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

Pemetrexed thiocarbamide salt and preparation method thereof

A technology of pemetrexed thiourea salt and pemetrexed, which is applied in the field of pharmacy, can solve the problems of complex preparation process, poor stability, and low yield, and achieve the effect of easy preparation and good stability

Active Publication Date: 2010-04-07
SHENZHEN NEPTUNUS PHARM CO LTD
View PDF3 Cites 7 Cited by
  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0007] Existing pemetrexed salts as clinical drugs have disadvantages such as poor stability, complicated preparation process, and low yield. Therefore, it is important to develop new pemetrexed salts with good stability, simple preparation process and good clinical drug effect. significance

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
  • Pemetrexed thiocarbamide salt and preparation method thereof
  • Pemetrexed thiocarbamide salt and preparation method thereof
  • Pemetrexed thiocarbamide salt and preparation method thereof

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0022] Embodiment 1 Preparation process 1 of pemetrexed thiourea salt

[0023] In a 100ml reaction bottle, put 2.50g (5.85mmol) of pemetrexed into it, add 25ml of deionized water, 0.668g (8.78mmol) of thiourea salt, stir and react at room temperature for 1 hour, filter, and the filtrate is distilled under reduced pressure to precipitate a solid, add Methanol, until most of the product was precipitated, filtered, and vacuum-dried to obtain 2.26g, yield 76.4%.

[0024] Elemental analysis: C: 49.90 (49.79% of theoretical value), H: 5.49 (5.57% of theoretical value), N: 19.53 (19.36% of theoretical value).

[0025] Infrared spectrum (KBr tablet): characteristic absorption peak (cm -1 ) and its attribution: 3330 (C-NH 2 , -NH, -OH), 3046 (C 6 h 4 , benzene ring hydrocarbon stretching vibration), 2929 (-CH 2 -), 2510(-NH 3 '), 1648 (C=O), 1500, 1392 (C 6 h 4 , benzene ring skeleton vibration).

[0026] 1 H NMR spectrum (DMSO-d 6 ), chemical shift δ (ppm) and assignment o...

Embodiment 2

[0027] Embodiment 2 The preparation process 2 of pemetrexed thiourea salt

[0028] In a 100ml reaction bottle, put 2.50g (5.85mmol) of pemetrexed, add 60ml of anhydrous methanol, stir to dissolve, add 0.445g (5.85mmol) of thiourea, stir and react at room temperature for 0.5 hours, filter, wash with methanol and water , dried in vacuum to obtain 1.64g, yield 55.3%.

Embodiment 3

[0029] Embodiment 3 The preparation process 3 of pemetrexed thiourea salt

[0030] In a 100ml reaction bottle, put 2.50g (5.85mmol) of pemetrexed, add 60ml of absolute ethanol, stir to dissolve, add 2.23g (29.27mmol) of thiourea, stir at room temperature for 1 hour, filter, wash with ethanol and water , dried in vacuo to obtain 1.90 g, yield 64.2%.

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 discloses a pemetrexed thiocarbamide salt and a preparation method thereof, and a medicinal composition containing the pemetrexed thiocarbamide salt. The pemetrexed thiocarbamide salt is generated through the reaction of pemetrexed and thiocarbamide in water and / or an organic solvent. The preparation process is simple, the yield is high and the stability is good.

Description

technical field [0001] The invention belongs to the field of pharmacy, and in particular relates to pemetrexed thiourea salt and a preparation method thereof. Background technique [0002] Pemetrexed disodium is a second-line new drug developed by Eli Lily for the treatment of malignant pleural mesothelioma and non-small cell lung cancer. Its trade name is Alimta, and its structural formula is as follows: [0003] [0004] Alimta is an anti-folate-metabolizing antineoplastic drug that works by interfering with folate-dependent metabolic processes during cell replication. In vitro tests have shown that the drug can inhibit folate-dependent enzymes such as thymidylate synthase, dihydrofolate reductase, and glycine ribonucleoside formyltransferase. These enzymes are involved in the biosynthesis of thymidine and purine nucleosides, and when one or more of these enzymes are blocked, cancer cells cannot grow and multiply. Among the currently approved folic acid antagonists, e...

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): C07D487/04A61K31/519A61P35/00
Inventor 唐田王彦青朱丹吴筱昆李勇陈萍黄传贵刘碧秀
Owner SHENZHEN NEPTUNUS PHARM CO LTD
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