DIASTEREOSELECTIVITY IN THE ALKYLATION OF CHIRAL 2-AMINOMETHYL-1,3,2-DIOXAPHOSPHORINANE 2-OXIDES

Abstract
The alkylation of chiral cyclic diesters of α-aminomethyl-phosphonate derivatives was investigated as a potential route to the asymmetric synthesis of phosphonic acid analogs of α-amino acids. The 1,3,2-dioxaphosphorinanes derived from d,l-2,4-pentanediol (1D-c and 1D-d), which adopt primarily the C-equatorial conformation, were compared to the homologs 1T-c and 1T-e derived from 2-methyl-2,4-pentanediol, in which the aminomethyl moiety is fixed in the axial configuration. While neither series shows high stereoselectivity (de ≤ 50%), it was shown that the two chiral auxiliaries produce asymmetric induction of the opposite sense.

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