Scheme 3: Synthesis of oxazolines through catalytic cyclodehydration. Many oxazoline natural products contain a hydroxamate group present in metal binding-siderophores such as acinetobactin. These are attractive synthetic targets due to their therapeutic potential to treat Gram-negative bacterial infections and to interrogate the biology of iron. Oxazoline L-161,240 is an inhibitor of LpxC activity, a key enzyme involved in the early steps of lipid A biosynthesis (Scheme 4). We found that the O-benzyl protected hydroxamate 37 could be cyclized to 38 in 46% yield, demonstrating the effectiveness of the 6methylpicolinate ligands. The synthesis of compound L-161,240 39 was completed by hydrogenation, which conserved the hydroxamic acid while selectively cleaving the benzyl group. In conclusion, we have demonstrated that bis-(6-methylpicolinate) molybdenum (VI) dioxide is an excellent and highly robust dehydrative cyclization catalyst. This system holds advantages over stoichiometric dehydrating agents due to the selectivity and compatibility with various reactive functional groups. The mild conditions used in the reaction enable cyclodehydration even with sensitive substrates, including the conservation of potentially epimerization-pone positions.