JP2020536870A - アルファカルボキサミドピロリジン誘導体の調製方法 - Google Patents
アルファカルボキサミドピロリジン誘導体の調製方法 Download PDFInfo
- Publication number
- JP2020536870A JP2020536870A JP2020519296A JP2020519296A JP2020536870A JP 2020536870 A JP2020536870 A JP 2020536870A JP 2020519296 A JP2020519296 A JP 2020519296A JP 2020519296 A JP2020519296 A JP 2020519296A JP 2020536870 A JP2020536870 A JP 2020536870A
- Authority
- JP
- Japan
- Prior art keywords
- formula
- compound
- boc
- tert
- solution
- Prior art date
- Legal status (The legal status 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 status listed.)
- Withdrawn
Links
- 0 CC=C(COc1ccc([C@@]2NC(*)CC2)cc1)C(F)=CC Chemical compound CC=C(COc1ccc([C@@]2NC(*)CC2)cc1)C(F)=CC 0.000 description 7
- YCGMPAXMEBEMKS-UHFFFAOYSA-N CC(C)COC(N(C(CC1)C(OC)=O)C1c(cc1)ccc1OCc1ccccc1F)=O Chemical compound CC(C)COC(N(C(CC1)C(OC)=O)C1c(cc1)ccc1OCc1ccccc1F)=O YCGMPAXMEBEMKS-UHFFFAOYSA-N 0.000 description 1
- CJMXGRVFGINRRL-LBAQZLPGSA-N CC(C)COC(N([C@@H](CC1)C(N)=O)C1c(cc1)ccc1OCc(cccc1)c1F)=O Chemical compound CC(C)COC(N([C@@H](CC1)C(N)=O)C1c(cc1)ccc1OCc(cccc1)c1F)=O CJMXGRVFGINRRL-LBAQZLPGSA-N 0.000 description 1
- NIEMUMKRKYONDX-CABCVRRESA-N CC(C)COC(N([C@@H](CC1)C(OC)=O)[C@H]1c(cc1)ccc1O)=O Chemical compound CC(C)COC(N([C@@H](CC1)C(OC)=O)[C@H]1c(cc1)ccc1O)=O NIEMUMKRKYONDX-CABCVRRESA-N 0.000 description 1
- NFDARDIYMFTSRD-NRFANRHFSA-N CC(C)COC(N[C@@H](CCC(c(cc1)ccc1OCc1ccccc1)=O)C(OC)=O)=O Chemical compound CC(C)COC(N[C@@H](CCC(c(cc1)ccc1OCc1ccccc1)=O)C(OC)=O)=O NFDARDIYMFTSRD-NRFANRHFSA-N 0.000 description 1
- CZNBAUFYLUBFCC-UHFFFAOYSA-N CCCC(C1C)[O]1C(N(C(CC1)C(OC)=O)C1=O)=O Chemical compound CCCC(C1C)[O]1C(N(C(CC1)C(OC)=O)C1=O)=O CZNBAUFYLUBFCC-UHFFFAOYSA-N 0.000 description 1
- FFWQLZFIMNTUCZ-UHFFFAOYSA-N Fc1ccccc1CBr Chemical compound Fc1ccccc1CBr FFWQLZFIMNTUCZ-UHFFFAOYSA-N 0.000 description 1
- JESCETIFNOFKEU-DJNXLDHESA-N NC([C@H](CC1)NC1c(cc1)ccc1OCc1ccccc1F)=O Chemical compound NC([C@H](CC1)NC1c(cc1)ccc1OCc1ccccc1F)=O JESCETIFNOFKEU-DJNXLDHESA-N 0.000 description 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
- C07D207/10—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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/401—Proline; Derivatives thereof, e.g. captopril
-
- 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)
- Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyrrole Compounds (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762568651P | 2017-10-05 | 2017-10-05 | |
| US62/568,651 | 2017-10-05 | ||
| PCT/US2018/054661 WO2019071162A2 (en) | 2017-10-05 | 2018-10-05 | PROCESS FOR THE PREPARATION OF PYRROLIDINE ALPHA-CARBOXAMIDE DERIVATIVES |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020536870A true JP2020536870A (ja) | 2020-12-17 |
| JP2020536870A5 JP2020536870A5 (https=) | 2021-11-25 |
Family
ID=65995302
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020519296A Withdrawn JP2020536870A (ja) | 2017-10-05 | 2018-10-05 | アルファカルボキサミドピロリジン誘導体の調製方法 |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11192856B2 (https=) |
| EP (1) | EP3691634A4 (https=) |
| JP (1) | JP2020536870A (https=) |
| KR (1) | KR20200061381A (https=) |
| CN (1) | CN112153968A (https=) |
| AU (2) | AU2018346763A1 (https=) |
| CA (1) | CA3076823A1 (https=) |
| IL (1) | IL273639B2 (https=) |
| MA (1) | MA50630A (https=) |
| MX (1) | MX2020003811A (https=) |
| SG (2) | SG11202002706XA (https=) |
| WO (1) | WO2019071162A2 (https=) |
Families Citing this family (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11192856B2 (en) | 2017-10-05 | 2021-12-07 | Biogen Inc. | Process for preparing alpha-carboxamide pyrrolidine derivatives |
Citations (6)
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| JP2007290973A (ja) * | 2006-04-21 | 2007-11-08 | Univ Nagoya | 亜鉛−マグネシウムアート錯体を含む求核試薬及びそれを使用する求核付加体の製造方法 |
| JP2009511519A (ja) * | 2005-10-10 | 2009-03-19 | グラクソ グループ リミテッド | ナトリウムチャネルモジュレーターとしてのプロリンアミド誘導体 |
| JP5182088B2 (ja) * | 2006-04-19 | 2013-04-10 | アステラス製薬株式会社 | アゾールカルボキサミド誘導体 |
| JP2013513636A (ja) * | 2009-12-15 | 2013-04-22 | エフ.ホフマン−ラ ロシュ アーゲー | ピロリジン誘導体 |
| WO2016102967A1 (en) * | 2014-12-23 | 2016-06-30 | Convergence Pharmaceuticals Limited | Process for preparing alpha-carboxamide pyrrolidine derivatives |
| CN106467513A (zh) * | 2016-09-30 | 2017-03-01 | 陕西科技大学 | 一种制备Niraparib的合成方法 |
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| US3164597A (en) | 1962-12-17 | 1965-01-05 | Geigy Chem Corp | 5-carboxylic acid-2-phenyl-pyrrolines, corresponding pyrrolidines and functional derivatives thereof |
| CH674205A5 (https=) * | 1988-05-11 | 1990-05-15 | Lonza Ag | |
| IL94466A (en) | 1989-05-25 | 1995-01-24 | Erba Carlo Spa | Pharmaceutical preparations containing the history of A-amino carboxamide N-phenylalkyl are converted into such new compounds and their preparation |
| US6201016B1 (en) | 1994-06-27 | 2001-03-13 | Cytomed Incorporated | Compounds and methods for the treatment of cardiovascular, inflammatory and immune disorders |
| GB9618349D0 (en) | 1996-09-03 | 1996-10-16 | Pharmacia Spa | N-substituted 2-amino-4-phenyl-4-oxo-butanoic acid derivatives with kynurenine-3-hydroxylase inhibitory activity |
| IT1290910B1 (it) | 1997-02-03 | 1998-12-14 | Sigma Tau Ind Farmaceuti | 2-amminotetralina otticamente attiva, procedimento per la sua preparazione e composizioni farmaceutiche che la contengono, attive |
| GB9727523D0 (en) | 1997-12-31 | 1998-02-25 | Pharmacia & Upjohn Spa | Alpha-aminoamide derivatives useful as analgesic agents |
| TW502019B (en) | 1999-03-26 | 2002-09-11 | Cocensys Inc | Aryl substituted pyrazoles, imidazoles, oxazoles, thiazoles and pyrroles, and the use thereof |
| GB9923748D0 (en) | 1999-10-07 | 1999-12-08 | Glaxo Group Ltd | Chemical compounds |
| IT1317049B1 (it) | 2000-06-23 | 2003-05-26 | Sigma Tau Ind Farmaceuti | Composti utili per la preparazione di medicamenti ad attivita'inibitrice della fosfodiesterasi iv. |
| GB0115517D0 (en) | 2001-06-25 | 2001-08-15 | Ferring Bv | Novel antidiabetic agents |
| PE20050077A1 (es) | 2002-09-20 | 2005-03-01 | Hoffmann La Roche | Derivados de 4-pirrolidino-fenil-bencil-eter |
| MY142651A (en) | 2003-03-18 | 2010-12-15 | Merck Sharp & Dohme | Biaryl substituted triazoles as sodium channel blockers |
| US7589116B2 (en) | 2003-04-03 | 2009-09-15 | Merck & Co. Inc. | Biaryl substituted pyrazoles as sodium channel blockers |
| CA2522476A1 (en) | 2003-04-18 | 2004-11-04 | Merck & Co., Inc. | Biaryl substituted thiazoles, oxazoles and imidazoles as sodium channel blockers |
| WO2005000309A2 (en) | 2003-06-27 | 2005-01-06 | Ionix Pharmaceuticals Limited | Chemical compounds |
| EP1524265A1 (en) | 2003-10-15 | 2005-04-20 | Newron Pharmaceuticals S.p.A. | Prolinamide derivatives as sodium and/or calcium channel blockers or selective MAO-B inhibitors |
| WO2005110982A2 (en) | 2004-04-07 | 2005-11-24 | Neurogen Corporation | Substituted 1-benzyl-4-substituted piperazine analogues |
| WO2005100334A1 (en) | 2004-04-14 | 2005-10-27 | Pfizer Products Inc. | Dipeptidyl peptidase-iv inhibitors |
| JP2008540443A (ja) | 2005-05-04 | 2008-11-20 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なピリミジンおよびピラジン |
| WO2006119390A1 (en) | 2005-05-04 | 2006-11-09 | Vertex Pharmaceuticals Incorporated | Pyridines useful as modulators of ion channels |
| JP2008540665A (ja) | 2005-05-19 | 2008-11-20 | バーテックス ファーマシューティカルズ インコーポレイテッド | イオンチャネルのモジュレーターとして有用なビアリール |
| EA013909B1 (ru) | 2005-09-09 | 2010-08-30 | Смитклайн Бичам Корпорейшн | Пиридиновые производные и их применение для лечения психотических расстройств |
| TW200728258A (en) | 2005-10-10 | 2007-08-01 | Glaxo Group Ltd | Novel compounds |
| EP1943216B1 (en) | 2005-10-10 | 2010-06-30 | Glaxo Group Limited | Prolinamide derivatives as sodium channel modulators |
| GB0701366D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| EP2117538A1 (en) | 2007-01-24 | 2009-11-18 | Glaxo Group Limited | Pharmaceutical compositions comprising 2-methoxy-5- (5-trifluoromethyl-tetrazol-i-yl-benzyl) - (2s-phenyl-piperidin-3s-yl-) |
| GB0701365D0 (en) | 2007-01-24 | 2007-03-07 | Glaxo Group Ltd | Novel pharmaceutical compositions |
| GB0706630D0 (en) | 2007-04-04 | 2007-05-16 | Glaxo Group Ltd | Novel compounds |
| DK2477964T5 (en) | 2009-09-14 | 2015-05-26 | Convergence Pharmaceuticals | A process for the preparation of alpha-carboxamide |
| WO2011155337A1 (ja) | 2010-06-11 | 2011-12-15 | シャープ株式会社 | 液晶装置 |
| ES2428439T1 (es) * | 2010-11-11 | 2013-11-07 | Aarti Healthcare Limited | Un procedimiento para la preparación de Ramipril |
| WO2016160574A2 (en) | 2015-03-27 | 2016-10-06 | Scifluor Life Sciences, Inc. | Aryl- and heteroaryl-pyrrolidine-2-carboxamide compounds |
| US11192856B2 (en) | 2017-10-05 | 2021-12-07 | Biogen Inc. | Process for preparing alpha-carboxamide pyrrolidine derivatives |
| WO2020210486A1 (en) | 2019-04-10 | 2020-10-15 | Biogen Inc. | Processes for preparing alpha-carboxamide pyrrolidine derivatives |
| CN114026066A (zh) | 2019-04-10 | 2022-02-08 | 生物基因麻省公司 | 制备α-甲酰胺吡咯烷衍生物的方法 |
-
2018
- 2018-10-05 US US16/753,680 patent/US11192856B2/en not_active Expired - Fee Related
- 2018-10-05 SG SG11202002706XA patent/SG11202002706XA/en unknown
- 2018-10-05 SG SG10202112966SA patent/SG10202112966SA/en unknown
- 2018-10-05 WO PCT/US2018/054661 patent/WO2019071162A2/en not_active Ceased
- 2018-10-05 EP EP18864468.6A patent/EP3691634A4/en not_active Withdrawn
- 2018-10-05 CA CA3076823A patent/CA3076823A1/en not_active Withdrawn
- 2018-10-05 MA MA050630A patent/MA50630A/fr unknown
- 2018-10-05 AU AU2018346763A patent/AU2018346763A1/en not_active Abandoned
- 2018-10-05 KR KR1020207011959A patent/KR20200061381A/ko not_active Withdrawn
- 2018-10-05 CN CN201880078496.0A patent/CN112153968A/zh not_active Withdrawn
- 2018-10-05 MX MX2020003811A patent/MX2020003811A/es unknown
- 2018-10-05 JP JP2020519296A patent/JP2020536870A/ja not_active Withdrawn
-
2020
- 2020-03-26 IL IL273639A patent/IL273639B2/en unknown
-
2021
- 2021-11-24 US US17/534,679 patent/US20220356154A1/en not_active Abandoned
-
2023
- 2023-06-26 AU AU2023204011A patent/AU2023204011A1/en not_active Withdrawn
Patent Citations (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2009511519A (ja) * | 2005-10-10 | 2009-03-19 | グラクソ グループ リミテッド | ナトリウムチャネルモジュレーターとしてのプロリンアミド誘導体 |
| JP5182088B2 (ja) * | 2006-04-19 | 2013-04-10 | アステラス製薬株式会社 | アゾールカルボキサミド誘導体 |
| JP2007290973A (ja) * | 2006-04-21 | 2007-11-08 | Univ Nagoya | 亜鉛−マグネシウムアート錯体を含む求核試薬及びそれを使用する求核付加体の製造方法 |
| JP2013513636A (ja) * | 2009-12-15 | 2013-04-22 | エフ.ホフマン−ラ ロシュ アーゲー | ピロリジン誘導体 |
| WO2016102967A1 (en) * | 2014-12-23 | 2016-06-30 | Convergence Pharmaceuticals Limited | Process for preparing alpha-carboxamide pyrrolidine derivatives |
| CN106467513A (zh) * | 2016-09-30 | 2017-03-01 | 陕西科技大学 | 一种制备Niraparib的合成方法 |
Non-Patent Citations (5)
| Title |
|---|
| CHAO-SHAN DA; ET AL: "HIGHLY CATALYTIC ASYMMETRIC ADDITION OF DEACTIVATED ALKYL GRIGNARD REAGENTS TO ALDEHYDES", ORGANIC LETTERS, vol. VOL:11, NR:24, JPN5021001659, 2009, pages 5578 - 5581, ISSN: 0004915424 * |
| JOURNAL OF FLOW CHEMISTRY, vol. 4, JPN5021001657, 2014, pages 40 - 43, ISSN: 0005124050 * |
| ORGANIC PROCESS RESEARCH & DEVELOPMENT, vol. 17, JPN5021001655, 2013, pages 1192 - 1208, ISSN: 0005124049 * |
| 井上 淳、他: "有機マグネシウム反応剤を用いた新規合成反応の開拓", 有機合成化学協会誌, vol. 61, JPN7022005200, 2003, pages 331 - 342, ISSN: 0005124046 * |
| 佐藤 健太郎: "ターボGrignard試薬の展開", WAKO ORGANIC SQUARE, JPN7022005201, 2013, pages 2 - 5, ISSN: 0005124047 * |
Also Published As
| Publication number | Publication date |
|---|---|
| AU2023204011A1 (en) | 2023-07-13 |
| WO2019071162A2 (en) | 2019-04-11 |
| IL273639B1 (en) | 2023-03-01 |
| IL273639A (en) | 2020-05-31 |
| CA3076823A1 (en) | 2019-04-11 |
| US11192856B2 (en) | 2021-12-07 |
| EP3691634A2 (en) | 2020-08-12 |
| SG11202002706XA (en) | 2020-04-29 |
| MA50630A (fr) | 2021-03-31 |
| CN112153968A (zh) | 2020-12-29 |
| MX2020003811A (es) | 2021-01-15 |
| IL273639B2 (en) | 2023-07-01 |
| EP3691634A4 (en) | 2021-03-31 |
| US20200270206A1 (en) | 2020-08-27 |
| SG10202112966SA (en) | 2021-12-30 |
| WO2019071162A3 (en) | 2020-03-26 |
| AU2018346763A1 (en) | 2020-04-16 |
| KR20200061381A (ko) | 2020-06-02 |
| US20220356154A1 (en) | 2022-11-10 |
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