L. Yin
2013
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Journal
Applied Chemical Industry
Abstract
2-Halomethyl-3-nitrobenzoate(2) was obtained from 2-methyl-3-nitrobenzoate(1) via halogenation reactions.Glutamine methyl ester(4) was obtained from L-glutamine(3) via esterification,3-amino-piperidine-2,6-dione(7) was obtained from intramolecular cyclization under Boc reagent,condensing agent and catalyst.Compound(2) and(7) cyclization under weak base condensation,followed by nitro-reduction to give lenalidomide(9).This synthetic method can shorten reaction steps,reduce production costs and improve yield to about 40% in a mild reaction condition.