MX2022015952A - Proceso para preparar {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)- 1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo. - Google Patents
Proceso para preparar {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)- 1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo.Info
- Publication number
- MX2022015952A MX2022015952A MX2022015952A MX2022015952A MX2022015952A MX 2022015952 A MX2022015952 A MX 2022015952A MX 2022015952 A MX2022015952 A MX 2022015952A MX 2022015952 A MX2022015952 A MX 2022015952A MX 2022015952 A MX2022015952 A MX 2022015952A
- Authority
- MX
- Mexico
- Prior art keywords
- fluoro
- pyrazolo
- pyrimidin
- diamino
- carbamate
- Prior art date
Links
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- QZFHIXARHDBPBY-UHFFFAOYSA-N vericiguat Chemical compound N1=C(N)C(NC(=O)OC)=C(N)N=C1C(C1=CC(F)=CN=C11)=NN1CC1=CC=CC=C1F QZFHIXARHDBPBY-UHFFFAOYSA-N 0.000 title abstract 2
- 238000000034 method Methods 0.000 abstract 2
- 230000004048 modification Effects 0.000 abstract 2
- 238000012986 modification Methods 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 238000002955 isolation Methods 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D471/00—Heterocyclic 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
- C07D471/02—Heterocyclic 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
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic 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
- C07D295/04—Heterocyclic 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D295/00—Heterocyclic 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
- C07D295/04—Heterocyclic 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
- C07D295/06—Heterocyclic 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
- C07D295/067—Heterocyclic 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)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Agricultural Chemicals And Associated Chemicals (AREA)
Abstract
La presente solicitud se refiere a un proceso novedoso y eficiente para preparar {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil )-1H-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo de la fórmula (I) (ver Fórmula) (I) en la forma cristalina de la modificación I, donde el difractograma de rayos X del compuesto de la fórmula (I) en la modificación I presenta máximos pico del ángulo 2 theta en 5.9, 6.9, 22.7, de pureza muy alta, resultando significativamente más rentable que el proceso conocido en la técnica y pudiéndose obtener con equipamientos piloto y en plantas de producción tradicionales (depósitos de agitación/dispositivos para aislamiento).
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 |
---|---|
MX2022015952A true MX2022015952A (es) | 2023-01-24 |
Family
ID=71103286
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2022015952A MX2022015952A (es) | 2020-06-16 | 2021-06-15 | Proceso para preparar {4,6-diamino-2-[5-fluoro-1-(2-fluorobencil)- 1h-pirazolo[3,4-b]piridin-3-il]pirimidin-5-il}carbamato de metilo. |
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)
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 |
ES2956054A1 (es) * | 2022-05-03 | 2023-12-12 | 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)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
DE19834044A1 (de) | 1998-07-29 | 2000-02-03 | Bayer Ag | Neue substituierte Pyrazolderivate |
RS54433B1 (en) * | 2009-11-27 | 2016-04-28 | Adverio Pharma Gmbh | PROCEDURE FOR THE PRODUCTION OF METHYL- {4,6-DIAMINO-2- [1- (2-FLUOROBENZYL) -1H-PYRAZOLO [3,4-B] PYRIDIN-3-IL] PYRIMIDIN-5-IL} METHYLCARBAMATE AND ITS Purification thereof ITS USE AS A PHARMACEUTICAL AGENCY |
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 |
DE102010021637A1 (de) | 2010-05-26 | 2011-12-01 | Bayer Schering Pharma Aktiengesellschaft | Substituierte 5-Fluor-1H-Pyrazolopyridine und ihre Verwendung |
CN103038232B (zh) * | 2010-05-26 | 2016-01-20 | 阿德弗里奥药品有限责任公司 | 单独的和与PDE5抑制剂相组合的sGC刺激剂、sGC活化剂用于治疗系统性硬化症(SSc)的用途 |
DE102010040233A1 (de) * | 2010-09-03 | 2012-03-08 | Bayer Schering Pharma Aktiengesellschaft | Bicyclische Aza-Heterocyclen und ihre Verwendung |
PE20141582A1 (es) * | 2011-09-02 | 2014-11-06 | Bayer Ip Gmbh | Pirimidinas anilladas sustituidas y uso de las mismas |
HUE041592T2 (hu) * | 2011-11-25 | 2019-05-28 | Adverio Pharma Gmbh | Eljárás szubsztituált 5-fluor-1H-pirazolopiridinek elõállítására |
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 |
-
2020
- 2020-06-16 EP EP20180229.5A patent/EP3925953A1/en not_active Ceased
-
2021
- 2021-06-11 TW TW110121384A patent/TW202214625A/zh unknown
- 2021-06-15 EP EP21732878.0A patent/EP4165028A1/en active Pending
- 2021-06-15 MX MX2022015952A patent/MX2022015952A/es unknown
- 2021-06-15 US US18/001,834 patent/US20230219952A1/en active Pending
- 2021-06-15 JP JP2022577364A patent/JP2023530142A/ja active Pending
- 2021-06-15 KR KR1020237001194A patent/KR20230025862A/ko active Search and Examination
- 2021-06-15 BR BR112022023035A patent/BR112022023035A2/pt unknown
- 2021-06-15 WO PCT/EP2021/066019 patent/WO2021254981A1/en unknown
- 2021-06-15 AU AU2021294233A patent/AU2021294233A1/en active Pending
- 2021-06-15 CA CA3187147A patent/CA3187147A1/en active Pending
- 2021-06-15 CR CR20220647A patent/CR20220647A/es unknown
- 2021-06-15 IL IL298913A patent/IL298913A/en unknown
- 2021-06-15 CN CN202180043045.5A patent/CN115697978A/zh active Pending
- 2021-06-15 PE PE2022002944A patent/PE20231553A1/es unknown
- 2021-06-16 AR ARP210101637A patent/AR122635A1/es unknown
-
2022
- 2022-12-15 CO CONC2022/0018232A patent/CO2022018232A2/es unknown
- 2022-12-15 CL CL2022003600A patent/CL2022003600A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
EP3925953A1 (en) | 2021-12-22 |
JP2023530142A (ja) | 2023-07-13 |
CR20220647A (es) | 2023-03-03 |
CO2022018232A2 (es) | 2022-12-20 |
AU2021294233A1 (en) | 2022-12-22 |
CA3187147A1 (en) | 2021-12-23 |
TW202214625A (zh) | 2022-04-16 |
KR20230025862A (ko) | 2023-02-23 |
CL2022003600A1 (es) | 2023-04-28 |
PE20231553A1 (es) | 2023-10-03 |
CN115697978A (zh) | 2023-02-03 |
AR122635A1 (es) | 2022-09-28 |
US20230219952A1 (en) | 2023-07-13 |
BR112022023035A2 (pt) | 2022-12-27 |
IL298913A (en) | 2023-02-01 |
EP4165028A1 (en) | 2023-04-19 |
WO2021254981A1 (en) | 2021-12-23 |
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