Tetrahedron Letters

A convenient route to 1-benzyl 3-aminopyrrolidine and 3-aminopiperidine

L Jean, I Baglin, J Rouden, J Maddaluno, MC Lasne

文献索引：Jean, Ludovic; Baglin, Isabelle; Rouden, Jacques; Maddaluno, Jacques; Lasne, Marie-Claire Tetrahedron Letters, 2001 , vol. 42, # 33 p. 5645 - 5649

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被引用次数: 25

摘要

1-Benzyl 3-aminopyrrolidine 1 and 1-benzyl 3-aminopiperidine 2 were prepared rapidly mainly in aqueous conditions in 55 and 75% yields, respectively, on a multi-gram scale starting from inexpensive and commercially available starting materials. The key step involved the Curtius rearrangement mediated by sodium nitrite and trifluoroacetic acid of the appropriate acylhydrazides. All the reactions (except LAH reductions) were performed in ...