AR113748A1 - Proceso estereoselectivo para preparar derivados de piridona policíclicos sustituidos - Google Patents
Proceso estereoselectivo para preparar derivados de piridona policíclicos sustituidosInfo
- Publication number
- AR113748A1 AR113748A1 ARP180102884A ARP180102884A AR113748A1 AR 113748 A1 AR113748 A1 AR 113748A1 AR P180102884 A ARP180102884 A AR P180102884A AR P180102884 A ARP180102884 A AR P180102884A AR 113748 A1 AR113748 A1 AR 113748A1
- Authority
- AR
- Argentina
- Prior art keywords
- hydrogen
- compound
- formula
- group
- protecting group
- Prior art date
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Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/12—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains three hetero rings
- C07D498/14—Ortho-condensed systems
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- 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
- A61K31/535—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
- C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C215/04—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated
- C07C215/06—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic
- C07C215/10—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being saturated and acyclic with one amino group and at least two hydroxy groups bound to the carbon skeleton
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C217/00—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
- C07C217/02—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
- C07C217/04—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated
- C07C217/06—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted
- C07C217/08—Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton having etherified hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being acyclic and saturated having only one etherified hydroxy group and one amino group bound to the carbon skeleton, which is not further substituted the oxygen atom of the etherified hydroxy group being further bound to an acyclic carbon atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
- C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
- C07D213/89—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members with hetero atoms directly attached to the ring nitrogen atom
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/34—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D309/36—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with oxygen atoms directly attached to ring carbon atoms
- C07D309/40—Oxygen atoms attached in positions 3 and 4, e.g. maltol
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/13—Crystalline forms, e.g. polymorphs
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- 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)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Pyridine Compounds (AREA)
- Pyrane Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Preparation Of Compounds By Using Micro-Organisms (AREA)
Abstract
Reivindicación 1: Un proceso para preparar un compuesto de la fórmula (7) o una de sus sales, en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; X es O ó CH₂; caracterizado por remover -RA de un compuesto de la fórmula (4), en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; RA¹ es hidrógeno o RA; RA² es hidrógeno o RA; RA³ es hidrógeno o RA; X es O, CH₂ o CHRA; RA es un grupo funcional removible; y el átomo de carbono al que se liga RA es ópticamente activo; siempre que uno de RA¹, RA² y RA³ sea RA, los otros dos son hidrógeno y X es O ó CH₂ o RA¹, RA² y RA³ son hidrógeno y X es CHRA. Reivindicación 2: Un proceso para preparar un compuesto de la fórmula (4) o una de sus sales, en donde cada símbolo es como se define más abajo; caracterizado por someter un compuesto de la fórmula (3) a una reacción intramolecular de ciclación, en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; RA¹ es hidrógeno o RA; RA² es hidrógeno o RA; RA³ es hidrógeno o RA; X es O, CH₂ o CHRA; RA es un grupo funcional removible y el átomo de carbono al que se liga RA es ópticamente activo; siempre que uno de RA¹, RA² y RA³ sea RA, los otros dos son hidrógeno y X es O ó CH₂ o RA¹, RA² y RA³ son hidrógeno y X es CHRA; R⁷ es NH₂ o NHR²; R² es un grupo protector para grupo amino; R⁸ es -CHO o -CH(OR⁴)(OR⁴); R⁴ cada uno es, de modo independiente, hidrógeno o un grupo protector desprotegible por un ácido o dos R⁴ se pueden tomar juntos para formar un anillo. Reivindicación 5: Un proceso para preparar un compuesto de la fórmula (3) o una de sus sales, en donde cada símbolo es como se define más abajo; caracterizado por la reacción de un compuesto de la fórmula (1a), en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; R⁷ es NH₂ o NHR²; R² es un grupo protector para grupo amino; con un compuesto de la fórmula (2), en donde RA¹ es hidrógeno o RA; RA² es hidrógeno o RA; RA³ es hidrógeno o RA; X es O, CH₂ o CHRA; RA es un grupo funcional removible y el átomo de carbono al que se liga RA es ópticamente activo; siempre que uno de RA¹, RA² y RA³ sea RA, los otros dos son hidrógeno y X es O ó CH₂ o RA¹, RA² y RA³ son hidrógeno y X es CHRA; R⁸ es -CHO o -CH(OR⁴)(OR⁴); R⁴ cada uno es, de modo independiente, hidrógeno o un grupo protector desprotegible por un ácido o dos R⁴ se pueden tomar juntos para formar un anillo. Reivindicación 6: Un proceso para preparar un compuesto de la fórmula (4) o una de sus sales, en donde cada símbolo es como se define más abajo; caracterizado por someter un compuesto de la fórmula (6) a una reacción intramolecular de ciclación, en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; RA¹ es hidrógeno o RA; RA² es hidrógeno o RA; RA³ es hidrógeno o RA; X es O, CH₂ o CHRA; RA es un grupo funcional removible y el átomo de carbono al que se liga RA es ópticamente activo; siempre que uno de RA¹, RA² y RA³ sea RA, los otros dos son hidrógeno y X es O ó CH₂ o RA¹, RA² y RA³ son hidrógeno y X es CHRA; R³ es un grupo protector para grupo carboxilo; R⁵ es hidrógeno o un grupo protector para grupo amino. Reivindicación 9: Un proceso para preparar un compuesto de la fórmula (6) o una de sus sales, en donde cada símbolo es como se define más abajo; caracterizado por la reacción de un compuesto de la fórmula (1b), en donde R¹ es hidrógeno o un grupo protector para grupo hidroxilo; R³ es un grupo protector para grupo carboxilo; con un compuesto de la fórmula (5), en donde R⁵ es un grupo protector para grupo amino; R⁶ es alquilo sustituido o no sustituido o carbociclilo aromático sustituido o no sustituido; RA¹ es hidrógeno o RA; RA² es hidrógeno o RA; RA³ es hidrógeno o RA; X es O, CH₂ o CHRA; RA es un grupo funcional removible y el átomo de carbono al que se liga RA es ópticamente activo; siempre que uno de RA¹, RA² y RA³ sea RA, los otros dos son hidrógeno y X es O ó CH; o RA¹, RA² y RA³ son hidrógeno y X es CHRA. Reivindicación 11: Un proceso para preparar un compuesto de la fórmula (8) o una de sus sales, en donde cada símbolo es como se define más abajo, caracterizado porque comprende (Etapa 1) hacer reaccionar un compuesto de la fórmula (9), en donde R¹ᵃ es un grupo protector para grupo hidroxilo excepto carbociclilalquilo aromático opcionalmente sustituido y heterociclilalquilo aromático opcionalmente sustituido, con un agente de halogenación para obtener un compuesto de la fórmula (10), en donde Z¹ es halógeno y los otros símbolos son como se definieron con anterioridad; (Etapa 2) hacer reaccionar el compuesto de la fórmula (10) con ión hidróxido para obtener un compuesto de la fórmula (11), en donde cada símbolo es como se definió con anterioridad; y (Etapa 3) hacer reaccionar el compuesto de la fórmula (11) con un agente oxidante para obtener el compuesto de la fórmula (8).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2017195802 | 2017-10-06 |
Publications (1)
Publication Number | Publication Date |
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AR113748A1 true AR113748A1 (es) | 2020-06-10 |
Family
ID=65995109
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP180102884A AR113748A1 (es) | 2017-10-06 | 2018-10-05 | Proceso estereoselectivo para preparar derivados de piridona policíclicos sustituidos |
Country Status (13)
Country | Link |
---|---|
US (2) | US11286262B2 (es) |
EP (1) | EP3693373A4 (es) |
JP (1) | JP6924839B2 (es) |
KR (1) | KR20200066644A (es) |
CN (1) | CN111386276B (es) |
AR (1) | AR113748A1 (es) |
AU (1) | AU2018344739B2 (es) |
BR (1) | BR112020006639A2 (es) |
CA (1) | CA3078442A1 (es) |
IL (1) | IL273821B2 (es) |
MX (1) | MX2020003469A (es) |
SG (1) | SG11202002789XA (es) |
WO (1) | WO2019070059A1 (es) |
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CN109912553A (zh) * | 2019-04-19 | 2019-06-21 | 山东百诺医药股份有限公司 | 一种中间体及其制备方法 |
CN110105372B (zh) * | 2019-06-05 | 2022-05-10 | 南京焕然生物科技有限公司 | 一种r-7-(苄氧基)-四氢-1h-恶嗪并吡啶并-三嗪-6,8-二酮的制备方法 |
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CN113072454B (zh) * | 2021-04-09 | 2022-03-04 | 南京正济医药研究有限公司 | 一种氧代乙胺化合物的新晶型 |
CN113845502A (zh) * | 2021-11-29 | 2021-12-28 | 山东诚创蓝海医药科技有限公司 | 一种3-(苄氧基)-4-氧代-4h-吡喃-2-羧酸的制备方法 |
CN114014874B (zh) * | 2021-12-20 | 2023-04-28 | 中国科学院上海药物研究所 | 一种玛巴洛沙韦中间体的制备方法 |
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CN114315957B (zh) * | 2021-12-30 | 2023-07-07 | 深圳瑞德林生物技术有限公司 | 一种多肽的制备方法 |
CN114436879A (zh) * | 2022-01-14 | 2022-05-06 | 海南三帝制药有限公司 | 一种盐酸三甲卡因的制备方法 |
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CN107923376B (zh) | 2015-08-20 | 2020-07-03 | 豪格绍尔压缩机公司 | 往复式活塞压缩机、用于往复式活塞压缩机的备件套装和连接杆在往复式活塞压缩机中的应用 |
WO2017087256A1 (en) | 2015-11-17 | 2017-05-26 | Merck Sharp & Dohme Corp. | Spirocyclic pyridotriazine derivatives useful as hiv integrase inhibitors |
CA3008607A1 (en) | 2015-12-15 | 2017-06-22 | Shionogi & Co., Ltd. | A medicament for treating influenza characterized by combining a cap-dependent endonuclease inhibitor and an anti-influenza drug |
EP4194459A1 (en) | 2016-06-20 | 2023-06-14 | Shionogi & Co., Ltd | Process for preparing substituted polycyclic pyridone derivative and crystal thereof |
KR20190007517A (ko) * | 2016-08-10 | 2019-01-22 | 시오노기세야쿠 가부시키가이샤 | 치환된 다환성 피리돈 유도체 및 그의 프로드러그를 함유하는 의약 조성물 |
EP3753936A4 (en) | 2018-01-17 | 2022-03-23 | Jiangxi Caishi Pharmaceutical Technology Co., Ltd. | PYRIDONE DERIVATIVE, COMPOSITION THEREOF AND USE THEREOF AS AN AGAINST FLU MEDICATION |
-
2018
- 2018-10-05 CN CN201880072447.6A patent/CN111386276B/zh active Active
- 2018-10-05 AR ARP180102884A patent/AR113748A1/es unknown
- 2018-10-05 KR KR1020207011759A patent/KR20200066644A/ko not_active Application Discontinuation
- 2018-10-05 BR BR112020006639-7A patent/BR112020006639A2/pt unknown
- 2018-10-05 AU AU2018344739A patent/AU2018344739B2/en active Active
- 2018-10-05 CA CA3078442A patent/CA3078442A1/en active Pending
- 2018-10-05 EP EP18865221.8A patent/EP3693373A4/en active Pending
- 2018-10-05 WO PCT/JP2018/037390 patent/WO2019070059A1/ja unknown
- 2018-10-05 SG SG11202002789XA patent/SG11202002789XA/en unknown
- 2018-10-05 US US16/652,122 patent/US11286262B2/en active Active
- 2018-10-05 JP JP2019547031A patent/JP6924839B2/ja active Active
- 2018-10-05 MX MX2020003469A patent/MX2020003469A/es unknown
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2020
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CA3078442A1 (en) | 2019-04-11 |
CN111386276B (zh) | 2023-06-23 |
CN111386276A (zh) | 2020-07-07 |
SG11202002789XA (en) | 2020-04-29 |
US20200247818A1 (en) | 2020-08-06 |
US20230040262A1 (en) | 2023-02-09 |
WO2019070059A1 (ja) | 2019-04-11 |
AU2018344739B2 (en) | 2023-04-13 |
US11286262B2 (en) | 2022-03-29 |
IL273821B (en) | 2022-12-01 |
EP3693373A1 (en) | 2020-08-12 |
BR112020006639A2 (pt) | 2020-09-24 |
AU2018344739A1 (en) | 2020-04-30 |
JPWO2019070059A1 (ja) | 2020-10-22 |
IL273821A (en) | 2020-05-31 |
MX2020003469A (es) | 2020-08-03 |
KR20200066644A (ko) | 2020-06-10 |
EP3693373A4 (en) | 2021-11-03 |
IL273821B2 (en) | 2023-04-01 |
JP6924839B2 (ja) | 2021-08-25 |
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