New crystal form of pemetrexed diacid and preparation method thereof

A crystal form, dihydrogen technology, applied in the field of medicinal chemistry, can solve the problems of long preparation time, difficult separation, and difficult removal, etc., and achieves the effect of simple preparation method, small electrostatic effect, and improved quality.
CN106478632AActive Publication Date: 2017-03-08JIANGSU HANSOH PHARMA CO LTD +1
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
JIANGSU HANSOH PHARMA CO LTD
Publication Date
2017-03-08

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Abstract

The invention discloses a new crystal form of pemetrexed diacid and a preparation method thereof. Specifically, the invention relates to a new crystal form of N-{4-[2-(2-amino-4, 7-dihydro-4-oxy-1 H-pyrrole [2, 3-d] pyrimidine-5-yl) ethyl] benzoyl}-L-glutamate dehydrate and a preparation method thereof, wherein an XRPD (X-ray powder diffraction) spectrum of the new crystal form at least contains diffraction peaks of 2theta + / -0.20 degree of 5.7, 11.5, 12.3, 18.4, 20.3, 27.6 and 28.1. The new crystal form has the advantages of good stability, high purity, simple preparation and easy operation, and is suitable for industrial production.
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Description

technical field

[0001] The present invention relates to the field of medicinal chemistry, in particular to N-{4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrole[2,3-d]pyrimidin-5-yl)ethyl Base]benzoyl}-L-glutamic acid dihydrate new crystal form and its preparation method and pharmaceutical use. Background technique

[0002] N-{4-[2-(2-Amino-4,7-dihydro-4-oxo-1H-pyrrole[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L- Glutamic acid dihydrate (formula I, pemetrexed diacid) has the following structure:

[0003]

[0004] N-{4-[2-(2-Amino-4,7-dihydro-4-oxo-1H-pyrrole[2,3-d]pyrimidin-5-yl)ethyl]benzoyl}-L- Glutamic acid dihydrate (I) is an antifolate metabolite, which enters cells through reduced folic acid carrier, α-folate receptor and diprotic folic acid carrier, and rapidly generates polyglutamine in vivo catalyzed by folic acid polyglutamic acid synthase Pemetrexed acid; more stable and better affinity for target enzymes than monomer, N-{4-[2-(2-amino-4,7-dihydro-4-oxo-1H -pyrrole[2,3-d...

Claims

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