4-[2-(2-Amino-4,7-dihydro-4-oxo-1H-pymol[2,3-d]pyrimodin-5-yl)ethyl]benzoic acid, as key intermediates of pemetrexed disodium, is used in the synthesis of antitumor drugs and is also an important chemical building block in drug development and analysis. Pemetrexed disodium is a multi-target antifolate metabolism antitumor drug, clinically used to treat diseases such as non-small cell lung cancer and malignant pleural mesothelioma.
Methyl 4-[2-(2-amino-4,7-dihydro-4-oxo-1H-pyrrolo[2,3-d]pyrimidin-5-yl)ethyl]benzoate was obtained from the dehydration condensation of its corresponding 2,4-diamino-6-hydroxypyrimidine and corresponding 2-bromoaldehyde under certain conditions, and the ester product obtained was hydrolyzed to carboxylic acid under alkaline conditions to obtain 4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3]pyrimidin-5-yl)ethyl]benzoic acid. 4-[2-(2-amino-4,7-dihydro-4-oxo-3H-pyrrolo[2,3]pyrimidin-5-yl)ethyl]benzoic acid.