения для получения агомелатина представляет собой соединение А в соответствии с следующей формулой. Также обеспечены два новых промежуточных соединения. Когда применяются эти новые промежуточные соединения для получения агомелатина, способ является простым для управления, хорошо контролируемым, и дает продукт с высокой чистотой, без сложных операций, таких как ректификация и разделение хроматографией на колонке, и является подходящим для промышленного производства. При этом, способы получения самих двух новых промежуточных соединений являются простыми и с высоким выходом, только когда применяют наиболее широко используемый 7-метокситетралон в качестве исходного стартового материала и проводят одну стадию реакции для получения промежуточных соединений с последующей еще одной стадией преобразования промежуточного соединения в желаемый продукт агомелатин. Упомянутые процессы реакции очень упрощены, с улучшенным выходом реакции, а также преодолевают трудности в очистке предыдущего способа при сравнении с предыдущей методикой получения агомелатина. Обычно выход настоящего изобретения составляет свыше 70%.
EA201201666A 2010-06-08 2011-06-08 Промежуточные соединения агомелатина и способ их получения EA020271B1 (ru)

Applications Claiming Priority (2)

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
PCT/CN2011/075438 WO2011153939A1 (en) 2010-06-08 2011-06-08 Agomelatine intermediates and preparation method thereof

Publications (2)

Publication Number Publication Date
EA201201666A1 true EA201201666A1 (ru) 2013-05-30
EA020271B1 EA020271B1 (ru) 2014-09-30

Family

ID=45097542

Family Applications (1)

Application Number Title Priority Date Filing Date
EA201201666A EA020271B1 (ru) 2010-06-08 2011-06-08 Промежуточные соединения агомелатина и способ их получения

Country Status (40)

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

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
JP2023506144A (ja) * 2019-12-23 2023-02-15 ディーエスエム アイピー アセッツ ビー．ブイ． 脱水素化方法

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
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
FR2866335B1 (fr) 2004-02-13 2006-05-26 Servier Lab Nouveau procede de 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
CN101472884A (zh) * 2006-06-20 2009-07-01 弗·哈夫曼-拉罗切有限公司 1,2,3,4-四氢化萘和茚满衍生物及其用途
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
EP2705023A4 (en) * 2011-01-04 2014-11-19 Symed Labs Ltd PROCESSES FOR THE PREPARATION OF N- [2- (7-METHOXY-1-NAPHTHYLLELYHYL) ACETAMIDE

Also Published As

Publication number Publication date
WO2011153939A1 (en) 2011-12-15
MA34292B1 (fr) 2013-06-01
ME02992B (me) 2018-10-20
PT2580189T (pt) 2017-12-06
US20130267738A1 (en) 2013-10-10
DK2580189T3 (da) 2018-01-29
KR20130028134A (ko) 2013-03-18
NZ604081A (en) 2014-01-31
GT201200328A (es) 2014-06-09
AU2011264206A1 (en) 2012-12-13
US8779199B2 (en) 2014-07-15
IL223180A (en) 2014-06-30
CR20120592A (es) 2013-03-04
JP5519863B2 (ja) 2014-06-11
ECSP12012328A (es) 2012-12-28
LT2580189T (lt) 2017-12-11
EP2580189B1 (en) 2017-10-25
ZA201208764B (en) 2014-01-29
SI2580189T1 (en) 2018-01-31
NO2580189T3 (ru) 2018-03-24
IL223180A0 (en) 2013-02-03
AP3205A (en) 2015-03-31
CY1119857T1 (el) 2018-06-27
AP2013006659A0 (en) 2013-01-31
UA104684C2 (ru) 2014-02-25
EP2580189A1 (en) 2013-04-17
EA020271B1 (ru) 2014-09-30
TN2012000542A1 (en) 2014-04-01
HRP20171751T1 (hr) 2017-12-29
JP2013531639A (ja) 2013-08-08
SG185667A1 (en) 2012-12-28
MY160954A (en) 2017-03-31
RS56659B1 (sr) 2018-03-30
PL2580189T3 (pl) 2018-04-30
AU2011264206B2 (en) 2013-08-15
NI201200177A (es) 2013-02-06
BR112012031086B1 (pt) 2020-12-08
BR112012031086A2 (pt) 2017-06-20
CA2801822C (en) 2015-03-24
CU20120163A7 (es) 2013-01-30
KR101470874B1 (ko) 2014-12-09
CN102276492A (zh) 2011-12-14
CU24148B1 (es) 2016-02-29
CN102276492B (zh) 2013-04-10
PE20130252A1 (es) 2013-03-16
MX2012013870A (es) 2013-01-24
ES2656968T3 (es) 2018-03-01
GEP20156234B (en) 2015-01-26
CL2012003371A1 (es) 2013-03-22
CA2801822A1 (en) 2011-12-15
HUE035850T2 (en) 2018-05-28
EP2580189A4 (en) 2016-01-06

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