Looking for breakthrough ideas for innovation challenges? Try Patsnap Eureka!

Method for preparing antitumor drug darolutamide

A technique for laminamine and its compounds, which is applied in the field of preparing the antineoplastic drug dolamide, can solve the problems that the preparation method of dolamamine needs to be improved, and achieve the effects of good experimental operability, high reaction yield, and easy operation

Inactive Publication Date: 2020-05-08
武汉九州钰民医药科技有限公司
View PDF9 Cites 0 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0005] The preparation method of dolamide still needs to be improved at present

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
  • Method for preparing antitumor drug darolutamide
  • Method for preparing antitumor drug darolutamide
  • Method for preparing antitumor drug darolutamide

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0041] 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.

[0042] Synthesis of compound shown in embodiment 1 formula 3

[0043] At room temperature, compound 1 (6.0 g, 27.7 mmol) and compound 2 (5.43 g, 27.7 mmol) were dissolved in THF (50 mL) and H 2 O (10mL), add K 2 CO 3 (7.66g, 55.4mmol) and catalyst (Ph 3 P) 2 PdCl 2 (972mg, 1.385mmol), vacuumized and replaced with nitrogen three times, the reaction solution was kept at 40°C and stirred for 3h, cooled...

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

PropertyMeasurementUnit
quality scoreaaaaaaaaaa
Login to View More

Abstract

The invention relates to a method for preparing an antitumor drug darolutamide. A one-step Suzuki reaction is carried out, and then deprotection, hydroxylamine condensation and amide condensation reactions are carried out to obtain the darolutamide. The method has the advantages of few reaction steps, high reaction yield of each step, and simplicity in operation, so the total yield of the whole route is high, and the method has good experiment operationality.

Description

technical field [0001] The invention relates to the technical field of medicine, in particular to a method for preparing the antitumor drug dolamide. Background technique [0002] Prostate cancer is the second most common malignancy in men worldwide, with approximately 1.2 million men diagnosed with prostate cancer and 358,000 deaths worldwide in 2018. Dolamide (Darolutamide) is a non-steroidal androgen receptor (AR) antagonist with a unique chemical structure that can bind to the receptor with high affinity and has strong antagonistic activity, thereby inhibiting receptor function and prostate The growth of cancer cells. On July 30, 2019, the U.S. FDA approved the marketing of dolamide tablets (oral, specification 300MG, trade name NUBEQA) of BAYER HEALTHCARE for the treatment of non-metastatic castration-resistant prostate cancer. [0003] The molecular weight of dolamide is 398.85, and the molecular formula is C 19 h 19 ClN 6 o 2 . Its structural formula is as the ...

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): C07D231/14
CPCC07D231/14
Inventor 许勇范昭泽陈龙余艳平
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 Patsnap Eureka
  • Industry Leading Data Capabilities
  • Powerful AI technology
  • Patent DNA Extraction
Social media
Patsnap Eureka Blog
Learn More
PatSnap group products

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

© 2024 PatSnap. All rights reserved.Legal|Privacy policy|Modern Slavery Act Transparency Statement|Sitemap|About US| Contact US: help@patsnap.com