Development of synthesis of chiral nitrogen-containing building blocks

我们发现Ru(CO)-salen配合物是一种有效的催化剂，用于以N-(2-三甲基甲硅烷基)乙磺酰叠氮化物作为氮烯前体进行乙烯基酮的氮丙啶化反应。该反应与几乎对映体纯的氮丙啶酮发生。此外，我们还可以证明 ( )-PD 128907 的对映选择性短步骤正式合成，它是一种有效的多巴胺 D3 受体激动剂。

We found that Ru(CO)-salen complex is a potent efficient catalyst for the aziridination of vinyl ketones with N-(2-trimethylsilyl)ethanesulfonyl azide as a nitrene precursor. The reaction generated with almost enantiomerically pure aziridino ketones. Furthermore, we could demonstrate that enantioselective short step formal synthesis of (+)-PD 128907 which is a potent dopamine D3 receptor agonist.