BR112017024051A2 - processos para preparação de derivados mostarda de nitrogênio - Google Patents

processos para preparação de derivados mostarda de nitrogênio

Info

Publication number
BR112017024051A2
BR112017024051A2 BR112017024051-3A BR112017024051A BR112017024051A2 BR 112017024051 A2 BR112017024051 A2 BR 112017024051A2 BR 112017024051 A BR112017024051 A BR 112017024051A BR 112017024051 A2 BR112017024051 A2 BR 112017024051A2
Authority
BR
Brazil
Prior art keywords
processes
nitrogen derivatives
mustard nitrogen
preparing
iii
Prior art date
Application number
BR112017024051-3A
Other languages
English (en)
Inventor
Håkan WAHLSTRÖM Niklas
Anders Wennerberg Johan
Original Assignee
Oncopeptides Ab
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
Application filed by Oncopeptides Ab filed Critical Oncopeptides Ab
Publication of BR112017024051A2 publication Critical patent/BR112017024051A2/pt

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C227/00Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C227/14Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof
    • C07C227/18Preparation of compounds containing amino and carboxyl groups bound to the same carbon skeleton from compounds containing already amino and carboxyl groups or derivatives thereof by reactions involving amino or carboxyl groups, e.g. hydrolysis of esters or amides, by formation of halides, salts or esters
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00Preparation of carboxylic acid amides
    • C07C231/02Preparation of carboxylic acid amides from carboxylic acids or from esters, anhydrides, or halides thereof by reaction with ammonia or amines
    • 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
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic 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
    • C07C237/20Carboxylic 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 containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/02Carboxylic 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
    • C07C237/22Carboxylic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/14Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by halogen atoms or by nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/20Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by nitrogen atoms not being part of nitro or nitroso groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06Esters of carbamic acids
    • C07C271/08Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K1/00General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/006General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length of peptides containing derivatised side chain amino acids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/06Dipeptides
    • C07K5/06008Dipeptides with the first amino acid being neutral
    • C07K5/06078Dipeptides with the first amino acid being neutral and aromatic or cycloaliphatic
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C205/00Compounds containing nitro groups bound to a carbon skeleton
    • C07C205/06Compounds containing nitro groups bound to a carbon skeleton having nitro groups bound to carbon atoms of six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C229/00Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/40Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C229/42Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
    • YGENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

a presente invenção provê um processo para a produção de composto (iii) ou um produto desprotegido do mesmo: (iii) compreendendo composto de reação (ii) (ii) com ácido cloroacético, em presença de um agente redutor; em que pg é um grupo protetor e r é oh em uma forma adequadamente protegida ou . a invenção ainda provê compostos intermediários formados no processo da invenção, e processos para a produção de compostos in-termediários.
BR112017024051-3A 2015-05-08 2016-05-06 processos para preparação de derivados mostarda de nitrogênio BR112017024051A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
GBGB1507903.1A GB201507903D0 (en) 2015-05-08 2015-05-08 Process for preparation of nitrogen mustard derivatives
GB1507903.1 2015-05-08
PCT/EP2016/060242 WO2016180740A1 (en) 2015-05-08 2016-05-06 Process for preparation of nitrogen mustard derivatives

Publications (1)

Publication Number Publication Date
BR112017024051A2 true BR112017024051A2 (pt) 2018-07-24

Family

ID=53489337

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112017024051-3A BR112017024051A2 (pt) 2015-05-08 2016-05-06 processos para preparação de derivados mostarda de nitrogênio

Country Status (24)

Country Link
US (1) US10287316B2 (pt)
EP (1) EP3280721B1 (pt)
JP (1) JP6862354B2 (pt)
KR (1) KR102593509B1 (pt)
CN (1) CN107810189B (pt)
AU (1) AU2016260693B2 (pt)
BR (1) BR112017024051A2 (pt)
CA (1) CA2983559C (pt)
CY (1) CY1123468T1 (pt)
ES (1) ES2826401T3 (pt)
GB (1) GB201507903D0 (pt)
HK (1) HK1250732A1 (pt)
HR (1) HRP20201616T1 (pt)
HU (1) HUE051196T2 (pt)
IL (1) IL255428B (pt)
LT (1) LT3280721T (pt)
MX (1) MX2017014292A (pt)
PL (1) PL3280721T3 (pt)
PT (1) PT3280721T (pt)
RS (1) RS60952B1 (pt)
RU (1) RU2715233C2 (pt)
SI (1) SI3280721T1 (pt)
WO (1) WO2016180740A1 (pt)
ZA (1) ZA201707226B (pt)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK3866931T3 (da) 2018-10-18 2023-04-24 Oncopeptides Ab Forbindelser indeholdende deuterium
JP7475635B2 (ja) * 2020-01-30 2024-04-30 公立大学法人大阪 含窒素化合物およびその製造方法、ならびに該含窒素化合物を含む光機能性材料
CN112546969B (zh) * 2020-12-07 2022-12-23 安徽贝克制药股份有限公司 催化加氢连续生产装置和利托那韦中间体的制备方法
EP4347615A1 (en) 2021-06-01 2024-04-10 Synthon B.V. Process for making melflufen or a salt thereof
GB202204171D0 (en) 2022-03-24 2022-05-11 Oncopeptides Ab Novel formulations

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SE0002202D0 (sv) * 2000-06-13 2000-06-13 Karolinska Innovations Ab New peptides
US6992207B2 (en) * 2000-06-13 2006-01-31 Oncopeptides Ab Melphalan derivatives and their use as cancer chemotherapeutic drugs
ES2393900T3 (es) * 2001-12-03 2012-12-28 Bayer Healthcare Llc Compuestos de aril-urea en combinación con otros agentes citostáticos o citotóxicos para tratamiento de cánceres humanos
TW200615273A (en) * 2004-11-10 2006-05-16 Nicholas Piramal India Ltd Fused tricyclic compounds as inhibitors of tumor necrosis factor-alpha
AU2006251620B8 (en) * 2005-05-20 2013-07-18 Elan Pharmaceuticals, Inc. Imidazolone phenylalanine derivatives as VLA-4 antagonists
CN100491339C (zh) 2007-04-20 2009-05-27 苏州市立德化学有限公司 一种抗肿瘤药物美法仑的合成工艺
AU2009302493B2 (en) * 2008-10-08 2015-04-09 Cephalon Llc Processes for the preparation of bendamustine
US20140128462A1 (en) 2011-04-28 2014-05-08 Oncopeptides Ab Lyophilized preparation of cytotoxic dipeptides
US20130079383A1 (en) * 2011-07-13 2013-03-28 Arrowhead Research Corporation Lipid Compounds Targeting VLA-4
US10285946B2 (en) 2012-10-26 2019-05-14 Oncopeptides Ab Lyophilized preparations of melphalan flufenamide
EP2970102B1 (en) * 2013-03-11 2019-05-08 Biophore India Pharmaceuticals Pvt. Ltd. An improved process for the synthesis of melphalan and the hydrochloride salt
ITMI20130896A1 (it) * 2013-05-31 2014-12-01 Farmabios Spa Processo di purificazione di melphalan

Also Published As

Publication number Publication date
CA2983559C (en) 2023-11-07
HRP20201616T1 (hr) 2021-01-08
CN107810189A (zh) 2018-03-16
RS60952B1 (sr) 2020-11-30
ES2826401T3 (es) 2021-05-18
PL3280721T3 (pl) 2021-01-25
CA2983559A1 (en) 2016-11-17
CY1123468T1 (el) 2022-03-24
SI3280721T1 (sl) 2020-11-30
AU2016260693B2 (en) 2020-05-14
CN107810189B (zh) 2022-02-11
RU2017142725A (ru) 2019-06-10
GB201507903D0 (en) 2015-06-24
KR102593509B1 (ko) 2023-10-24
US20180148473A1 (en) 2018-05-31
HUE051196T2 (hu) 2021-03-01
JP6862354B2 (ja) 2021-04-21
NZ736564A (en) 2023-10-27
LT3280721T (lt) 2020-12-28
PT3280721T (pt) 2020-10-20
IL255428A0 (en) 2017-12-31
KR20180005214A (ko) 2018-01-15
HK1250732A1 (zh) 2019-01-11
AU2016260693A1 (en) 2017-11-23
RU2017142725A3 (pt) 2019-09-09
JP2018515512A (ja) 2018-06-14
EP3280721B1 (en) 2020-07-22
IL255428B (en) 2021-07-29
ZA201707226B (en) 2019-01-30
WO2016180740A1 (en) 2016-11-17
US10287316B2 (en) 2019-05-14
MX2017014292A (es) 2018-03-07
EP3280721A1 (en) 2018-02-14
RU2715233C2 (ru) 2020-02-26

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]

Free format text: DE ACORDO COM O ARTIGO 229-C DA LEI NO 10196/2001, QUE MODIFICOU A LEI NO 9279/96, A CONCESSAO DA PATENTE ESTA CONDICIONADA A ANUENCIA PREVIA DA ANVISA. CONSIDERANDO A APROVACAO DOS TERMOS DO PARECER NO 337/PGF/EA/2010, BEM COMO A PORTARIA INTERMINISTERIAL NO 1065 DE 24/05/2012, ENCAMINHA-SE O PRESENTE PEDIDO PARA AS PROVIDENCIAS CABIVEIS.

B07E Notification of approval relating to section 229 industrial property law [chapter 7.5 patent gazette]
B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]