Pemetrexed salt and preparation method thereof

A technology of pemetrexed dipotassium salt and pemetrexed, which is applied in the field of pemetrexed salt, pemetrexed salt and preparation thereof, and can solve the problems of poor water solubility, inconvenient storage, high toxicity of ethylenediamine salt, etc. question

Inactive Publication Date: 2014-10-15
CHONGQING PHARMA RES INST
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

Among the above salt types, magnesium and calcium salts have poor solubility; meglumine and gluco

Method used

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

Examples

Experimental program
Comparison scheme
Effect test

Embodiment 1

[0035] Preparation of Pemetrexed Dipotassium Salt

[0036] Add 2.0g of pemetrexed to the reaction vessel, add 20ml of deionized water to suspend, add 5N aqueous potassium hydroxide solution dropwise under stirring to adjust the pH to 9-10 to dissolve, add 100ml of ethanol, stir and crystallize, filter, and vacuum dry to obtain Pemetrexed dipotassium salt solid 1.9g, yield 80.5%.

[0037]

Embodiment 2

[0039] Preparation of Pemetrexed Dipotassium Salt

[0040] Add 2.0g of pemetrexed to the reaction vessel, add 30ml of N,N-dimethylformamide to dissolve the clear solution, add the solution to 300ml of acetone containing 0.6g of potassium hydroxide and 10% water, stir and crystallize, and filter , and vacuum-dried to obtain 1.7 g of pemetrexed dipotassium salt as a solid, with a yield of 72.0%.

[0041]

Embodiment 3

[0043] Preparation of Pemetrexed Dipotassium Salt

[0044] Add 2.0g of pemetrexed to the reaction vessel, add 12ml of deionized water to suspend, add 0.6g of potassium hydroxide solid under stirring, add 60ml of acetonitrile to stir and crystallize, filter, and vacuum dry to obtain pemetrexed dipotassium salt solid 1.5 g, yield 63.6%.

[0045]

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Abstract

The invention discloses a pemetrexed salt and a preparation method and use thereof, the pemetrexed salt can be dipotassium salt, arginine salt, heme-L-lysinate salt and tromethamine salt of the pemetrexed, and the pemetrexed salt can be used for treatment of various cancers such as mesothelioma, lung cancer and the like.

Description

technical field [0001] The invention relates to the fields of synthetic organic chemistry and pharmacy, in particular to a pemetrexed salt, a preparation method thereof, and an application of the pemetrexed salt. Background technique [0002] Pemetrexed and its salts are disclosed as a variety of folate-dependent enzymes including thymidylate synthase (TS), dihydrofolate reductase (DHFR) and glycinamide ribonucleotide formyltransferase ( GARFT) powerful inhibitors, such as EP334636, EP432677, CN1552713, CN101033227 and other reports, have anticancer activity. [0003] The disodium salt of pemetrexed, that is, pemetrexed disodium (compound of formula I) has been listed in China, the United States, the European Union and other countries as an anticancer drug. Currently, pemetrexed disodium has been approved for use in the treatment of cancer. Four indications: (1) Combined with cisplatin for the treatment of inoperable malignant pleural mesothelioma, pemetrexed disodium is th...

Claims

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Application Information

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IPC IPC(8): C07D487/04C07C279/14C07C277/08C07C229/26C07C227/18C07C215/10C07C213/08A61K31/519A61P35/00
CPCC07D487/04
Inventor 林蒙蔡中文张检冯浩叶文润邓杰
Owner CHONGQING PHARMA RES INST
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