An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.

The present invention provides salts of Pralatrexate, in particular, sodium, lithium and potassium salts and their polymorphic forms, process for the preparation thereof, pharmaceutical compositions comprising these salts and at least one pharmaceutically acceptable excipient, and the use of pharmaceutical composition for the treatment of conditions related to human tumors.

An improved process for the preparation of Pralatrexate which is less hazardous. The invention further relates to novel intermediates and process thereof useful for the preparation of Pralatrexate. The present invention also relates to a substantially pure Pralatrexate and a process for obtaining the same in high yield.

The specification relates to a process for preparation of an antifolate compound of formula 7, such as Pralatrexate. Also, disclosed are intermediates and processes for preparation of intermediates useful in the preparation of the antifolate compound. The substituents Y, Z, R, R1 and R2 are as described herein. The processes and intermediates can provide an alternate route to the synthesis of the antifolate compound. Further, the processes can help to avoid distillation or evaporation of high bo...

A process for preparation of 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid and other key intermediates in synthesis of 10-propargyl-10-deazaaminopterin (Pralatrexate) and the intermediates thereof. The 10-propargyl-10-deazaaminopterin (Pralatrexate) is obtained by peptide formation and ester hydrolysis of the intermediate compound 4-(1-(2,4-diaminopteridin-6-yl)pent-4-yn-2-yl)benzoic acid by methods known in the art.

Processes for preparing and purifying Pralatrexate are described in the present application, as well as intermediates in these processes, and salts and solid state forms of the Pralatrexate intermediates.