Crystallization of deuteration Palbociclib isethionate

A technology of isethionate and crystallization, applied in the field of crystallization of pharmaceutical compounds, and can solve problems such as unreported crystallization

Inactive Publication Date: 2017-02-22
CHIA TAI TIANQING PHARMA GRP CO LTD
View PDF2 Cites 2 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

In the prior art, WO2014150925 and CN104447739A disclose a variety of deuterated Palbociclib

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
  • Crystallization of deuteration Palbociclib isethionate
  • Crystallization of deuteration Palbociclib isethionate
  • Crystallization of deuteration Palbociclib isethionate

Examples

Experimental program
Comparison scheme
Effect test

Embodiment

[0046]

[0047] Add compound II (0.5 g, 1.11 mmol) and methanol (2 mL) to the reaction flask respectively, and stir at room temperature to form a suspension. Isethionic acid (0.14 g, 1.11 mmol) was added dropwise to the suspension. The solid dissolved rapidly and then precipitated a yellow solid. Methanol (2 mL) was added, and the temperature was raised to 45° C. and stirred for 4 hours. Slowly let cool to room temperature, and cooled and precipitated at 4°C overnight. A yellow solid was obtained by suction filtration, and dried in a vacuum oven at 50°C to obtain deuterated palbociclib isethionate crystals (0.55 g) as shown in Formula I.

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 provides a crystallization, preparation method and medical application of a deuteration Palbociclib isethionate as shown in the formula I and particularly relates to the crystallization of the deuteration Palbociclib isethionate shown in equation I, a preparation method of the crystal, the crystal compositions containing the crystal, the medicine compositions containing the crystal and the crystal compositions, and the medical application of the crystal and the crystal compositions. The crystal has the advantages of having high purity and high crystallinity, having good stability and being easy to prepare. The crystal can be adopted for the preparation of drugs for the treatment of the diseases caused by cyclin dependent kinase 4 and 6. Please see the formula in the description.

Description

technical field [0001] The present invention relates to the crystallization of pharmaceutical compounds, in particular, the present invention relates to a crystallization of deuterated palbociclib isethionate. The present invention also relates to a method for preparing crystals of deuterated Palbociclib isethionate, a crystal composition containing crystals of deuterated Palbociclib isethionate, a pharmaceutical composition and its use in the field of medicine. Background technique [0002] Cyclin-dependent protein kinases (CDKs) are important cellular enzymes that play important functions in regulating cell differentiation and proliferation. Cyclin-dependent kinases are a group of serine / threonine protein kinases that cooperate with cyclin and are important factors in cell cycle regulation. CDK can combine with cyclin to form a heterodimer, in which CDK is the catalytic subunit, and cyclin is the regulatory subunit. Different cyclin-CDK complexes can regulate the phosphor...

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): C07D471/04A61K31/519A61P35/00
CPCC07D471/04C07B59/002C07B2200/05C07B2200/13
Inventor 张寅生高勇
Owner CHIA TAI TIANQING PHARMA GRP CO LTD
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