Synthesis of methotrexate, anticancer compound, catalyzed by iodide


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Jerzy Król-Bogomilski Ph.D.


Synthesis of methotrexate, folic acid analogue

metotrexat, metotreksat manufacturing

I propose the efficient way of the synthesis of methotrexate.

The yield and the reactions rate is relatively high.

I propose the use of potassium iodide KI as a catalyst to obtain the title compound.

The catalysts may be other iodides, sodium iodide NaI for instance.

This catalyst enhances both yield and rate of the key reaction step.

This organic synthesis of methotrexate has three steps.

The use of polar solvents is essential.

The substrates in the metotrexat synthesis are:


diethyl N-[4-(methylamino)benzoyl]-L-glutamate

1,3-dihydroxyacetone

2,4,5,6-tetraaminopyrimidine


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