A versatile synthesis of α-amino bisphosphonates has been achieved through one-pot interrupted Ritter-type reaction under mild conditions. The reactive Ritter intermediate nitrilium is in situ generated by treatment of nitrile with readily accessible Tf₂O/HC(OR¹)₃, which is trapped by phosphite ester to deliver the desired product. This protocol is efficient, scalable, and well compatible with a broad scope of substrates. In addition, plentiful characteristic J_P–C couplings including unusual five-bond long-range ⁵J_P–C and ³J_P–C across quaternary carbon and hetero (N) atoms were observed in ¹³C NMR spectra.

中文翻译：

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通过 Tf2O/HC(OR)3 介导的间断 Ritter 型反应从腈中一锅法合成 α-氨基双膦酸盐

通过在温和条件下的一锅中断 Ritter 型反应实现了 α-氨基双膦酸盐的通用合成。反应性 Ritter 中间体腈是通过用容易获得的 Tf ₂ O/HC(OR ¹ ) _3处理腈原位产生的，它被亚磷酸酯捕获以提供所需的产物。该协议高效、可扩展，并且与广泛的底物兼容。此外，在季碳和杂（N）原子上观察到丰富的特征J _P-C偶联，包括不寻常的五键长程⁵ J _P-C和³ J _P-C¹³ C 核磁共振谱。