First- and Second-Generation Practical Syntheses of Chroman-4-one Derivative: A Key Intermediate for the Preparation of SERT/5-HT_(1A) Dual Inhibitors

Tomoaki Nishida; Hidefumi Yoshinaga; Tomohiro Toyoda

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First- and Second-Generation Practical Syntheses of Chroman-4-one Derivative: A Key Intermediate for the Preparation of SERT/5-HT_(1A) Dual Inhibitors

机译：Chroman-4-one衍生物的第一代和第二代实用合成：制备SERT / 5-HT_（1A）双重抑制剂的关键中间体

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Two approaches to large-scale synthesis of the key intermediate 9, a precursor of novel dual inhibitors of SERT/5-HT_(1A)receptor, are described. These two approaches each feature a mild and efficient method for construction of the chroman-4-one scaffold, which can be used with substrates containing base-sensitive functionalities and enable synthesis on kilogram scale without chromatographic purification. The first-generation synthesis enables quick delivery of a kilogram quantity of the key intermediate 9 with only one slurry purification step. On the other hand, the highly practical second-generation synthesis is suitable for the multikilogram campaign.

机译：描述了关键中间体9（一种新型的SERT / 5-HT_（1A）受体双重抑制剂的前体）的大规模合成方法。这两种方法各自以温和而有效的方法构建苯并二氢吡喃-4-酮骨架，可与含有碱基敏感功能的底物一起使用，并且无需进行色谱纯化即可以千克规模合成。第一代合成仅通过一个浆液纯化步骤就可以快速递送千克量的关键中间体9。另一方面，高度实用的第二代合成适合多千克运动。

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《Organic process research & development》 |2012年第4期|共10页
作者
Tomoaki Nishida; Hidefumi Yoshinaga; Tomohiro Toyoda;
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机译：Chroman-4-one衍生物的第一代和第二代实用合成：制备SERT / 5-HT_（1A）双重抑制剂的关键中间体
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First- and Second-Generation Practical Syntheses of Chroman-4-one Derivative: A Key Intermediate for the Preparation of SERT/5-HT_(1A) Dual Inhibitors

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