Radiosynthesis of antitumor spliceosome modulators

► The radiosynthesis of two antitumor drug lead compounds; analogs of FR901464. ► Tritium incorporation via reduction of a (S)-4-acetoxypent-2-ynoic acid derivative. ► The amidation of (S,Z)-4-acetoxypent-2-enoic acid derivative to obtain analogs. ► These analogs are important tools for biochemical and pharmacology experiments.