Lactic acid-mediated tandem one-pot synthesis of 2-aminothiazole derivatives: A rapid, scalable, and sustainable process

Mohan Reddy Bodireddy; P.Md. Khaja Mohinuddin; Trivikram Reddy Gundala; N.C. Gangi Reddy

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Lactic acid-mediated tandem one-pot synthesis of 2-aminothiazole derivatives: A rapid, scalable, and sustainable process

机译：乳酸介导的串联一锅法合成2-氨基噻唑衍生物：快速，可扩展且可持续的过程

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Environmentally benign and biodegradable lactic acid is identified as alternative solvent and catalyst for the tandem one-pot synthesis of Hantzsch 2-aminothiazole derivatives (4) from readily available aralkyl ketones (1) through in situ regioselective α-bromination using N -bromosuccinimide (2) followed by heterocyclization using thiourea (3) at 90–100°C. The major advantages of the present method include short reaction times (10–15?min), practical, simple to perform, easy work-up, good yield of products (up to 96%), productive for large-scale applications, free from apply of α-bromoketones (lachrymator) as substrates, avoids column purification. Hence, the present method meets with the concepts of both Wender’s “ideal synthesis” and sustainable chemical process.

机译：已鉴定出对环境无害且可生物降解的乳酸，它是使用从现成的芳烷基酮（1）通过原位区域选择性α-溴化串联合成一锅Hantzsch 2-氨基噻唑衍生物（4）的替代溶剂和催化剂> N-溴代琥珀酰亚胺（2），然后在90–100°C下使用硫脲（3）进行杂环化。本方法的主要优点包括反应时间短（10-15分钟），实用，易于执行，易于后处理，产品收率好（高达96％），可用于大规模应用且无使用α-溴代酮（催乳剂）作为底物，避免柱纯化。因此，本方法符合Wender的“理想合成”和可持续化学过程的概念。

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《Cogent Chemistry》 |2016年第1期|共13页
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Mohan Reddy Bodireddy; P.Md. Khaja Mohinuddin; Trivikram Reddy Gundala; N.C. Gangi Reddy;
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7. Lactic acid-mediated tandem one-pot synthesis of 2-aminothiazole derivatives: A rapid, scalable, and sustainable process [O] . Mohan Reddy Bodireddy, P.Md. Khaja Mohinuddin, Trivikram Reddy Gundala, 2016

机译：乳酸介导的串联一锅法合成2-氨基噻唑衍生物：快速，可扩展和可持续的过程

Lactic acid-mediated tandem one-pot synthesis of 2-aminothiazole derivatives: A rapid, scalable, and sustainable process

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