DK3362433T3 - Industriel fremgangsmåde til fremstilling af (5s,10s)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (e)-3-carboxyacrylat-salt - Google Patents

Industriel fremgangsmåde til fremstilling af (5s,10s)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (e)-3-carboxyacrylat-salt Download PDF

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DK3362433T3
DK3362433T3 DK16784446.3T DK16784446T DK3362433T3 DK 3362433 T3 DK3362433 T3 DK 3362433T3 DK 16784446 T DK16784446 T DK 16784446T DK 3362433 T3 DK3362433 T3 DK 3362433T3
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Denmark
Prior art keywords
azahenicosan
trithia
trioxo
aminium
trioxa
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DK16784446.3T
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English (en)
Inventor
Hervé Poras
Xinjun Zhao
Luca Gamberoni
Rosa Sabrina De
Rosario Velardi
Loïc Lefebvre
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Pharmaleads
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23Thiols, 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
    • C07C323/24Thiols, 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
    • C07C323/25Thiols, 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/22Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J19/00Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J19/18Stationary reactors having moving elements inside
    • B01J19/1862Stationary reactors having moving elements inside placed in series
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/02Preparation of thiols, sulfides, hydropolysulfides or polysulfides of thiols
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/22Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides
    • C07C319/24Preparation of thiols, sulfides, hydropolysulfides or polysulfides of hydropolysulfides or polysulfides by reactions involving the formation of sulfur-to-sulfur bonds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C319/00Preparation of thiols, sulfides, hydropolysulfides or polysulfides
    • C07C319/26Separation; Purification; Stabilisation; Use of additives
    • C07C319/28Separation; Purification
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, 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
    • C07C323/51Thiols, 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
    • C07C323/56Thiols, 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/50Thiols, 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
    • C07C323/51Thiols, 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
    • C07C323/60Thiols, 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C327/00Thiocarboxylic acids
    • C07C327/20Esters of monothiocarboxylic acids
    • C07C327/32Esters of monothiocarboxylic acids having sulfur atoms of esterified thiocarboxyl groups bound to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D215/00Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02Heterocyclic 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
    • C07D215/16Heterocyclic 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
    • C07D215/20Oxygen atoms
    • C07D215/24Oxygen atoms attached in position 8
    • C07D215/26Alcohols; Ethers thereof
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002Chemical plants
    • B01J2219/00027Process aspects
    • B01J2219/00029Batch processes
    • BPERFORMING OPERATIONS; TRANSPORTING
    • B01PHYSICAL OR CHEMICAL PROCESSES OR APPARATUS IN GENERAL
    • B01JCHEMICAL OR PHYSICAL PROCESSES, e.g. CATALYSIS OR COLLOID CHEMISTRY; THEIR RELEVANT APPARATUS
    • B01J2219/00Chemical, physical or physico-chemical processes in general; Their relevant apparatus
    • B01J2219/00002Chemical plants
    • B01J2219/00027Process aspects
    • B01J2219/0004Processes in series
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07Optical isomers
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C323/00Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups
    • C07C323/23Thiols, 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
    • C07C323/39Thiols, 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
    • C07C323/40Y being a hydrogen or a carbon atom

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  • 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)
DK16784446.3T 2015-10-14 2016-10-14 Industriel fremgangsmåde til fremstilling af (5s,10s)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (e)-3-carboxyacrylat-salt DK3362433T3 (da)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
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 (1)

Publication Number Publication Date
DK3362433T3 true DK3362433T3 (da) 2020-09-21

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Application Number Title Priority Date Filing Date
DK16784446.3T DK3362433T3 (da) 2015-10-14 2016-10-14 Industriel fremgangsmåde til fremstilling af (5s,10s)-10-benzyl-16-methyl-11,14,18-trioxo-15,17,19-trioxa-2,7,8-trithia-12-azahenicosan-5-aminium (e)-3-carboxyacrylat-salt

Country Status (15)

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

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
BR112018007505A2 (pt) 2018-10-23
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
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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