BR112022012153A2 - Processo para preparar um composto e composto - Google Patents
Processo para preparar um composto e compostoInfo
- Publication number
- BR112022012153A2 BR112022012153A2 BR112022012153A BR112022012153A BR112022012153A2 BR 112022012153 A2 BR112022012153 A2 BR 112022012153A2 BR 112022012153 A BR112022012153 A BR 112022012153A BR 112022012153 A BR112022012153 A BR 112022012153A BR 112022012153 A2 BR112022012153 A2 BR 112022012153A2
- Authority
- BR
- Brazil
- Prior art keywords
- compound
- preparing
- compounds
- upadacitinib
- weinreb
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 238000004519 manufacturing process Methods 0.000 title abstract 2
- 239000000543 intermediate Substances 0.000 abstract 2
- WYQFJHHDOKWSHR-MNOVXSKESA-N (3S,4R)-3-ethyl-4-(1,5,7,10-tetrazatricyclo[7.3.0.02,6]dodeca-2(6),3,7,9,11-pentaen-12-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide Chemical compound CC[C@@H]1CN(C(=O)NCC(F)(F)F)C[C@@H]1C1=CN=C2N1C(C=CN1)=C1N=C2 WYQFJHHDOKWSHR-MNOVXSKESA-N 0.000 abstract 1
- UTZVSIXTYYWUOB-USJZOSNVSA-N 2-[(1s,2s,4as,8as)-2-hydroxy-2,5,5,8a-tetramethyl-3,4,4a,6,7,8-hexahydro-1h-naphthalen-1-yl]-n-methoxy-n-methylacetamide Chemical compound CC1(C)CCC[C@]2(C)[C@H](CC(=O)N(C)OC)[C@@](C)(O)CC[C@H]21 UTZVSIXTYYWUOB-USJZOSNVSA-N 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 238000002360 preparation method Methods 0.000 abstract 1
- 238000003786 synthesis reaction Methods 0.000 abstract 1
- 229950000088 upadacitinib Drugs 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
- C07D207/10—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members 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
- C07D207/16—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/20—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/18—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D207/22—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member 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
- C07D207/24—Oxygen or sulfur atoms
- C07D207/26—2-Pyrrolidones
- C07D207/273—2-Pyrrolidones 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 other ring carbon atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
- C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
- C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/12—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains three hetero rings
- C07D487/14—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
- C07F7/1804—Compounds having Si-O-C linkages
- C07F7/1872—Preparation; Treatments not provided for in C07F7/20
- C07F7/188—Preparation; Treatments not provided for in C07F7/20 by reactions involving the formation of Si-O linkages
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
PROCESSO PARA PREPARAR UM COMPOSTO E COMPOSTO. A invenção se refere a um processo para a preparação de compostos de fórmula (I), que são intermediários úteis na síntese de Upadacitinibe e compostos estruturalmente relacionados, usando amida de Weinreb (III), ou um equivalente da mesma, como intermediário chave.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19383150 | 2019-12-19 | ||
| PCT/EP2020/087194 WO2021123288A1 (en) | 2019-12-19 | 2020-12-18 | Process and intermediates for the preparation of upadacitinib |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BR112022012153A2 true BR112022012153A2 (pt) | 2022-08-30 |
Family
ID=69411198
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BR112022012153A BR112022012153A2 (pt) | 2019-12-19 | 2020-12-18 | Processo para preparar um composto e composto |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US12552746B2 (pt) |
| EP (1) | EP4077276A1 (pt) |
| JP (1) | JP7648027B2 (pt) |
| KR (1) | KR20220118522A (pt) |
| CN (1) | CN115151529B (pt) |
| BR (1) | BR112022012153A2 (pt) |
| WO (1) | WO2021123288A1 (pt) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN111909160B (zh) * | 2019-05-09 | 2024-05-28 | 苏州鹏旭医药科技有限公司 | 一种乌帕替尼盐类化合物及其制备方法 |
| WO2022044037A1 (en) * | 2020-08-24 | 2022-03-03 | Mylan Laboratories Limited | An improved process for the preparation of upadacitinib intermediate |
| CN114621127A (zh) * | 2020-12-08 | 2022-06-14 | 苏州鹏旭医药科技有限公司 | 一种取代二氢吡咯的合成方法 |
| CN117285537B (zh) * | 2023-11-27 | 2024-02-06 | 中节能万润股份有限公司 | 一种乌帕替尼的制备方法 |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2543667B1 (en) | 2006-03-24 | 2015-01-28 | Array Biopharma, Inc. | A method of preparing 2-aminopyridine analogs as glucokinase activators |
| CA2681695A1 (en) | 2007-03-23 | 2008-10-02 | Array Biopharma Inc. | 2-aminopyridine analogs as glucokinase activators |
| JP2010006722A (ja) | 2008-06-25 | 2010-01-14 | Hokko Chem Ind Co Ltd | ピリダジン誘導体および殺菌剤 |
| JP5607174B2 (ja) | 2009-12-01 | 2014-10-15 | アッヴィ・インコーポレイテッド | 新規な三環式化合物 |
| US20130072470A1 (en) | 2011-09-21 | 2013-03-21 | Abbvie Inc. | Novel tricyclic compounds |
| JP6407108B2 (ja) | 2015-07-06 | 2018-10-17 | ユニ・チャーム株式会社 | 吸収性物品及び吸収性物品の製造方法 |
| BR112018000254A2 (pt) | 2015-07-07 | 2018-09-04 | H Lundbeck As | inibidores de pde9 com cadeia principal de imidazotriazinona e cadeia principal de imidazopirazinona para o tratamento de doenças periféricas |
| US10550126B2 (en) * | 2015-10-16 | 2020-02-04 | Abbvie Inc. | Processes for the preparation of (3S,4R)-3-ethyl-4-(3H-imidazo[1,2-A]pyrrolo[2,3-e]-pyrazin-8-yl)-N-(2,2,2-trifluoroethyl)pyrrolidine-1-carboxamide and solid state forms thereof |
| SG10201913999PA (en) | 2015-10-16 | 2020-03-30 | Abbvie Inc | PROCESSES FOR THE PREPARATION OF (3S,4R)-3-ETHYL-4-(3H-IMIDAZO[1,2-a]PYRROLO[2,3-e]-PYRAZIN-8-YL)-N-(2,2,2-TRIFLUOROETHYL)PYRROLIDINE-1-CARBOXAMIDE AND SOLID STATE FORMS THEREOF |
| WO2017066975A1 (zh) | 2015-10-23 | 2017-04-27 | 揭东巴黎万株纱华纺织有限公司 | 一种有色阻燃聚酯纤维制备工艺 |
| AU2017292650A1 (en) | 2016-07-06 | 2018-12-13 | H. Lundbeck A/S | PDE9 inhibitors for treatment of peripheral diseases |
| US20210163409A1 (en) | 2017-07-19 | 2021-06-03 | Dr. Reddy's Laboratories Limited | Alternate processes for the preparation of pyrrolidine derivatives |
| MA52482B1 (fr) * | 2018-05-01 | 2024-12-31 | Merck Sharp & Dohme Llc | Dérivés de spiropipéridine en tant que modulateurs allostériques des récepteurs nicotiniques de l'acétylcholine |
| CN110872250B (zh) * | 2018-08-31 | 2023-01-10 | 苏州鹏旭医药科技有限公司 | 两种化合物及其制备方法和在合成乌西替尼中的用途 |
| HUE069611T2 (hu) | 2018-08-31 | 2025-03-28 | Suzhou Pengxu Pharmatech Co Ltd | Eljárások upadacitinib és intermedierjei szintézisére |
| CN109369659B (zh) | 2018-12-06 | 2020-10-27 | 浙江师范大学 | 一种jak抑制剂的合成方法 |
| WO2020202183A1 (en) | 2019-03-29 | 2020-10-08 | Mylan Laboratories Limited | The process for the preparation of upadacitinib and its intermediates |
-
2020
- 2020-12-18 JP JP2022537689A patent/JP7648027B2/ja active Active
- 2020-12-18 KR KR1020227025097A patent/KR20220118522A/ko active Pending
- 2020-12-18 US US17/787,000 patent/US12552746B2/en active Active
- 2020-12-18 BR BR112022012153A patent/BR112022012153A2/pt unknown
- 2020-12-18 EP EP20838039.4A patent/EP4077276A1/en active Pending
- 2020-12-18 WO PCT/EP2020/087194 patent/WO2021123288A1/en not_active Ceased
- 2020-12-18 CN CN202080093160.9A patent/CN115151529B/zh active Active
Also Published As
| Publication number | Publication date |
|---|---|
| WO2021123288A1 (en) | 2021-06-24 |
| JP7648027B2 (ja) | 2025-03-18 |
| US12552746B2 (en) | 2026-02-17 |
| CN115151529A (zh) | 2022-10-04 |
| JP2023510111A (ja) | 2023-03-13 |
| EP4077276A1 (en) | 2022-10-26 |
| US20230139156A1 (en) | 2023-05-04 |
| CN115151529B (zh) | 2025-04-22 |
| KR20220118522A (ko) | 2022-08-25 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| B06W | Patent application suspended after preliminary examination (for patents with searches from other patent authorities) chapter 6.23 patent gazette] |