Continuous-flow synthesis of acyclic amides and macrolactams has been demonstrated successfully via N-benzylation of amides using a highly reusable heterogeneous Ru-Zeolite as a catalyst, which gives only water as the byproduct. N-Benzylation of acyclic amides furnished 30 N-benzylated amides whereas intramolecular N-benzylation with alcohols was well tolerated with 15 examples of macrolactams bearing 11- to 15-membered rings. Notably, the scalability of this flow process has been demonstrated from milligrams to gram scale using the Ru-Zeolite heterogeneous catalyst. Moreover, the reusability of the catalyst is exemplified by the 16 reaction cycles carried out with one time-packed heterogeneous catalyst in the reactor bed.

中文翻译：

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钌-沸石催化的酰胺脱水 N-苄基化反应用于在连续流下构建大内酰胺


通过使用高度可重复使用的异质 Ru-沸石作为催化剂，仅产生水作为副产品，通过酰胺的 N-苄基化成功证明了无环酰胺和大内酰胺的连续流合成。无环酰胺的 N-苄基化提供了 30 个 N-苄基化酰胺，而与醇的分子内 N-苄基化反应对 15 个带有 11 至 15 元环的大内酰胺类化合物耐受性良好。值得注意的是，使用 Ru-沸石异相催化剂已经证明了该流动过程的可扩展性从毫克级到克级。此外，催化剂的可重复使用性还体现在反应床层中用一种时间填充的非均相催化剂进行的 16 次反应循环中。