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

Synthesis method of abiraterone acetate highly finished product

A kind of technology of abiraterone acetate and synthesis method, applied in the direction of steroids, organic chemistry, etc., can solve the problems of long synthesis steps, purification method and product yield, serious corrosion of equipment, etc., to achieve improved results efficiency, shorten the synthesis steps, and improve the effect of purification yield

Inactive Publication Date: 2018-11-13
XUZHOU COLLEGE OF INDAL TECH
View PDF3 Cites 1 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0024] (1) The synthesis steps are longer
[0025] (2) Strong acid or strong alkali substances are used in the synthesis process, which will seriously corrode the equipment
[0026] (3) The method of purification and the yield of product need to be improved
[0028] (1) The synthesis steps are long and the raw materials used are various
[0029] (2) Strong acid or strong alkali substances are used in the synthesis process, which will seriously corrode the equipment
[0030] (3) The method of purification and the yield of product need to be improved
[0031] Technical problems: selection of reaction raw materials and experimental conditions, solvents and purification methods, and improvement of reaction yield

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 method of abiraterone acetate highly finished product
  • Synthesis method of abiraterone acetate highly finished product
  • Synthesis method of abiraterone acetate highly finished product

Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0079] In order to make the object, technical solution and advantages of the present invention more clear, the present invention will be further described in detail below in conjunction with the examples. It should be understood that the specific embodiments described here are only used to explain the present invention, not to limit the present invention.

[0080] Such as figure 1 As shown, the synthetic method of abiraterone acetate refined product provided by the embodiments of the present invention comprises the following steps:

[0081] The reaction scheme of the synthetic side of the refined product of abiraterone acetate that the embodiment of the present invention provides is:

[0082] Add dehydroepiandrosterone acetate (SM1), sequentially add absolute ethanol, hydrazine hydrate and glacial acetic acid at 20-30°C to prepare reactant B; add tetrahydrofuran and iodine grains, -5-5°C, slowly add tetramethyl Guanidine, control the temperature below 10°C, add the tetrahyd...

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 belongs to the technical field of organic chemistry, and discloses a synthesis method of an abiraterone acetate highly finished product. The synthesis method comprises the following steps: sequentially adding absolute ethyl alcohol, hydrazine hydrate and glacial acetic acid in dehydroisoandrosterone 3-acetate (SM1), and preparing a reactant B at the temperature of 20-30 DEG C; addingtetrahydrofuran and iodine, slowly adding tetramethyl guanidine at the temperature of -5 to 5 DEG C, controlling the temperature to be 10 DEG C or below, and dropwise adding a tetrahydrofuran solution of the compound B at the temperature of -5 to 5 DEG C for 6 h to obtain a compound C; sequentially adding tetrahydrofuran, diethyl-(3-pyridine)borane, trans-dichlorobis(triphenyl-phosphine)palladiumand a tetrabutylammonium fluoride trihydrate in the compound C to obtain a compound D; and adding dichloromethane and 4-dimethylaminopyridine in the compound D, slowly adding acetic anhydride at thetemperature of 15-35 DEG C, and adding activated carbon and methanol-water after finishing the reaction to obtain a compound E, and highly finishing the compound E to prepare the abiraterone acetate highly finished product.

Description

technical field [0001] The invention belongs to the technical field of organic chemistry, in particular to a method for synthesizing a refined product of abiraterone acetate. Background technique [0002] At present, the existing technologies commonly used in the industry are as follows: [0003] (1) Taking dehydroepiandrosterone as the starting material synthetic route [0004] Using dehydroepiandrosterone as the starting raw material for synthesis, dehydroepiandrosterone is first reacted with hydrazine hydrate to obtain dehydroepiandrosterone-17-hydrazone, and then iodized to form 17-iodo-androster-5,16-di En-3β-alcohol, and then react with diethyl (3-pyridyl) borane to produce abiraterone, and finally esterify to get abiraterone acetate. [0005] [0006] (2) Synthetic route using 3β-acetyl dehydrocortisol as starting material [0007] Using 3β-acetyldrocorticosterone as the starting material [11], 3β-acetyldorhydrocorticosterone was trifluoromethylated to obtain 3...

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
IPC IPC(8): C07J43/00
CPCC07J43/003
Inventor 刘郁刘连新刘春杰卜伟
Owner XUZHOU COLLEGE OF INDAL TECH
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