TWI816651B - 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 - Google Patents

7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 Download PDF

Info

Publication number
TWI816651B
TWI816651B TW106144830A TW106144830A TWI816651B TW I816651 B TWI816651 B TW I816651B TW 106144830 A TW106144830 A TW 106144830A TW 106144830 A TW106144830 A TW 106144830A TW I816651 B TWI816651 B TW I816651B
Authority
TW
Taiwan
Prior art keywords
compound
formula
salt
item
acid
Prior art date
Application number
TW106144830A
Other languages
English (en)
Chinese (zh)
Other versions
TW201829422A (zh
Inventor
滝口大夢
東昭伸
稲葉𨺓之
渡辺
竹市翼
安德斯 卡拉斯考夫 彼得森
佩兒 韋德索
金姆 勒貝克 詹森
詹 伯恩候特
索倫 艾伯杜魯普
Original Assignee
日商日本煙草產業股份有限公司
丹麥商理奧藥品公司
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by 日商日本煙草產業股份有限公司, 丹麥商理奧藥品公司 filed Critical 日商日本煙草產業股份有限公司
Publication of TW201829422A publication Critical patent/TW201829422A/zh
Application granted granted Critical
Publication of TWI816651B publication Critical patent/TWI816651B/zh

Links

Images

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C271/00—Derivatives of carbamic acids, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C271/06—Esters of carbamic acids
    • C07C271/08—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms
    • C07C271/10—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C271/22—Esters of carbamic acids having oxygen atoms of carbamate groups bound to acyclic carbon atoms with the nitrogen atoms of the carbamate groups bound to hydrogen atoms or to acyclic carbon atoms to carbon atoms of hydrocarbon radicals substituted by carboxyl groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C269/00—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups
    • C07C269/06—Preparation of derivatives of carbamic acid, i.e. compounds containing any of the groups, the nitrogen atom not being part of nitro or nitroso groups by reactions not involving the formation of carbamate groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/30—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings 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
    • C07D307/32—Oxygen atoms
    • C07D307/33—Oxygen atoms in position 2, the oxygen atom being in its keto or unsubstituted enol form
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • 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
    • C07D487/02—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 two hetero rings
    • C07D487/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
    • C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
    • 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
    • C07B2200/07—Optical isomers
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
TW106144830A 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體 TWI816651B (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
JP2016-247607 2016-12-21
JP2016247607 2016-12-21

Publications (2)

Publication Number Publication Date
TW201829422A TW201829422A (zh) 2018-08-16
TWI816651B true TWI816651B (zh) 2023-10-01

Family

ID=62627423

Family Applications (2)

Application Number Title Priority Date Filing Date
TW106144830A TWI816651B (zh) 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體
TW112133483A TWI854815B (zh) 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體

Family Applications After (1)

Application Number Title Priority Date Filing Date
TW112133483A TWI854815B (zh) 2016-12-21 2017-12-20 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體

Country Status (14)

Country Link
US (3) US11673900B2 (enExample)
EP (2) EP4793278A2 (enExample)
JP (2) JP6434678B2 (enExample)
KR (1) KR102546513B1 (enExample)
CN (2) CN117865992A (enExample)
AU (2) AU2017384317C1 (enExample)
BR (1) BR112019012688A2 (enExample)
CA (1) CA3047891A1 (enExample)
ES (1) ES3068086T3 (enExample)
IL (2) IL288080B2 (enExample)
MX (2) MX2019007542A (enExample)
PL (1) PL3560932T3 (enExample)
TW (2) TWI816651B (enExample)
WO (1) WO2018117152A1 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
BR112017026173A2 (pt) 2015-07-07 2018-08-14 Japan Tobacco, Inc. Método para produção de derivado de 7h-pirrolo [2,3-d]pirimidina e intermediário do mesmo
PL3560932T3 (pl) 2016-12-21 2026-06-29 Japan Tobacco Inc. Sposób wytwarzania pochodnych 7H‑pirolo[2,3‑d]pirymidyny i ich syntetycznych produktów pośrednich
CN111606929B (zh) * 2020-06-30 2023-07-07 中瀚(齐河县)生物医药科技有限公司 德高替尼的制备方法
CN111560021B (zh) * 2020-06-30 2023-05-26 上海鲲博玖瑞医药科技发展有限公司 一种德高替尼中间体及其制备方法
CN111574540B (zh) * 2020-06-30 2023-08-29 云南华派医药科技有限公司 一种德高替尼的制备方法
JP2026509302A (ja) 2023-03-17 2026-03-17 レオ ファーマ アクティーゼルスカブ 中等症ないし重症の慢性手湿疹を有する患者における慢性手湿疹を処置する方法
KR20260019479A (ko) 2023-05-04 2026-02-10 레볼루션 메디슨즈, 인크. Ras 관련 질환 또는 장애를 위한 병용 요법
CN121889155A (zh) 2023-08-07 2026-04-17 锐新医药公司 用于治疗ras蛋白相关疾病或病症的rmc-6291
AU2024360465A1 (en) 2023-10-12 2026-04-09 Revolution Medicines, Inc. Macrocyclic ras inhibitors
WO2025171296A1 (en) 2024-02-09 2025-08-14 Revolution Medicines, Inc. Ras inhibitors
WO2025240847A1 (en) 2024-05-17 2025-11-20 Revolution Medicines, Inc. Ras inhibitors
US20250375445A1 (en) 2024-06-07 2025-12-11 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2025265060A1 (en) 2024-06-21 2025-12-26 Revolution Medicines, Inc. Therapeutic compositions and methods for managing treatment-related effects
WO2026006747A1 (en) 2024-06-28 2026-01-02 Revolution Medicines, Inc. Ras inhibitors
WO2026015801A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015825A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Use of ras inhibitor for treating pancreatic cancer
WO2026015790A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026015796A1 (en) 2024-07-12 2026-01-15 Revolution Medicines, Inc. Methods of treating a ras related disease or disorder
WO2026050446A1 (en) 2024-08-29 2026-03-05 Revolution Medicines, Inc. Ras inhibitors
WO2026072904A2 (en) 2024-09-26 2026-04-02 Revolution Medicines, Inc. Compositions and methods for treating lung cancer
WO2026090116A2 (en) 2024-10-21 2026-04-30 Revolution Medicines, Inc. Ras inhibitors
US20260108528A1 (en) 2024-10-22 2026-04-23 Revolution Medicines, Inc. Methods of treating a ras protein-related disease or disorder
WO2026090245A1 (en) 2024-10-22 2026-04-30 Revolution Medicines, Inc. Use of ras inhibitors for treating cancer
WO2026106912A1 (en) 2024-11-12 2026-05-21 Revolution Medicines, Inc. Ras inhibitors
WO2026112260A1 (en) 2024-11-21 2026-05-28 Revolution Medicines, Inc. Ras inhibitors
WO2026122764A2 (en) 2024-12-06 2026-06-11 Revolution Medicines, Inc. Ras inhibitors
WO2026128688A2 (en) 2024-12-13 2026-06-18 Revolution Medicines, Inc. Ras inhibitors
WO2026161839A1 (en) 2025-01-27 2026-07-30 Revolution Medicines, Inc. Ras inhibitors

Family Cites Families (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US7662960B2 (en) 2001-04-26 2010-02-16 Choongwae Pharma Corporation Beta-strand mimetics and method relating thereto
EP1646633B1 (en) * 2003-05-30 2009-04-15 Choongwae Pharma Corporation Beta-strand mimetics
US7230119B2 (en) 2004-08-25 2007-06-12 Biocryst Pharmaceuticals, Inc. Process for the preparation of substituted pyrrolidine derivatives and intermediates
WO2008036755A1 (en) 2006-09-22 2008-03-27 Janssen Pharmaceutica N.V. Spiro benzazepines used as vasopressin antagonists
TWI466885B (zh) * 2009-07-31 2015-01-01 Japan Tobacco Inc 含氮螺環化合物及其醫藥用途
SG191291A1 (en) 2011-01-19 2013-07-31 Galapagos Nv Azetidine derivatives useful for the treatment of metabolic and inflammatory diseases
CN103570601B (zh) 2012-07-20 2016-03-30 重庆博腾制药科技股份有限公司 一种光学活性药物中间体的制备方法
HUE034210T2 (hu) 2013-03-05 2018-02-28 Theravance Biopharma R&D Ip Llc Neprilizininhibitorok
JP6500634B2 (ja) * 2015-06-24 2019-04-17 株式会社Ihi 溶接装置及び溶接方法
BR112017026173A2 (pt) * 2015-07-07 2018-08-14 Japan Tobacco, Inc. Método para produção de derivado de 7h-pirrolo [2,3-d]pirimidina e intermediário do mesmo
TWI822666B (zh) * 2016-12-21 2023-11-21 日商日本煙草產業股份有限公司 Ｊａｎｕｓ激酶抑制劑之結晶型
PL3560932T3 (pl) 2016-12-21 2026-06-29 Japan Tobacco Inc. Sposób wytwarzania pochodnych 7H‑pirolo[2,3‑d]pirymidyny i ich syntetycznych produktów pośrednich

Also Published As

Publication number Publication date
AU2017384317B2 (en) 2022-03-10
CA3047891A1 (en) 2018-06-28
JPWO2018117152A1 (ja) 2018-12-20
RU2019122691A3 (enExample) 2021-02-08
WO2018117152A1 (ja) 2018-06-28
AU2017384317C1 (en) 2022-06-30
EP3560932B1 (en) 2026-03-11
PL3560932T3 (pl) 2026-06-29
CN110300756B (zh) 2024-01-02
BR112019012688A2 (pt) 2019-11-19
IL267385B2 (en) 2023-06-01
US20200216470A1 (en) 2020-07-09
US20250084106A1 (en) 2025-03-13
IL288080B2 (en) 2024-03-01
CN110300756A (zh) 2019-10-01
KR102546513B1 (ko) 2023-06-23
JP6434678B2 (ja) 2018-12-05
US11673900B2 (en) 2023-06-13
RU2019122691A (ru) 2021-01-25
IL288080A (en) 2022-01-01
EP4793278A2 (en) 2026-08-19
ES3068086T3 (es) 2026-05-27
CN117865992A (zh) 2024-04-12
US12195481B2 (en) 2025-01-14
IL288080B1 (en) 2023-11-01
EP3560932A4 (en) 2020-10-28
MX2019007542A (es) 2019-11-18
IL267385A (enExample) 2019-07-31
JP7098496B2 (ja) 2022-07-11
TW202400613A (zh) 2024-01-01
JP2019048806A (ja) 2019-03-28
AU2022203506A1 (en) 2022-06-09
US20240140967A1 (en) 2024-05-02
AU2017384317A1 (en) 2019-07-11
IL267385B1 (enExample) 2023-02-01
AU2022203506B2 (en) 2024-02-08
EP3560932A1 (en) 2019-10-30
KR20190095408A (ko) 2019-08-14
TW201829422A (zh) 2018-08-16
TWI854815B (zh) 2024-09-01
EP3560932C0 (en) 2026-03-11
MX2024005335A (es) 2024-05-20

Similar Documents

Publication Publication Date Title
TWI854815B (zh) 7H-吡咯并[2,3-d]嘧啶衍生物的製造方法及其合成中間體
JP6871856B2 (ja) ７Ｈ−ピロロ［２，３−ｄ］ピリミジン誘導体の製造方法及びその中間体
KR102702286B1 (ko) 7H-피롤로[2,3-d]피리미딘 유도체의 제조 방법 및 그의 공결정
EP2914582A2 (en) Chiral fluorinating reagents
RU2776802C2 (ru) Способ получения производных 7h-пирроло[2,3-d]пиримидина и промежуточных продуктов для их синтеза