Synthesis and preparation process of antitumor drug CFI-402257

A technology of CFI-402257 and preparation process, which is applied in the field of biomedicine, can solve the problems such as the need to improve the synthesis and preparation process of CFI-402257, and achieve the effects of improving the total yield and industrial operability, reducing the number of reaction steps and improving the selectivity.

Active Publication Date: 2021-12-10
武汉九州钰民医药科技有限公司
View PDF3 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0006] At present, the synthesis and preparation process of CFI-402257 still needs to be improved

Method used

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
View more

Image

Smart Image Click on the blue labels to locate them in the text.
Viewing Examples
Smart Image
  • Synthesis and preparation process of antitumor drug CFI-402257
  • Synthesis and preparation process of antitumor drug CFI-402257
  • Synthesis and preparation process of antitumor drug CFI-402257

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0053] Embodiments of the present invention are described in detail below. The embodiments described below are exemplary only for explaining the present invention and should not be construed as limiting the present invention. If no specific technique or condition is indicated in the examples, it shall be carried out according to the technique or condition described in the literature in this field or according to the product specification. The reagents or instruments used were not indicated by the manufacturer, and they were all commercially available conventional products.

[0054] Synthesis of compound shown in embodiment 1 formula 2

[0055] Add the compound shown in formula 1 (5.0g, 26.94mmol) into acetonitrile (30mL) and stir, slowly add POCl 3 (3.1g, 20.21mmol), the mixture was stirred and contacted at room temperature for 12 hours. After the reaction was complete, the mixture was poured on ice, neutralized to a pH value of about 8 with solid sodium bicarbonate, and the...

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

PUM

No PUM Login to view more

Abstract

The invention relates to a synthesis and preparation process of an antitumor drug CFI-402257. Compared with the synthesis route in the prior art in which the hydroxyl is protected by boc in the third step and then the reaction is performed, the synthesis route disclosed by the invention does not need to be protected, and one-step reaction is reduced. Besides, in the preparation process provided by the invention, the organic zinc reagent participates in the specific halogenation reaction in the last step, so that side reaction on hydroxyl in reactants when chemical alkali is used is avoided, and the overall yield of the route is higher.

Description

technical field [0001] The invention relates to the technical field of biomedicine, in particular to a synthesis and preparation process of an antitumor drug CFI-402257. Background technique [0002] Treadwell Therapeutics has licensed from University HealthNetwork (University Health Network, Ontario, Canada) to develop CFI-402257, a potent, highly selective and orally active small molecule inhibitor of monopolar spindle protein kinase 1 (Mps1) orally Capsule formulation. CFI-402257 is currently in phase 2 clinical trials in Canada for metastatic breast cancer indications, and phase 1 clinical trials for advanced solid tumors in Canada. [0003] Human cancer cells treated with CFI-402257 exhibited effects consistent with Mps1 kinase inhibition, and specifically CFI-402257 treatment resulted in SAC inactivation, chromosomal mismatch, aneuploidy, and ultimately cell death. CFI-402257 demonstrated monotherapy efficacy in tumor cell lines and patient-derived xenograft (PDX) mo...

Claims

the structure of the environmentally friendly knitted fabric provided by the present invention; figure 2 Flow chart of the yarn wrapping machine for environmentally friendly knitted fabrics and storage devices; image 3 Is the parameter map of the yarn covering machine
Login to view more

Application Information

Patent Timeline
no application Login to view more
Patent Type & Authority Applications(China)
IPC IPC(8): C07D487/04
CPCC07D487/04
Inventor 柳少群陈程范昭泽
Owner 武汉九州钰民医药科技有限公司
Who we serve
  • R&D Engineer
  • R&D Manager
  • IP Professional
Why Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Try Eureka
PatSnap group products

Browse by: Latest US Patents, China's latest patents, Technical Efficacy Thesaurus, Application Domain, Technology Topic.

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap