BR112018007505A2 - processo industrial para a preparação de sal de (e)-3-carboxiacrilato de (5s,10s)-10-benzil-16-metil-11,14,18-trioxo-15,17,19-trioxa-2,7,8-tritia-12-aza-henicosan-5-amínio - Google Patents

processo industrial para a preparação de sal de (e)-3-carboxiacrilato de (5s,10s)-10-benzil-16-metil-11,14,18-trioxo-15,17,19-trioxa-2,7,8-tritia-12-aza-henicosan-5-amínio

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Publication number
BR112018007505A2
BR112018007505A2 BR112018007505-1A BR112018007505A BR112018007505A2 BR 112018007505 A2 BR112018007505 A2 BR 112018007505A2 BR 112018007505 A BR112018007505 A BR 112018007505A BR 112018007505 A2 BR112018007505 A2 BR 112018007505A2
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BR
Brazil
Prior art keywords
tritia
henicosan
trioxo
trioxa
aza
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Application number
BR112018007505-1A
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English (en)
Other versions
BR112018007505B1 (pt
Inventor
Poras Hervé
Lefebvre Loïc
Zhao Xinjun
Gamberoni Luca
De Rosa Sabrina
Velardi Rosario
Original Assignee
Pharmaleads
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Publication date
Application filed by Pharmaleads filed Critical Pharmaleads
Publication of BR112018007505A2 publication Critical patent/BR112018007505A2/pt
Publication of BR112018007505B1 publication Critical patent/BR112018007505B1/pt

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/24—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/25—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton being acyclic and saturated
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J19/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/18—Stationary reactors having moving elements inside
    • B01J19/1862—Stationary reactors having moving elements inside placed in series
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/02—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of thiols
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/22—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/22—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides
    • C07C319/24—Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides by reactions involving the formation of sulfur-to-sulfur bonds
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00—Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/26—Separation; Purification; Stabilisation; Use of additives
    • C07C319/28—Separation; Purification
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/56—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton the carbon skeleton containing six-membered aromatic rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton
    • C07C323/51—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton
    • C07C323/60—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atoms of the thio groups bound to acyclic carbon atoms of the carbon skeleton with the carbon atom of at least one of the carboxyl groups bound to nitrogen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00—Thiocarboxylic acids
    • C07C327/20—Esters of monothiocarboxylic acids
    • C07C327/32—Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/16—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D215/20—Oxygen atoms
    • C07D215/24—Oxygen atoms attached in position 8
    • C07D215/26—Alcohols; Ethers thereof
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002—Chemical plants
    • B01J2219/00027—Process aspects
    • B01J2219/00029—Batch processes
    • B—PERFORMING OPERATIONS; TRANSPORTING
    • B01—PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01J—CHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00—Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002—Chemical plants
    • B01J2219/00027—Process aspects
    • B01J2219/0004—Processes in series
    • 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
    • C07C323/00—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton
    • C07C323/39—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and nitrogen atoms, not being part of nitro or nitroso groups, bound to the same carbon skeleton at least one of the nitrogen atoms being part of any of the groups, X being a hetero atom, Y being any atom
    • C07C323/40—Y being a hydrogen or a carbon atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

a presente invenção se refere a um processo industrial para a preparação de sal de (e)-3-carboxiacrilato de (5s,10s)-10-benzil-16-metil-11,14,18-trioxo-15,17,19-trioxa-2,7,8-tritia-12-aza-henicosan-5-amínio da seguinte fórmula (i): em que xé fumarato. este processo compreende as seguintes etapas-chave sucessivas: uma resolução cinética, formação decomposto de dissulfureto, acoplamento peptídico e reação de troca aniônica para obter o produto desejado de fórmula (i).
BR112018007505-1A 2015-10-14 2016-10-14 PROCESSO INDUSTRIAL PARA A PREPARAÇÃO DE SAL DE (E)-3-CARBOXIACRILATO DE (5S,10S)-10-BENZIL16-METIL-ll,14,18-TRIOXO-15,17,19-TRIOXA-2,7,8-TRITIA-12-AZA-HENICOSAN-5-AMÍNIO BR112018007505B1 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP15306626.1 2015-10-14
EP15306626 2015-10-14
PCT/EP2016/074709 WO2017064250A1 (en) 2015-10-14 2016-10-14 Industrial process for the preparation of (5s,10s)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (e)-3-carboxyacrylate salt

Publications (2)

Publication Number Publication Date
BR112018007505A2 true BR112018007505A2 (pt) 2018-10-23
BR112018007505B1 BR112018007505B1 (pt) 2020-11-17

Family

ID=54330703

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112018007505-1A BR112018007505B1 (pt) 2015-10-14 2016-10-14 PROCESSO INDUSTRIAL PARA A PREPARAÇÃO DE SAL DE (E)-3-CARBOXIACRILATO DE (5S,10S)-10-BENZIL16-METIL-ll,14,18-TRIOXO-15,17,19-TRIOXA-2,7,8-TRITIA-12-AZA-HENICOSAN-5-AMÍNIO

Country Status (15)

Country Link
US (1) US10399936B2 (pt)
EP (1) EP3362433B1 (pt)
JP (2) JP6998864B2 (pt)
KR (1) KR20180095507A (pt)
CN (1) CN108430968B (pt)
AU (1) AU2016336891B2 (pt)
BR (1) BR112018007505B1 (pt)
CA (1) CA3016962A1 (pt)
DK (1) DK3362433T3 (pt)
ES (1) ES2818185T3 (pt)
IL (1) IL258663B (pt)
MX (1) MX2018004631A (pt)
TW (1) TWI712582B (pt)
WO (1) WO2017064250A1 (pt)
ZA (1) ZA201803105B (pt)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN107814708A (zh) * 2017-11-27 2018-03-20 杭州新博思生物医药有限公司 一种拆分剂奎宁的回收套用方法
FR3077201B1 (fr) 2018-01-26 2020-01-17 Pharmaleads Derives aminoacides contenant un groupement disulfanyle sous forme d'un inhibiteur de nep et d'apn pour la prevention et le traitement des douleurs relatives au nerf trijumeau
CN113651745B (zh) * 2021-09-09 2023-06-02 上海医药工业研究院 布瓦西坦中间体及其制备方法和纯化方法

Family Cites Families (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2651229B1 (fr) * 1989-08-24 1991-12-13 Inst Nat Sante Rech Med Nouveaux derives d'amino-acides, leur procede de preparation et leur application therapeutique.
US5552397A (en) 1992-05-18 1996-09-03 E. R. Squibb & Sons, Inc. Substituted azepinone dual inhibitors of angiotensin converting enzyme and neutral exdopeptidase
JPH11228532A (ja) * 1998-02-16 1999-08-24 Ajinomoto Co Inc 光学活性２−アセチルチオメチル−３−フェニルプロピオン酸の製造方法
ES2369256T3 (es) * 2000-06-26 2011-11-28 Helen Of Troy Limited Sistema de lámpara recargable.
AR036237A1 (es) 2001-07-27 2004-08-25 Bayer Corp Derivados del acido indan acetico, intermediarios, y metodo para su preparacion, composicion farmaceutica y el uso de dichos derivados para la manufactura de un medicamento
EP1940818B1 (fr) 2005-10-25 2011-08-24 Pharmaleads Derives d'amino-acides contenant un groupement disulfanyle comme inhibiteurs mixtes de la neprilysine et de l 'aminopeptidase n
CN100497296C (zh) * 2006-07-07 2009-06-10 沈阳药科大学 旋光活性的苯乙醇胺类化合物及其制法
FR2931151A1 (fr) 2008-05-13 2009-11-20 Pharmaleads Soc Par Actions Si Nouveaux derives d'amino-acides, leur procede de preparation et leur utilisation therapeutique
FR2997080B1 (fr) * 2012-10-23 2015-11-27 Pharmaleads Inhibiteurs de neprilysine

Also Published As

Publication number Publication date
AU2016336891B2 (en) 2020-07-09
AU2016336891A1 (en) 2018-05-31
JP2021193127A (ja) 2021-12-23
WO2017064250A1 (en) 2017-04-20
CN108430968A (zh) 2018-08-21
CN108430968B (zh) 2021-01-05
TWI712582B (zh) 2020-12-11
BR112018007505B1 (pt) 2020-11-17
JP2018531946A (ja) 2018-11-01
ZA201803105B (en) 2019-02-27
IL258663B (en) 2020-08-31
EP3362433A1 (en) 2018-08-22
JP6998864B2 (ja) 2022-02-04
KR20180095507A (ko) 2018-08-27
EP3362433B1 (en) 2020-07-08
MX2018004631A (es) 2018-11-09
DK3362433T3 (da) 2020-09-21
CA3016962A1 (en) 2017-04-20
US10399936B2 (en) 2019-09-03
US20180305308A1 (en) 2018-10-25
TW201718479A (zh) 2017-06-01
IL258663A (en) 2018-06-28
ES2818185T3 (es) 2021-04-09

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Legal Events

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B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 14/10/2016, OBSERVADAS AS CONDICOES LEGAIS.