PE20231553A1 - Proceso para preparar carbamato de metil {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il} - Google Patents

Proceso para preparar carbamato de metil {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}

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Publication number
PE20231553A1
PE20231553A1 PE2022002944A PE2022002944A PE20231553A1 PE 20231553 A1 PE20231553 A1 PE 20231553A1 PE 2022002944 A PE2022002944 A PE 2022002944A PE 2022002944 A PE2022002944 A PE 2022002944A PE 20231553 A1 PE20231553 A1 PE 20231553A1
Authority
PE
Peru
Prior art keywords
compound
dmso
formula
fluorobenzyl
pyrazolo
Prior art date
Application number
PE2022002944A
Other languages
English (en)
Inventor
Peter Fey
Nadine Bremeyer
Markus Longerich
Thomas Frenzel
Helene Faber
Michal Sowa
Joerg Brockob
Guido Becker
Heike Neumann
Original Assignee
Adverio Pharma Gmbh
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 Adverio Pharma Gmbh filed Critical Adverio Pharma Gmbh
Publication of PE20231553A1 publication Critical patent/PE20231553A1/es

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D471/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
    • C07D471/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
    • C07D471/04Ortho-condensed systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D295/00Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms
    • C07D295/04Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms
    • C07D295/06Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals
    • C07D295/067Heterocyclic compounds containing polymethylene-imine rings with at least five ring members, 3-azabicyclo [3.2.2] nonane, piperazine, morpholine or thiomorpholine rings, having only hydrogen atoms directly attached to the ring carbon atoms with substituted hydrocarbon radicals attached to ring nitrogen atoms substituted by halogen atoms or nitro radicals with the ring nitrogen atoms and the substituents attached to the same carbon chain, which is not interrupted by carbocyclic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Agricultural Chemicals And Associated Chemicals (AREA)

Abstract

REFERIDO A UN PROCESO PARA PREPARAR CARBAMATO DE METIL {4,6-DIAMINO-2-[5-FLUORO-1-(2-FLUOROBENCIL)-1H-PIRAZOLO[3,4-B]PIRIDIN-3-IL]PIRIMIDIN-5-IL} DE FORMULA (I) EN FORMA CRISTALINA DE LA MODIFICACION I, DONDE EL DIFRACTOGRAMA DE RAYOS X DE DICHO COMPUESTO PRESENTA MAXIMOS PICO DE ANGULO 2 THETA EN 5.9, 6.9, 22.7; EN DONDE EL CLORHIDRATO DEL COMPUESTO (I) SE PREPARA CALENTANDO EL COMPUESTO DE FORMULA (IX) EN TETRAHIDROFURANO COMO SOLVENTE, AGREGANDO 1,0 EQ. A 1,2 EQ. CLOROFORMATO DE METILO, AGITANDO DENTRO DE UN TIEMPO DE REACCION DE 1H A 10H, Y AISLANDO EL CLORHIDRATO DEL COMPUESTO (I), LUEGO EL SOLVATO DE DI-DMSO DEL COMPUESTO DE FORMULA (I) SE PREPARA DISOLVIENDO EL CLORHIDRATO DEL COMPUESTO DE LA FORMULA (I) EN DMSO, ANADIENDO TRI-N-BUTILAMINA Y CARBONO ACTIVADO, RETIRANDO EL CARBONO ACTIVADO, CRISTALIZANDO EL SOLVATO DE DI-DMSO POR ENFRIAMIENTO Y ANADIENDO ACETATO DE ETILO, AISLANDO EL DI-DMSO EN FORMA CRISTALIZADA, Y LAVANDO CON UNA MEZCLA DE DMSO Y ACETATO DE ETILO; POSTERIORMENTE SE PREPARA LA FORMA CRISTALINA DE LA MODIFICACION I DEL COMPUESTO (I).
PE2022002944A 2020-06-16 2021-06-15 Proceso para preparar carbamato de metil {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il} PE20231553A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP20180229.5A EP3925953A1 (en) 2020-06-16 2020-06-16 Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate
PCT/EP2021/066019 WO2021254981A1 (en) 2020-06-16 2021-06-15 Process for preparing methyl {4,6-diamino-2-[5-fluoro-1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}carbamate

Publications (1)

Publication Number Publication Date
PE20231553A1 true PE20231553A1 (es) 2023-10-03

Family

ID=71103286

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022002944A PE20231553A1 (es) 2020-06-16 2021-06-15 Proceso para preparar carbamato de metil {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}

Country Status (17)

Country Link
US (1) US20230219952A1 (es)
EP (2) EP3925953A1 (es)
JP (1) JP2023530142A (es)
KR (1) KR20230025862A (es)
CN (1) CN115697978A (es)
AR (1) AR122635A1 (es)
AU (1) AU2021294233A1 (es)
BR (1) BR112022023035A2 (es)
CA (1) CA3187147A1 (es)
CL (1) CL2022003600A1 (es)
CO (1) CO2022018232A2 (es)
CR (1) CR20220647A (es)
IL (1) IL298913A (es)
MX (1) MX2022015952A (es)
PE (1) PE20231553A1 (es)
TW (1) TW202214625A (es)
WO (1) WO2021254981A1 (es)

Families Citing this family (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TWI830835B (zh) * 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
ES2956054B2 (es) * 2022-05-03 2024-07-01 Moehs Iberica Sl 2-(5-FLUORO-1-(2-FLUOROBENCIL)-1H-PIRAZOLO[3,4-b]PIRIDIN-3-IL)-5-NITROSOPIRIMIDIN-4,6-DIAMINA O UNA SAL DE LA MISMA, PROCEDIMIENTO PARA SU PREPARACION Y SU USO EN LA SINTESIS DE VERICIGUAT
CN115043835B (zh) * 2022-06-17 2023-05-09 常州制药厂有限公司 一种维立西呱的精制纯化方法

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19834044A1 (de) 1998-07-29 2000-02-03 Bayer Ag Neue substituierte Pyrazolderivate
UY33041A (es) * 2009-11-27 2011-06-30 Bayer Schering Pharma Aktienegesellschaft Procedimiento para la preparaciòn de {4,6-diamino-2-[1-(2-fluorobencil)-1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo y su purificaciòn para el uso como principio activo farmacèutico
EP2504334B1 (de) * 2009-11-27 2014-10-01 Bayer Intellectual Property GmbH Verfahren zur reinigung von methyl-{4,6-diamino-2-[1-(2-fluorobenzyl)-1h-pyrazolo[3,4-b]pyridin-3-yl]pyrimidin-5-yl}methylcarbamat
ES2549979T3 (es) * 2010-05-26 2015-11-03 Adverio Pharma Gmbh El uso de estimuladores de la sGC, activadores de la sGC, solos y en combinaciones con inhibidores de la PDE5 para el tratamiento de esclerosis sistémica (EcS)
DE102010021637A1 (de) 2010-05-26 2011-12-01 Bayer Schering Pharma Aktiengesellschaft Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung
DE102010040233A1 (de) * 2010-09-03 2012-03-08 Bayer Schering Pharma Aktiengesellschaft Bicyclische Aza-Heterocyclen und ihre Verwendung
BR112014005110A2 (pt) * 2011-09-02 2017-04-18 Bayer Ip Gmbh pirimidinas aneladas substituídas e utilização das mesmas
BR122020001312B1 (pt) 2011-11-25 2022-02-15 Adverio Pharma Gmbh Processo para preparação de 5-flúor-1h-pirazolopiridinas substituídas, e compostos intermediários
TWI830835B (zh) 2018-12-17 2024-02-01 德商亞德維瑞醫藥有限公司 具改善性質之{4,6-二胺基-2-[5-氟-1-(2-氟芐基)-1H-吡唑並[3,4-b]吡啶-3-基]嘧啶-5-基}胺基甲酸甲酯活性化合物產物、其製造及調配物
CN113272286B (zh) 2019-01-22 2024-04-16 阿德弗里奥药品有限责任公司 制备4-(2,2,3,3-四氟丙基)吗啉的方法

Also Published As

Publication number Publication date
CL2022003600A1 (es) 2023-04-28
JP2023530142A (ja) 2023-07-13
EP4165028A1 (en) 2023-04-19
BR112022023035A2 (pt) 2022-12-27
EP3925953A1 (en) 2021-12-22
TW202214625A (zh) 2022-04-16
CN115697978A (zh) 2023-02-03
KR20230025862A (ko) 2023-02-23
IL298913A (en) 2023-02-01
CO2022018232A2 (es) 2022-12-20
WO2021254981A1 (en) 2021-12-23
AU2021294233A1 (en) 2022-12-22
AR122635A1 (es) 2022-09-28
US20230219952A1 (en) 2023-07-13
CA3187147A1 (en) 2021-12-23
MX2022015952A (es) 2023-01-24
CR20220647A (es) 2023-03-03

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