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Asymmetric Synthesis via Heterocyclic intermediates, L. – Trichloroacetimidates, II. Asymmetric Synthesis of α-Amino Acid Benzyl Esters via the Bisbenzyl Bislactim Ether of cyclo(-L-Val-Gly-)

✍ Scribed by Groth, Ulrich ;Schmeck, Carsten ;Schöllkopf, Ulrich


Publisher
John Wiley and Sons
Year
1993
Tongue
English
Weight
322 KB
Volume
1993
Category
Article
ISSN
0947-3440

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✦ Synopsis


Abstract

The diketopiperazine cyclo(‐L‐Val‐Gly‐) (1) can be O‐alkylated under mild acidic reaction conditions with the alkyl trichloroacetimidates 2 to the corresponding bisalkyl bislactim ethers. Alkylation of the bisbenzyl bislactim ether anion of cyclo(‐L‐Val‐Gly‐) 4c with benzyl bromide and subsequent hydrolysis with aqueous trifluoroacetic acid afforded D‐phenylalanine benzyl ester (8) with an enantiomeric excess of > 95%.