An intermolecular approach to the construction of 3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazines is reported for the first time using the oxa-Pictet–Spengler reaction. The method involves a sequence of carbon–carbon- and carbon–oxygen-bond formation between a substituted 2-(1H-pyrrol-1-yl)ethan-1-ol and an aldehyde/ketone. p-Toluenesulfonic acid (pTSA) was identified as a suitable catalyst to promote the reaction. The method provides a one-step conversion of various aldehydes/ketones into the corresponding 3,4-dihydro-1H-pyrrolo[2,1-c][1,4]oxazines. © 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim

中文翻译：

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通过theoxa-Pictet-Spengler反应轻松进入3,4-二氢-1H-吡咯并[2,1-c][1,4]恶嗪

首次报道了使用 oxa-Pictet-Spengler 反应构建 3,4-二氢-1H-吡咯并 [2,1-c][1,4] 恶嗪的分子间方法。该方法涉及在取代的 2-(1H-pyrrol-1-yl)ethan-1-ol 和醛/酮之间形成一系列碳-碳和碳-氧键。对甲苯磺酸 (pTSA) 被认为是促进反应的合适催化剂。该方法提供了将各种醛/酮一步转化为相应的 3,4-二氢-1H-吡咯并 [2,1-c][1,4] 恶嗪的方法。© 2016 WILEY-VCH Verlag GmbH & Co. KGaA, Weinheim