Synthesis of N -(4-propargylaminobenzoyl)-L-glutamates

Abstract

To facilitate the rather labour consuming synthesis of antifolate γ-oligo-L-glutamates including those with the propargyl group at position N10 , two synthons possessing this group, α-t-butyl γ-methyl N-(4-propargylaminobenzoyl)- L-glutamate (1) and a-t-butyl N-(4-propargylaminobenzoyl)-L-glutamate (2) have been elaborated (Scheme 2) and characterized by melting points, elemental analysis, NMR, TLC and HPLC. They are of purity >98.5% by the last method.

Keywords

• n-(4-propargylaminobenzoyl)-l-glutamates
• n10-propargyl antifolates. 'h nmr spectra
• hplc
• short column chromatography