4.4 Article

Synthesis of hindered tertiary amines by a mild reductive amination procedure

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TETRAHEDRON LETTERS
卷 48, 期 3, 页码 365-369

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PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2006.11.082

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organocatalysis; synthetic methodology; tertiary amines; reductive amination; Hantzsch ester

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An efficient metal-free procedure for the synthesis of tertiary amines by the reductive animation of carbonyl compounds is reported, which allows a convergent access to sterically hindered amines of the general formulas NR(R')(2) and NRR'R. The mild and operationally simple protocol uses the Hantzsch ester for transfer hydrogenation and catalytic amounts of thiourea for imine activation. (c) 2006 Elsevier Ltd. All rights reserved.

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