Pilot Plant Preparation of tert-Butyl-4-(2-hydroxyethyl)-4-(pyrrolidin-1-yl)-piperidine-1-carboxylate, An Intermediate of Novel Antiarteriosclerotics, Via a Safe, Scalable Reformatsky-Type Reaction

Hiroshi Osato; Motonari Osaki; Takao Oyama

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Pilot Plant Preparation of tert-Butyl-4-(2-hydroxyethyl)-4-(pyrrolidin-1-yl)-piperidine-1-carboxylate, An Intermediate of Novel Antiarteriosclerotics, Via a Safe, Scalable Reformatsky-Type Reaction

机译：通过安全，可扩展的Reformatsky型反应制备4-（2-羟乙基）-4-（吡咯烷-1-基）-哌啶-1-甲酸叔丁酯的中间体，该中间体是新型抗动脉硬化药的中间体

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Reported here is a safe, scalable process via a Refbrmatsky-type reaction of iminium salt (4) followed by Red-Al reduction giving tert-butyl-4-(2-hydroxyethyl)-4-(pyrrolidin-1-yl)-piperidine-1-carboxylate (6), an intermediate of novel antiarteriosclerotics (1), The key points of this safe process are the use of trifluoroacetic acid (TFA) for the iminium Salt formation, vigorous stirring for the Reformatsky reaction, and slow addition of methyl bromoacetate. Pilot manufacturing on the 500 L scale was achieved.

机译：这里报道的是一种安全，可扩展的过程，方法是亚硝酸盐（4）进行Refbrmatsky型反应，然后进行Red-Al还原，得到4-（2-羟乙基）-4-（吡咯烷-1-基）-哌啶叔丁基-1-羧酸盐（6），新型抗动脉硬化药（1）的中间体，此安全过程的关键是使用三氟乙酸（TFA）形成亚胺盐，剧烈搅拌以促进Reformatsky反应以及缓慢加入溴乙酸甲酯。实现了500升规模的中试生产。

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《Organic process research & development》 |2011年第6期|共5页
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Hiroshi Osato; Motonari Osaki; Takao Oyama;
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1. Pilot Plant Preparation of tert-Butyl-4-(2-hydroxyethyl)-4-(pyrrolidin-1-yl)-piperidine-1-carboxylate, An Intermediate of Novel Antiarteriosclerotics, Via a Safe, Scalable Reformatsky-Type Reaction [J] . Hiroshi Osato, Motonari Osaki, Takao Oyama Organic process research & development . 2011,第6期

机译：通过安全，可扩展的Reformatsky型反应制备4-（2-羟乙基）-4-（吡咯烷-1-基）-哌啶-1-甲酸叔丁酯的中间体，该中间体是新型抗动脉硬化药的中间体
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3. A convenient synthesis of 4-(2-hydroxyethyl)indolin-2-one, a useful intermediate for the preparation of both dopamine receptor agonists and protein kinase inhibitors [J] . Carlo Matera, Marta Quadri, Silvia Pelucchi Monatshefte fur Chemie . 2014,第7期

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4. PILOT PLANT SCALE-UP OF A PHARMACEUTICAL INTERMEDIATE [C] . Guillermo Daniel Zappi, Norman L.Weinberg The Meeting of the Electrochemical Society . 2000

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Pilot Plant Preparation of tert-Butyl-4-(2-hydroxyethyl)-4-(pyrrolidin-1-yl)-piperidine-1-carboxylate, An Intermediate of Novel Antiarteriosclerotics, Via a Safe, Scalable Reformatsky-Type Reaction

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