Abstract
The asymmetric addition intramolecular cyclization reaction to produce the piperazic acid precursor 3 was studied. A retroaddition of S -4-(phenylmethyl)oxazolidinyl-5-bromovalerimide to diazo-di-tert-butyl dicarboxylate in DMPU/THF was discovered. A process improvement based on the addition of catalytic tetra-butylammonium iodide to give 3 in 91% yield is reported.
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