Diethyl 4[(4-oxo-3-bromo) butyl] benzoyl-L-glutamate and preparation and use

A technology of diethyl glutamate and benzoyl, applied in the field of 4-[(4-oxo-3-bromo)butyl]benzoyl-L-diethyl glutamate and its preparation and application , can solve the problems of low total yield, long steps, unsuitable for large-scale industrial production, etc.
CN1821220AInactive Publication Date: 2006-08-23ZHEJIANG UNIV OF TECH
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
ZHEJIANG UNIV OF TECH
Publication Date
2006-08-23
Estimated Expiration
Not applicable · inactive patent

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Abstract

The present invention relates to new compound diethyl 4-[(4-oxo-3-bromo) butyl] benzoyl-L-glutamate and its preparation process and application. The compound diethyl 4-[(4-oxo-3-bromo) butyl] benzoyl-L-glutamate in the chemical expression as shown is prepared through the reaction of material diethyl 4-(4-oxo-butyl) benzoyl-L-glutamate and bromo reagent inside C1-C4 halohydrocarbon solvent at 20-30 deg.c. The compound diethyl 4-[(4-oxo-3-bromo) butyl] benzoyl-L-glutamate is used as the important intermediate of antitumor medicine Pemetrexed disodium. The present invention provides new path of synthesizing Pemetrexed disodium, and results in shortened Pemetrexed disodium synthesizing path and lowered production cost.
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Description

(1) Technical field

[0001] The invention relates to a new compound 4-[(4-oxo-3-bromo)butyl] benzoyl-L-glutamic acid diethyl ester, and a preparation method and application thereof. (2) Background technology

[0002] Pemetrexed (also known as LY231514, trade name Alimta) is a new type of antifolate antimetabolites. Its targets include multiple enzymes in the synthesis of pyrimidine and purine, so it is also known as multi-targeted antifolate (multi2targeted antifolate). , MTA). It has shown extensive anti-tumor activity in in vitro and clinical trials and is a promising anti-tumor drug.

[0003] Pemetrexed was successfully developed by Dr. Shi Quan, a Chinese scientist from Eli Lilly and Company, after a decade of research and development in the Department of Chemistry, Princeton University. Since the 1990s, there have been many patents and documents describing the chemical synthesis methods of pemetrexed and its disodium salt, such as Taylor, EC; Kuhnt.D.; Shih, C.; etc.J. Med. C...

Claims

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