CN114364668A - Cdk4/6抑制剂、及其盐和中间体的制备方法 - Google Patents
Cdk4/6抑制剂、及其盐和中间体的制备方法 Download PDFInfo
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- CN114364668A CN114364668A CN202080045555.1A CN202080045555A CN114364668A CN 114364668 A CN114364668 A CN 114364668A CN 202080045555 A CN202080045555 A CN 202080045555A CN 114364668 A CN114364668 A CN 114364668A
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D209/56—Ring systems containing three or more rings
- C07D209/96—Spiro-condensed ring systems
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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
- C07D401/04—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 directly linked by a ring-member-to-ring-member bond
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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
- C07D401/14—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 three or more hetero rings
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- 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
- C07D403/04—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 directly linked by a ring-member-to-ring-member bond
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
- C07F5/02—Boron compounds
- C07F5/027—Organoboranes and organoborohydrides
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Abstract
本发明涉及制备5‑氟‑4‑(7′‑氟‑2′‑甲基螺[环戊烷‑1，3′‑吲哚]‑5′‑基)‑氮‑(5‑(1‑甲基哌啶‑4‑基)吡啶‑2‑基)嘧啶‑2‑胺，及其盐、中间体的制备方法。本发明提供的方法对现有的合成方法进行了改进，简化了制备工艺，提高了收率及纯度，能够很好地适应工业化放大生产的需求。
Description
PCT国内申请，说明书已公开。
Claims (36)
- PCT国内申请，权利要求书已公开。
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN2019105400357 | 2019-06-21 | ||
| CN201910540035 | 2019-06-21 | ||
| PCT/CN2020/097378 WO2020253865A1 (zh) | 2019-06-21 | 2020-06-22 | Cdk4/6抑制剂、及其盐和中间体的制备方法 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN114364668A true CN114364668A (zh) | 2022-04-15 |
| CN114364668B CN114364668B (zh) | 2024-07-16 |
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ID=74040653
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN202080045555.1A Active CN114364668B (zh) | 2019-06-21 | 2020-06-22 | Cdk4/6抑制剂、及其盐和中间体的制备方法 |
Country Status (4)
| Country | Link |
|---|---|
| US (1) | US20220315532A1 (zh) |
| EP (1) | EP3988545A1 (zh) |
| CN (1) | CN114364668B (zh) |
| WO (1) | WO2020253865A1 (zh) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115636826A (zh) * | 2022-10-31 | 2023-01-24 | 常州英诺升康生物医药科技有限公司 | 一种cdk抑制剂的制备方法 |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN112575044B (zh) * | 2020-12-29 | 2022-11-04 | 山东铂源药业股份有限公司 | 一种化学-酶法制备cdk4/6抑制剂关键中间体的方法 |
| WO2022242563A1 (zh) * | 2021-05-17 | 2022-11-24 | 甘李药业股份有限公司 | 一种cdk4/6抑制剂的医药用途 |
| CN118339157A (zh) * | 2021-12-24 | 2024-07-12 | 江苏恒瑞医药股份有限公司 | 氢化吲哚类化合物、其制备方法及其在医药上的应用 |
| CN115385959B (zh) * | 2022-09-27 | 2023-07-28 | 浙江尖峰药业有限公司 | 一种高纯度磷酸特地唑胺及其制备方法 |
Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105418603A (zh) * | 2015-11-17 | 2016-03-23 | 重庆莱美药业股份有限公司 | 一种高纯度帕布昔利布及其反应中间体的制备方法 |
| WO2017092635A1 (zh) * | 2015-11-30 | 2017-06-08 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| CN107118211A (zh) * | 2017-05-24 | 2017-09-01 | 南京斯贝源医药科技有限公司 | 利奥西呱的制备方法 |
| WO2017202365A1 (zh) * | 2016-05-25 | 2017-11-30 | 四川海思科制药有限公司 | 一种三氟甲基取代的吡喃衍生物制备方法 |
| CN107827869A (zh) * | 2017-11-23 | 2018-03-23 | 上海再启生物技术有限公司 | 一种4‑(6‑氨基吡啶‑3‑基)哌啶‑1‑甲酸叔丁酯的制备方法 |
| WO2018082441A1 (zh) * | 2016-11-01 | 2018-05-11 | 山东特珐曼药业有限公司 | 4-亚甲基哌啶或其酸加成盐的制备方法 |
| CN109705089A (zh) * | 2019-02-27 | 2019-05-03 | 浙江华贝药业有限责任公司 | 化合物的纯化方法 |
-
2020
- 2020-06-22 WO PCT/CN2020/097378 patent/WO2020253865A1/zh active Application Filing
- 2020-06-22 CN CN202080045555.1A patent/CN114364668B/zh active Active
- 2020-06-22 US US17/596,714 patent/US20220315532A1/en active Pending
- 2020-06-22 EP EP20826066.1A patent/EP3988545A1/en not_active Withdrawn
Patent Citations (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN105418603A (zh) * | 2015-11-17 | 2016-03-23 | 重庆莱美药业股份有限公司 | 一种高纯度帕布昔利布及其反应中间体的制备方法 |
| WO2017092635A1 (zh) * | 2015-11-30 | 2017-06-08 | 甘李药业股份有限公司 | 一种蛋白激酶抑制剂及其制备方法和医药用途 |
| WO2017202365A1 (zh) * | 2016-05-25 | 2017-11-30 | 四川海思科制药有限公司 | 一种三氟甲基取代的吡喃衍生物制备方法 |
| WO2018082441A1 (zh) * | 2016-11-01 | 2018-05-11 | 山东特珐曼药业有限公司 | 4-亚甲基哌啶或其酸加成盐的制备方法 |
| CN107118211A (zh) * | 2017-05-24 | 2017-09-01 | 南京斯贝源医药科技有限公司 | 利奥西呱的制备方法 |
| CN107827869A (zh) * | 2017-11-23 | 2018-03-23 | 上海再启生物技术有限公司 | 一种4‑(6‑氨基吡啶‑3‑基)哌啶‑1‑甲酸叔丁酯的制备方法 |
| CN109705089A (zh) * | 2019-02-27 | 2019-05-03 | 浙江华贝药业有限责任公司 | 化合物的纯化方法 |
Non-Patent Citations (5)
| Title |
|---|
| LEI YIN，ET AL: "A highly potent CDK4/6 inhibitor was rationally designed to overcome blood brain barrier in gliobastoma therapy", EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY, no. 144, pages 17 - 18 * |
| LINNEPE P，ET AL: "2, 3-Disubstituted indoles from olefins and hydrazines via tandem hydroformylation-Fischer indole synthesis and skeletal rearrangement", ORGANIC & BIOMOLECULAR CHEMISTRY, vol. 04, no. 02, pages 302 * |
| 杨秀秀，等: "ALK抑制剂brigatinib的合成工艺改进", 中国药物化学杂志, no. 04, 20 August 2017 (2017-08-20), pages 38 - 42 * |
| 胡小霞，等: "抗癌新药帕布昔利布的合成工艺改进", 中国药物化学杂志, vol. 01, no. 05, pages 158 - 163 * |
| 鄢龙，等: "CDK4/6抑制剂abemaciclib合成工艺的优化", 武汉工程大学学报, vol. 14, no. 02, pages 1 - 6 * |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN115636826A (zh) * | 2022-10-31 | 2023-01-24 | 常州英诺升康生物医药科技有限公司 | 一种cdk抑制剂的制备方法 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3988545A1 (en) | 2022-04-27 |
| US20220315532A1 (en) | 2022-10-06 |
| WO2020253865A1 (zh) | 2020-12-24 |
| CN114364668B (zh) | 2024-07-16 |
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