Asymmetric Organocatalysis and Continuous Chemistry for an Efficient and Cost-Competitive Process to Pregabalin

Carlone Armando; Bernardi Luca; McCormack PeterWarr TonyOruganti SrinivasCobley Christopher J.

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Asymmetric Organocatalysis and Continuous Chemistry for an Efficient and Cost-Competitive Process to Pregabalin

机译：Asymmetric Organocatalysis and Continuous Chemistry for an Efficient and Cost-Competitive Process to Pregabalin

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Herein, we present the scale up development of an innovative synthetic process to pregabalin. The process is underpinned by two enabling technologies critical to its success; continuous chemistry allowed a safe and clean production of nitroalkene, and asymmetric organocatalysis gave access to the chiral intermediate in an enantioenriched form. Crucial to the success of the process was the careful development of a continuous process to nitroalkene and optimization of the organocatalyst and of the reaction conditions to attain remarkably high turn-over frequency in the catalytic asymmetric reaction. Successful recycle of the organocatalysts was also developed in order to achieve a cost-competitive process.

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来源
《Organic process research & development》 |2021年第12期|2795-2805|共11页
作者
Carlone Armando; Bernardi Luca; McCormack PeterWarr TonyOruganti SrinivasCobley Christopher J.;
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作者单位

Dr Reddys Labs EU Ltd;

Dr Reddys Inst Life Sci;

Univ Bologna;

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原文格式 PDF
正文语种英语
中图分类化学工业;
关键词
Pregabalin; organocatalysis; continuous chemistry; asymmetric catalysis; ENANTIOSELECTIVE MICHAEL ADDITION; NONCOVALENT ORGANOCATALYSIS; STEREOSELECTIVE-SYNTHESIS; SQUARAMIDE; NITROALKENES; MEMBRANE; MALONATE; ACID;

Asymmetric Organocatalysis and Continuous Chemistry for an Efficient and Cost-Competitive Process to Pregabalin

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