JP2019210273A - エドキサバンの製造方法 - Google Patents
エドキサバンの製造方法 Download PDFInfo
- Publication number
- JP2019210273A JP2019210273A JP2018175006A JP2018175006A JP2019210273A JP 2019210273 A JP2019210273 A JP 2019210273A JP 2018175006 A JP2018175006 A JP 2018175006A JP 2018175006 A JP2018175006 A JP 2018175006A JP 2019210273 A JP2019210273 A JP 2019210273A
- Authority
- JP
- Japan
- Prior art keywords
- solvent
- compound represented
- formula
- amine
- base
- 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.)
- Pending
Links
- IZABLUDXAWYTNU-WCQGTBRESA-N CN(C)C([C@@H](CC[C@@H]1NC(C(Nc(cc2)ncc2Cl)=O)=O)C[C@H]1N)=O Chemical compound CN(C)C([C@@H](CC[C@@H]1NC(C(Nc(cc2)ncc2Cl)=O)=O)C[C@H]1N)=O IZABLUDXAWYTNU-WCQGTBRESA-N 0.000 description 3
- HGVDHZBSSITLCT-JLJPHGGASA-N CN(C)C([C@@H](CC[C@@H]1NC(C(Nc(cc2)ncc2Cl)=O)=O)C[C@H]1NC(c1nc(CCN(C)C2)c2[s]1)=O)=O Chemical compound CN(C)C([C@@H](CC[C@@H]1NC(C(Nc(cc2)ncc2Cl)=O)=O)C[C@H]1NC(c1nc(CCN(C)C2)c2[s]1)=O)=O HGVDHZBSSITLCT-JLJPHGGASA-N 0.000 description 1
- URPHLHADYVVAIF-UHFFFAOYSA-N CN(CC1)Cc2c1nc(C(O)=O)[s]2 Chemical compound CN(CC1)Cc2c1nc(C(O)=O)[s]2 URPHLHADYVVAIF-UHFFFAOYSA-N 0.000 description 1
- LEFNWSATIDVVDK-IKVPFREESA-N Cc1ccc(NCC(C(N[C@@H](CCC(C2)C(N(C)C)=O)C2/C=N/C(c2nc(CCN(C)C3)c3[s]2)O)=O)=O)nc1 Chemical compound Cc1ccc(NCC(C(N[C@@H](CCC(C2)C(N(C)C)=O)C2/C=N/C(c2nc(CCN(C)C3)c3[s]2)O)=O)=O)nc1 LEFNWSATIDVVDK-IKVPFREESA-N 0.000 description 1
- PFKFTWBEEFSNDU-UHFFFAOYSA-N O=C([n]1cncc1)[n]1cncc1 Chemical compound O=C([n]1cncc1)[n]1cncc1 PFKFTWBEEFSNDU-UHFFFAOYSA-N 0.000 description 1
Classifications
-
- 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
- C07D213/04—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/26—Radicals substituted by halogen atoms or nitro 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
- A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
-
- 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
- C07D213/04—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—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 having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
- C07D213/36—Radicals substituted by singly-bound nitrogen atoms
Landscapes
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Organic Chemistry (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Veterinary Medicine (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2023101357A JP7664971B2 (ja) | 2018-06-08 | 2023-06-21 | エドキサバンの製造方法 |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| KR1020180065951A KR102087080B1 (ko) | 2018-06-08 | 2018-06-08 | 에독사반의 제조용 중간체의 제조 방법 및 에독사반의 제조 방법 |
| KR10-2018-0065951 | 2018-06-08 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023101357A Division JP7664971B2 (ja) | 2018-06-08 | 2023-06-21 | エドキサバンの製造方法 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JP2019210273A true JP2019210273A (ja) | 2019-12-12 |
Family
ID=68846363
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018175006A Pending JP2019210273A (ja) | 2018-06-08 | 2018-09-19 | エドキサバンの製造方法 |
| JP2023101357A Active JP7664971B2 (ja) | 2018-06-08 | 2023-06-21 | エドキサバンの製造方法 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023101357A Active JP7664971B2 (ja) | 2018-06-08 | 2023-06-21 | エドキサバンの製造方法 |
Country Status (2)
| Country | Link |
|---|---|
| JP (2) | JP2019210273A (https=) |
| KR (1) | KR102087080B1 (https=) |
Cited By (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102090912B1 (ko) * | 2019-12-18 | 2020-03-18 | 유니셀랩 주식회사 | 신규한 결정형 형태의 에독사반 및 이의 제조방법 |
| CN111393456A (zh) * | 2020-03-31 | 2020-07-10 | 内蒙古京东药业有限公司 | 一种由三氯乙酮鎓盐衍生物制备依度沙班的方法 |
| CN111763222A (zh) * | 2020-08-03 | 2020-10-13 | 珠海市海瑞德新材料科技有限公司 | 用于制备依度沙班游离碱的中间体及其制备方法和应用 |
| CN115594613A (zh) * | 2022-10-31 | 2023-01-13 | 上海柏狮生物科技有限公司（Cn） | 依度沙班中间体及其制备方法 |
| CN116332958A (zh) * | 2023-03-30 | 2023-06-27 | 浙江九洲药业股份有限公司 | 一种依度沙班对甲苯磺酸盐的制备方法 |
| CN116332957A (zh) * | 2023-03-30 | 2023-06-27 | 浙江九洲药业股份有限公司 | 一种FXa抑制剂化合物的制备方法 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102513519B1 (ko) * | 2020-06-08 | 2023-03-23 | 주식회사 파마코스텍 | 신규한 에독사반 벤젠술폰산염 1 수화물의 제조방법 |
| WO2023223346A1 (en) * | 2022-05-16 | 2023-11-23 | Mylan Laboratories Limited | An improved process for the preparation of edoxaban intermediate |
| WO2024197723A1 (zh) * | 2023-03-30 | 2024-10-03 | 浙江九洲药业股份有限公司 | 一种依度沙班对甲苯磺酸盐的制备方法 |
| KR20250049636A (ko) * | 2023-10-05 | 2025-04-14 | 주식회사 파마코스텍 | 신규한 에독사반 제조방법 |
Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003000680A1 (en) * | 2001-06-20 | 2003-01-03 | Daiichi Pharmaceutical Co., Ltd. | Diamine derivatives |
| JP2010120852A (ja) * | 2007-03-09 | 2010-06-03 | Daiichi Sankyo Co Ltd | 新規なジアミド誘導体 |
| WO2010131663A1 (ja) * | 2009-05-15 | 2010-11-18 | 第一三共株式会社 | オキサミド誘導体 |
| CN105399667A (zh) * | 2015-12-15 | 2016-03-16 | 南京艾德凯腾生物医药有限责任公司 | 一种依度沙班中间体的制备方法 |
| CN107641131A (zh) * | 2016-07-22 | 2018-01-30 | 江苏威凯尔医药科技有限公司 | 一种抗血栓药物的制备方法 |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2407457B1 (en) | 2009-03-10 | 2015-04-22 | Daiichi Sankyo Company, Limited | Process for producing diamine derivative |
| KR102371784B1 (ko) * | 2014-02-18 | 2022-03-07 | 다이이찌 산쿄 가부시키가이샤 | 활성화 혈액 응고 제 X 인자 (FXa) 의 저해약의 제조 방법 |
| CN104761571B (zh) | 2015-03-10 | 2017-03-08 | 山东科兴生物制品有限公司 | 一种依度沙班的合成方法 |
-
2018
- 2018-06-08 KR KR1020180065951A patent/KR102087080B1/ko active Active
- 2018-09-19 JP JP2018175006A patent/JP2019210273A/ja active Pending
-
2023
- 2023-06-21 JP JP2023101357A patent/JP7664971B2/ja active Active
Patent Citations (5)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2003000680A1 (en) * | 2001-06-20 | 2003-01-03 | Daiichi Pharmaceutical Co., Ltd. | Diamine derivatives |
| JP2010120852A (ja) * | 2007-03-09 | 2010-06-03 | Daiichi Sankyo Co Ltd | 新規なジアミド誘導体 |
| WO2010131663A1 (ja) * | 2009-05-15 | 2010-11-18 | 第一三共株式会社 | オキサミド誘導体 |
| CN105399667A (zh) * | 2015-12-15 | 2016-03-16 | 南京艾德凯腾生物医药有限责任公司 | 一种依度沙班中间体的制备方法 |
| CN107641131A (zh) * | 2016-07-22 | 2018-01-30 | 江苏威凯尔医药科技有限公司 | 一种抗血栓药物的制备方法 |
Cited By (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR102090912B1 (ko) * | 2019-12-18 | 2020-03-18 | 유니셀랩 주식회사 | 신규한 결정형 형태의 에독사반 및 이의 제조방법 |
| WO2021125474A1 (ko) * | 2019-12-18 | 2021-06-24 | 유니셀랩 주식회사 | 신규한 결정형 형태의 에독사반 및 이의 제조방법 |
| CN111393456A (zh) * | 2020-03-31 | 2020-07-10 | 内蒙古京东药业有限公司 | 一种由三氯乙酮鎓盐衍生物制备依度沙班的方法 |
| CN111393456B (zh) * | 2020-03-31 | 2022-07-12 | 内蒙古京东药业有限公司 | 一种由三氯乙酮鎓盐衍生物制备依度沙班的方法 |
| CN111763222A (zh) * | 2020-08-03 | 2020-10-13 | 珠海市海瑞德新材料科技有限公司 | 用于制备依度沙班游离碱的中间体及其制备方法和应用 |
| CN111763222B (zh) * | 2020-08-03 | 2021-05-25 | 珠海市海瑞德新材料科技有限公司 | 用于制备依度沙班游离碱的中间体及其制备方法和应用 |
| CN115594613A (zh) * | 2022-10-31 | 2023-01-13 | 上海柏狮生物科技有限公司（Cn） | 依度沙班中间体及其制备方法 |
| CN115594613B (zh) * | 2022-10-31 | 2024-04-19 | 上海柏狮生物科技有限公司 | 依度沙班中间体及其制备方法 |
| CN116332958A (zh) * | 2023-03-30 | 2023-06-27 | 浙江九洲药业股份有限公司 | 一种依度沙班对甲苯磺酸盐的制备方法 |
| CN116332957A (zh) * | 2023-03-30 | 2023-06-27 | 浙江九洲药业股份有限公司 | 一种FXa抑制剂化合物的制备方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| JP7664971B2 (ja) | 2025-04-18 |
| KR102087080B1 (ko) | 2020-03-10 |
| JP2023116769A (ja) | 2023-08-22 |
| KR20190139463A (ko) | 2019-12-18 |
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