Several novel and very potent folate antimetabolites, structurally based upon our previously described “open-chain” version of DDATHF but carrying 1-carbon substituents in the 10- position, have been synthesized. A key synthetic sequence involving a palladium-catalyzed C C coupling reaction, oxymercuration, and Wittig olefination constitutes a new route to α- branched 4-styrene carboxylic acids. Classical construction of the pyrimidine ring from the ...