Thermal N-Boc deprotection of a range of amines is readily effected in continuous flow, in the absence of an acid catalyst. While the optimum results were obtained in methanol or trifluoroethanol, deprotection can be effected in a range of solvents of different polarities. Sequential selective deprotection of N-Boc groups has been demonstrated through temperature control, as exemplified by effective removal of an aryl N-Boc group in the presence of an alkyl N-Boc group. As a proof of principle, a telescoped sequence involving selective deprotection of an aryl N-Boc group from 9h followed by benzoylation and deprotection of the remaining alkyl N-Boc group to form amide 13 proved successful.

中文翻译：

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N-Boc 保护胺在连续流中的选择性热脱保护

在不存在酸催化剂的情况下，一系列胺的热N -Boc 脱保护很容易在连续流中进行。虽然在甲醇或三氟乙醇中获得了最佳结果，但脱保护可以在一系列不同极性的溶剂中进行。已经通过温度控制证明了N -Boc基团的顺序选择性脱保护，如在烷基N -Boc基团存在下有效去除芳基N -Boc基团所例证的。作为原理证明，涉及从9h开始选择性脱保护芳基N -Boc 基团，然后苯甲酰化并脱除剩余烷基N -Boc 基团以形成酰胺13的伸缩序列被证明是成功的。