Synthesis of Arylglycines by Reaction of Diethyl N-Boc-iminomalonate with Organomagnesium Reagents
Patrizia Calí, Mikael Begtrup*
*Department of Medicinal Chemistry, Royal Danish School of Pharmacy, Universitetsparken 2, 2100 Copenhagen, Denmark, Email: mbdfuni.dk
P. Cali, M. Begtrup, Synthesis, 2002, 63-64.
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Diethyl N-Boc-iminomalonate, prepared on multi-gram scale, served as a stable and highly reactive electrophilic glycine equivalent which reacted with organomagnesium compounds affording substituted aryl N-Boc-aminomalonates. Subsequent hydrolysis produced arylglycines.
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amino acids, arylaminomalonates, arylglycines, imino esters, Grignard reaction, tert-butyl carbamates, decarboxylation