BR112012018625A2 - archimica - Google Patents

archimica

Info

Publication number
BR112012018625A2
BR112012018625A2 BR112012018625A BR112012018625A BR112012018625A2 BR 112012018625 A2 BR112012018625 A2 BR 112012018625A2 BR 112012018625 A BR112012018625 A BR 112012018625A BR 112012018625 A BR112012018625 A BR 112012018625A BR 112012018625 A2 BR112012018625 A2 BR 112012018625A2
Authority
BR
Brazil
Prior art keywords
lacosamide
enantiometer
low cost
racemic mixture
mixture
Prior art date
Application number
BR112012018625A
Other languages
English (en)
Inventor
Alberto Bologna
Domenico Vergani
Giorgio Bertolini
Patrizia Castoldi
Original Assignee
Euticals Spa
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=42174220&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=BR112012018625(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Euticals Spa filed Critical Euticals Spa
Publication of BR112012018625A2 publication Critical patent/BR112012018625A2/pt

Links

Classifications

    • 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
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/16—Preparation of optical isomers
    • C07C231/20—Preparation of optical isomers by separation of optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/04—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • C07C237/06—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated having the nitrogen atoms of the carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C237/22—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atoms of the carboxamide groups bound to acyclic carbon atoms of the carbon skeleton having nitrogen atoms of amino groups bound to the carbon skeleton of the acid part, further acylated
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C2601/00—Systems containing only non-condensed rings
    • C07C2601/06—Systems containing only non-condensed rings with a five-membered ring
    • C07C2601/08—Systems containing only non-condensed rings with a five-membered ring the ring being saturated

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Analytical Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Saccharide Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

processo para a preparação de lacosamida. é descrito um novo processo para a síntese de lacosamida usando d,l-serina como material de partida, em que a reação de metilação de hdiroxila é realizada utilizando uma base de baixo custo, tal como, naoh e um agente de alquilação de baixo custo, a tóxico e não carcinogênico, tal como, ptoluenossulfonato de metila, o enantiômetro r é isolado a partir da mistura racêmica de lacosamida após hidrólise seletiva da acetamida, salificação da mistura racêmica com um ácido quiral (hx*) em um solvente orgânico, decomposição da mistura diastereoisomérica, de preferência, por precipitação do enantiômetro r, e acetilação subsequente do intermediário opticamente puro.
BR112012018625A 2010-01-29 2010-12-22 archimica BR112012018625A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2010A000127A IT1398044B1 (it) 2010-01-29 2010-01-29 Processo per la preparazione della lacosamide
PCT/IB2010/056014 WO2011092559A1 (en) 2010-01-29 2010-12-22 Process for the synthesis of lacosamide

Publications (1)

Publication Number Publication Date
BR112012018625A2 true BR112012018625A2 (pt) 2016-04-05

Family

ID=42174220

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112012018625A BR112012018625A2 (pt) 2010-01-29 2010-12-22 archimica

Country Status (12)

Country Link
US (1) US8796488B2 (pt)
EP (1) EP2528892B1 (pt)
JP (1) JP5779592B2 (pt)
KR (1) KR101766506B1 (pt)
CN (1) CN102822140B (pt)
BR (1) BR112012018625A2 (pt)
CL (1) CL2012002082A1 (pt)
ES (1) ES2495815T3 (pt)
IL (1) IL220936A (pt)
IT (1) IT1398044B1 (pt)
RU (1) RU2585762C2 (pt)
WO (1) WO2011092559A1 (pt)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9133101B2 (en) 2011-08-29 2015-09-15 Signa S.A. De C.V. Processes for the preparation of (R)-2-acetamido-N-benzyl-3-methoxypropionamide and intermediates thereof
CN102516114B (zh) * 2011-10-28 2014-04-16 杭州迪克化工技术有限公司 一种r-(-)-2-氨基-3-甲氧基-n-苄基丙酰胺-d-酒石酸盐及其制备方法
CN102424655B (zh) * 2011-10-28 2014-04-16 杭州迪克化工技术有限公司 一种r-(-)-2-乙酰胺基-3-甲氧基-n-苄基丙酰胺的制备方法
GB201219627D0 (en) 2012-11-01 2012-12-12 Cambrex Karlskoga Ab New process
WO2016021711A1 (ja) * 2014-08-07 2016-02-11 株式会社エーピーアイ コーポレーション アミノ酸誘導体の製造方法
WO2016039393A1 (ja) * 2014-09-10 2016-03-17 株式会社エーピーアイ コーポレーション アミノ酸誘導体の製造方法
CN106699595B (zh) * 2015-07-21 2019-04-12 上海医药集团股份有限公司 一种拉科酰胺制备方法
CN106699605B (zh) * 2015-07-21 2019-08-20 上海医药集团股份有限公司 一种拉科酰胺中间体的甲基化方法
IN2015CH05001A (pt) 2015-09-18 2015-10-16 Divis Lab Ltd
EP3659997A1 (en) 2015-11-13 2020-06-03 API Corporation Method for producing lacosamide and intermediate thereof
CN107641087A (zh) * 2017-06-01 2018-01-30 合肥远志医药科技开发有限公司 一种工业化拉科酰胺的制备方法
CN112574058B (zh) * 2020-12-31 2023-04-28 珠海润都制药股份有限公司 一种拉考沙胺的合成路线

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1038522T3 (da) * 1996-03-15 2004-10-11 Res Corp Technologies Inc Antikonvulsive enantiomere aminosyrederivater
US5773475A (en) 1997-03-17 1998-06-30 Research Corporation Technologies, Inc. Anticonvulsant enantiomeric amino acid derivatives
EP1642889A1 (en) * 2004-10-02 2006-04-05 Schwarz Pharma Ag Improved synthesis scheme for lacosamide
CN100584821C (zh) * 2007-07-31 2010-01-27 浙江九洲药业股份有限公司 一种制备光学纯度叔亮氨酸的方法
US8093426B2 (en) 2007-12-04 2012-01-10 Ranbaxy Laboratories Limited Intermediate compounds and their use in preparation of lacosamide
CN101333175A (zh) * 2008-07-29 2008-12-31 东南大学 制备d-天冬酰胺及d-高丝氨酸的方法
CN104058991B (zh) * 2008-11-07 2017-04-12 优时比制药有限公司 制备氨基酸衍生物的新方法

Also Published As

Publication number Publication date
ES2495815T3 (es) 2014-09-17
JP2013518092A (ja) 2013-05-20
KR101766506B1 (ko) 2017-08-08
KR20130006438A (ko) 2013-01-16
CN102822140A (zh) 2012-12-12
CL2012002082A1 (es) 2013-07-26
IT1398044B1 (it) 2013-02-07
EP2528892B1 (en) 2014-06-04
US8796488B2 (en) 2014-08-05
WO2011092559A1 (en) 2011-08-04
RU2012131215A (ru) 2014-03-10
RU2585762C2 (ru) 2016-06-10
JP5779592B2 (ja) 2015-09-16
US20130030216A1 (en) 2013-01-31
IL220936A0 (en) 2012-09-24
IL220936A (en) 2014-11-30
ITMI20100127A1 (it) 2011-07-30
CN102822140B (zh) 2014-10-22
EP2528892A1 (en) 2012-12-05

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B08E Application fees: payment of additional fee required [chapter 8.5 patent gazette]

Free format text: COMPLEMENTAR A RETRIBUICAO DA 8A ANUIDADE, DE ACORDO COM TABELA VIGENTE, REFERENTE A GUIA DE RECOLHIMENTO 29409161803259778.

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B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: EM VIRTUDE DO ARQUIVAMENTO PUBLICADO NA RPI 2509 DE 05-02-2019 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDO O ARQUIVAMENTO DO PEDIDO DE PATENTE, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.