A scale-friendly alternate route to CP-547,632, a VEGF inhibitor for cancer treatment, was developed.  Dimethyl malonate was treated sequentially with base, carbon disulfide, dimethyl sulfate, and hydroxylamine-O-sulfonic acid to give isothiazole 3 in ~70% yield.  Next, a sulfide to sulfone oxidation protocol utilizing an in situ protecting group was optimized, followed by a regioselective O-benzylation to give 4.  Ammonia displacement of the sulfone, urea formation, and finally ammonia displacement of the methyl ester resulted in CP-547,632 in high yield.