2.6. Synthetic Application. The clinical candidate compound (+)-AG-041R is a gastrin/CCK-B receptor antagonist with an IC50 of 1.1 nmol. Few catalytic asymmetric methodologies have been developed for preparing this compound, but we envisioned that its core oxindole unit can be constructed from our arylation product by a reduction of the nitro group and an in situ intramolecular amidation reaction, and a new catalytic asymmetric synthetic route for this clinical candidate was anticipated. As we discussed in the section on substrate scope, the diethyl aspartate 1b reacted smoothly with 2-nitro fluorobenzene 2a under the optimal reaction conditions, and product 3o was obtained in 52% yield with > 99% ee. Then, we reduced the nitro group of 3o to an amine. An intramolecular amidation took place in situ to give 3-amino oxindole, product 11. Using the reported methods, urea moiety-contained oxindole 12 and Iwabuchi intermediate 13 were prepared, successively (Scheme 1). The spectra data and optical rotation of compound 13 agree with the literature (see Supporting Information). Thus, based on the chiral aldehyde-catalyzed arylation of amino acid esters, a new synthetic route for the formal synthesis of AG-041R was achieved. Scheme 1. The formal synthesis of AG-041R.