AR088564A1 - PROCESO PARA LA PREPARACION DE AGONISTAS Y COMPUESTOS INTERMEDIOS DE b3 - Google Patents
PROCESO PARA LA PREPARACION DE AGONISTAS Y COMPUESTOS INTERMEDIOS DE b3Info
- Publication number
- AR088564A1 AR088564A1 ARP120104036A ARP120104036A AR088564A1 AR 088564 A1 AR088564 A1 AR 088564A1 AR P120104036 A ARP120104036 A AR P120104036A AR P120104036 A ARP120104036 A AR P120104036A AR 088564 A1 AR088564 A1 AR 088564A1
- Authority
- AR
- Argentina
- Prior art keywords
- compound
- formula
- produce
- catalyst
- reduction
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 16
- 238000000034 method Methods 0.000 title abstract 2
- 239000000556 agonist Substances 0.000 title 1
- 239000003054 catalyst Substances 0.000 abstract 3
- 238000006243 chemical reaction Methods 0.000 abstract 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 abstract 2
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 1
- 125000003088 (fluoren-9-ylmethoxy)carbonyl group Chemical group 0.000 abstract 1
- FGQLGYBGTRHODR-UHFFFAOYSA-N 2,2-diethoxypropane Chemical compound CCOC(C)(C)OCC FGQLGYBGTRHODR-UHFFFAOYSA-N 0.000 abstract 1
- HEWZVZIVELJPQZ-UHFFFAOYSA-N 2,2-dimethoxypropane Chemical compound COC(C)(C)OC HEWZVZIVELJPQZ-UHFFFAOYSA-N 0.000 abstract 1
- YOWQWFMSQCOSBA-UHFFFAOYSA-N 2-methoxypropene Chemical compound COC(C)=C YOWQWFMSQCOSBA-UHFFFAOYSA-N 0.000 abstract 1
- QWOJMRHUQHTCJG-UHFFFAOYSA-N CC([CH2-])=O Chemical compound CC([CH2-])=O QWOJMRHUQHTCJG-UHFFFAOYSA-N 0.000 abstract 1
- 229910019142 PO4 Inorganic materials 0.000 abstract 1
- 239000002253 acid Substances 0.000 abstract 1
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 abstract 1
- 239000003153 chemical reaction reagent Substances 0.000 abstract 1
- 239000003638 chemical reducing agent Substances 0.000 abstract 1
- 239000007800 oxidant agent Substances 0.000 abstract 1
- 230000003647 oxidation Effects 0.000 abstract 1
- 238000007254 oxidation reaction Methods 0.000 abstract 1
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 abstract 1
- 239000010452 phosphate Substances 0.000 abstract 1
- -1 phosphate compound Chemical class 0.000 abstract 1
- 230000001681 protective effect Effects 0.000 abstract 1
- 239000002904 solvent Substances 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
- C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
-
- 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
- C12—BIOCHEMISTRY; BEER; SPIRITS; WINE; VINEGAR; MICROBIOLOGY; ENZYMOLOGY; MUTATION OR GENETIC ENGINEERING
- C12P—FERMENTATION OR ENZYME-USING PROCESSES TO SYNTHESISE A DESIRED CHEMICAL COMPOUND OR COMPOSITION OR TO SEPARATE OPTICAL ISOMERS FROM A RACEMIC MIXTURE
- C12P17/00—Preparation of heterocyclic carbon compounds with only O, N, S, Se or Te as ring hetero atoms
- C12P17/10—Nitrogen as only ring hetero atom
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Wood Science & Technology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Engineering & Computer Science (AREA)
- Zoology (AREA)
- Health & Medical Sciences (AREA)
- General Engineering & Computer Science (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biotechnology (AREA)
- Biochemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Microbiology (AREA)
- General Health & Medical Sciences (AREA)
- Genetics & Genomics (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
- Pyrrole Compounds (AREA)
- Catalysts (AREA)
Abstract
Reivindicación 1: Un proceso para la preparación del compuesto de fórmula (1), que comprende: (a) reacción del compuesto de fórmula (2), con un reactivo protector de acetonida seleccionado entre el grupo que consiste en 2,2-dimetoxipropano, 2,2-dietoxipropano, 2-metoxipropeno y acetona, para producir el compuesto de fórmula (3); (b) reducción del compuesto de fórmula (3) con un agente reductor a una temperatura de 0ºC a 40ºC para producir el compuesto de fórmula (4); (c) oxidación del compuesto de fórmula (4) con un agente oxidante en presencia de un disolvente y de un catalizador para producir el compuesto de fórmula (5); (d) reacción del compuesto de fórmula (5) con un compuesto de fosfato de fórmula (6) para producir el compuesto de fórmula (7); (e) reducción del compuesto de fórmula (7) en presencia de un catalizador para producir el compuesto (8); (f) reacción del compuesto de fórmula (8) con un ácido para producir el compuesto de fórmula (9); (g) reducción del compuesto de fórmula (9) en presencia de un catalizador para producir el compuesto de fórmula (1); en el que cada uno de P¹ y P² se selecciona independientemente entre el grupo que consiste en Ac, Bn, Boc, Bz, Cbz, DMPM, FMOC, Ns, Moz, y Ts; y R¹ se selecciona entre el grupo que consiste en alquilo C₁₋₆, bencilo y fenilo.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201161552200P | 2011-10-27 | 2011-10-27 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR088564A1 true AR088564A1 (es) | 2014-06-18 |
Family
ID=48168357
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP120104036A AR088564A1 (es) | 2011-10-27 | 2012-10-26 | PROCESO PARA LA PREPARACION DE AGONISTAS Y COMPUESTOS INTERMEDIOS DE b3 |
Country Status (7)
| Country | Link |
|---|---|
| US (4) | US9809536B2 (es) |
| EP (1) | EP2771006B1 (es) |
| JP (1) | JP6088535B2 (es) |
| AR (1) | AR088564A1 (es) |
| ES (1) | ES2584427T3 (es) |
| TW (1) | TW201323406A (es) |
| WO (1) | WO2013062878A1 (es) |
Families Citing this family (16)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2770996B1 (en) | 2011-10-27 | 2016-09-28 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| WO2013062878A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Process for making beta 3 angonists and intermediates |
| HUE045260T2 (hu) | 2013-03-15 | 2019-12-30 | Merck Sharp & Dohme | Eljárás béta 3 antagonisták és köztitermékeik elõállítására |
| WO2018224990A1 (en) | 2017-06-06 | 2018-12-13 | Urovant Sciences Gmbh | Dosing of vibegron for treatment of overactive bladder |
| CN117695287A (zh) | 2017-06-06 | 2024-03-15 | 住友制药(苏州)有限公司 | 使用维贝隆以治疗膀胱过度活动症 |
| AU2019273837A1 (en) | 2018-05-23 | 2020-11-19 | Urovant Sciences Gmbh | Use of vibegron to treat pain associated with irritable bowel syndrome |
| MX2021003980A (es) | 2018-12-05 | 2021-07-21 | Urovant Sciences Gmbh | Vibegrón para el tratamiento de los síntomas de la vejiga hiperactiva. |
| TW202506129A (zh) | 2019-03-18 | 2025-02-16 | 瑞士商優洛凡特科學公司 | 維貝隆（ｖｉｂｅｇｒｏｎ）用於治療膀胱過動症之用途 |
| CN114096662B (zh) | 2019-05-01 | 2025-04-15 | 科德克希思公司 | 工程化葡萄糖脱氢酶和用于酮和胺化合物的还原胺化的方法 |
| CN114746745B (zh) * | 2019-10-02 | 2025-06-17 | 美国雅培糖尿病护理公司 | 通过蛋白质开关检测分析物 |
| CN112708644B (zh) * | 2019-10-25 | 2024-05-28 | 弈柯莱生物科技(集团)股份有限公司 | 氟苯尼考中间体的制备方法 |
| CN112176007B (zh) * | 2020-10-12 | 2022-07-22 | 上海医药工业研究院 | 一种氨基醇手性中间体的制备方法 |
| US20240050457A1 (en) | 2020-12-22 | 2024-02-15 | Urovant Sciences Gmbh | Methods of monitoring digoxin with concomitant use of vibegron to treat overactive bladder |
| TW202245781A (zh) | 2021-02-16 | 2022-12-01 | 瑞士商優洛凡特科學公司 | 用維貝格龍（ｖｉｂｅｇｒｏｎ）治療心臟衰竭之方法 |
| GB202113588D0 (en) * | 2021-09-23 | 2021-11-10 | Atrogi Ab | New compounds and methods |
| CN113816917B (zh) * | 2021-11-19 | 2022-02-18 | 奥锐特药业(天津)有限公司 | 一种维贝格龙中间体的制备方法 |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6525202B2 (en) | 2000-07-17 | 2003-02-25 | Wyeth | Cyclic amine phenyl beta-3 adrenergic receptor agonists |
| DOP2003000587A (es) | 2002-02-27 | 2003-08-30 | Pfizer Prod Inc | AGONISTAS DEL RECEPTOR ß3-ADRENERGICO |
| FR2874011B1 (fr) | 2004-08-03 | 2007-06-15 | Sanofi Synthelabo | Derives de sulfonamides, leur preparation et leur application en therapeutique |
| EP2198018B1 (en) * | 2007-09-13 | 2013-11-20 | Codexis, Inc. | Ketoreductase polypeptides for the reduction of acetophenones |
| PE20091825A1 (es) | 2008-04-04 | 2009-12-04 | Merck & Co Inc | Hidroximetil pirrolidinas como agonistas del receptor adrenergico beta 3 |
| CN102186972B (zh) | 2008-08-29 | 2014-08-20 | 科德克希思公司 | 用于立体选择性生产(4s)-3-[(5s)-5-(4-氟苯基)-5-羟基戊酰基]-4-苯基-1，3-噁唑烷-2-酮的酮还原酶多肽 |
| EP2485595A4 (en) | 2009-10-07 | 2014-03-12 | Merck Sharp & Dohme | COMBINATION THERAPY WITH AN ADRENERGIC BETA-3 RECEPTOR AGONIST AND ANTIMIC CARCINU |
| US8748433B2 (en) | 2010-04-30 | 2014-06-10 | Merck Sharp & Dohme Corp. | β3 adrenergic receptor agonists |
| WO2013062878A1 (en) | 2011-10-27 | 2013-05-02 | Merck Sharp & Dohme Corp. | Process for making beta 3 angonists and intermediates |
| EP2770996B1 (en) | 2011-10-27 | 2016-09-28 | Merck Sharp & Dohme Corp. | Process for making beta 3 agonists and intermediates |
| EP2780448B1 (en) | 2011-11-18 | 2019-09-11 | Codexis, Inc. | Biocatalysts for the preparation of hydroxy substituted carbamates |
| HUE045260T2 (hu) | 2013-03-15 | 2019-12-30 | Merck Sharp & Dohme | Eljárás béta 3 antagonisták és köztitermékeik elõállítására |
-
2012
- 2012-10-22 WO PCT/US2012/061249 patent/WO2013062878A1/en not_active Ceased
- 2012-10-22 ES ES12842776.2T patent/ES2584427T3/es active Active
- 2012-10-22 EP EP12842776.2A patent/EP2771006B1/en active Active
- 2012-10-22 US US14/354,161 patent/US9809536B2/en active Active
- 2012-10-22 JP JP2014538852A patent/JP6088535B2/ja active Active
- 2012-10-26 AR ARP120104036A patent/AR088564A1/es active IP Right Grant
- 2012-10-26 TW TW101139811A patent/TW201323406A/zh unknown
-
2017
- 2017-09-26 US US15/715,493 patent/US10577316B2/en active Active
-
2020
- 2020-02-20 US US16/795,745 patent/US11124478B2/en active Active
-
2021
- 2021-09-17 US US17/478,601 patent/US11767292B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| US10577316B2 (en) | 2020-03-03 |
| JP6088535B2 (ja) | 2017-03-08 |
| US20220073459A1 (en) | 2022-03-10 |
| US20180029981A1 (en) | 2018-02-01 |
| US20200290962A1 (en) | 2020-09-17 |
| US11124478B2 (en) | 2021-09-21 |
| JP2015501319A (ja) | 2015-01-15 |
| EP2771006A1 (en) | 2014-09-03 |
| EP2771006B1 (en) | 2016-05-25 |
| US9809536B2 (en) | 2017-11-07 |
| WO2013062878A1 (en) | 2013-05-02 |
| EP2771006A4 (en) | 2015-04-15 |
| US11767292B2 (en) | 2023-09-26 |
| US20140242645A1 (en) | 2014-08-28 |
| ES2584427T3 (es) | 2016-09-27 |
| TW201323406A (zh) | 2013-06-16 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant, registration |