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Novel midbody of pemetrexed, preparing method and application thereof

A technology for pemetrexed and intermediates, which is applied in the preparation of organic compounds, the preparation of carboxylic acid amides, chemical instruments and methods, etc., can solve the problems of cumbersome reaction treatment process, long reaction steps, and high requirements for anhydrous reaction, and achieves The effect of easy industrial production, mild reaction conditions and easy purification

Active Publication Date: 2010-09-22
QILU PHARMA CO LTD +1
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  • Abstract
  • Description
  • Claims
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Problems solved by technology

The above route has the problems of high anhydrous reaction requirements, long reaction steps, and cumbersome reaction treatment process, and requires a preparation method of pemetrexed that is more suitable for industrial production

Method used

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  • Novel midbody of pemetrexed, preparing method and application thereof
  • Novel midbody of pemetrexed, preparing method and application thereof
  • Novel midbody of pemetrexed, preparing method and application thereof

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Abstract

The invention discloses a compound XI, which is a key intermediate for synthesizing pemetrexed with chemical name of N-[4-(2-halo-butyraldehyde-4-base)-benzoyl]-L-glutamic acid and structural formula shown in formula XI, wherein * represents L-configuration carbon, and X represent bromine, chlorine or iodine. The invention also discloses a preparation method of the intermediate and a method for preparing pemetrexed with the intermediate. The method for preparing pemetrexed with the compound XI has the advantages of simple reaction process, easy purification of intermediate, short preparation period, high product purify, and applicability to industrial production.

Description

technical field The present invention relates to a kind of preparation technology of compound, more specifically, the present invention relates to pemetrexed namely N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrole A new intermediate of [2,3-d]pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid and its application in the preparation of pemetrexed belongs to the field of medicine and chemical industry. Background technique Pemetrexed, the structure is as formula I, and the chemical name is N-[4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3-d]pyrimidine) -5-yl)ethyl]benzoyl]-L-glutamic acid, The configuration of the carbon represented by * is the L configuration. Pemetrexed is an antineoplastic drug that acts on folate-dependent pathways with multiple targets. DHFR), glycinamide nucleotide transformylase (GARFT), affects the synthesis of purine and pyrimidine through the inhibition of these key enzymes, and then inhibits DNA synthesis. Clinical studies have proved that its single...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C235/84C07C231/12C07D487/04
Inventor 林栋范传文王丽娟冷传新朱屹东张明会王晶翼
Owner QILU PHARMA CO LTD
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