反应详情

The synthesis of alkyne 5 is shown in Scheme 2. Aldehyde 2, though available from Aldrich, is expensive, therefore it can be more economical to prepare it from relatively inexpensive 4-bromobenzaldehyde 1 following a literature procedure as described in Thorand, S. and Krause, N. J. Org. Chem. 1998, 63, 8551. Next, reductive amination of aldehyde 2 with methylamine can afford amine 3, which can be subsequently protected to give methyl carbamate 4. Removal of the trimethylsilyl group (TMS) under basic conditions can yield 5 in 90% yield.