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Download fileEnantioselective Synthesis of H‑Phosphinic Acids Bearing Natural Amino Acid Residues
journal contribution
posted on 2013-07-19, 00:00 authored by Qiuli Yao, Chengye YuanThe
first systematic study on the asymmetric synthesis of H-phosphinic acids bearing natural protein amino acid residues was
reported on the basis of the asymmetric addition of ethyl diethoxymethylphosphinate
to N-tert-butanesulfinyl imines.
Good yields and moderate to high enantioselectivities were obtained.
Reliable methods were developed for the elucidation of the stereochemistry
of these phosphinic acids and derivatives thereof. The transformation
of the side chains of these analogues was studied. Methods for the
conversion of the α-aminophosphinates to oligopetides were reported.