流动化学在药物合成中最新进展.docVIP

. . 　　 本文档下载自 HYPERLINK / 文库下载网，内容可能不完整，您可以点击以下网址继续阅读或下载：  HYPERLINK /doc/6ecdc8126bd97f192279e9cb.html /doc/6ecdc8126bd97f192279e9cb.html 流动化学在药物合成中的最新进展 有机化学 Chinese Journal of Organic Chemistry DOI: 10.6023/cjoc201208002 学术动态 REPORT 流动化学在药物合成中的最新进展 赵东波 (拜耳技术工程(上海)有限公司 上海201507) 摘要 作为不断成熟的一项过程强化技术, 流动化学近十年来不论在学术研究还是工业应用方面均取得令人瞩目的发展; 综述了流动化学技术在药物合成中的最新研发进展. 当前的流动化学技术与其早期的研究相比有许多突破, 例如不再局限于某类反应可行性概念的验证、越来越多的知名国际制药企业公开发展该技术以及已经有不少相关多步全合成成功案例的报道等. 在简单介绍流动化学的优势、存在的挑战和应对之策之后, 列举大量实例从不同工艺类型重点介绍流动化学在多步复杂药物合成工艺中的最新进展. 关键词 流动化学; 微反应器; 微反应技术; 药物合成; 多步流动合成; 工艺类型 Updated Applications of Flow Chemistry in Pharmaceutical Synthesis Zhao, Dongbo (Bayer Technology and Engineering (Shanghai) Co. Ltd., Shanghai 201507) Abstract As a further-developing process intensification technology, flow chemistry has achieved a striking development either in academic or industrial area in the past decade. Updated applications of flow chemistry in pharmaceutical synthesis areoverviewed. Compared with its early research and development (RD)/doc/6ecdc8126bd97f192279e9cb.html, current flow chemistry has already shown a lot of breakthroughs. For instance, no more limitations to the proof of feasibility concept for some certain reaction, public develop-ment of this technology by more and more distinguished international pharmaceutical companies and quite a few correspond-ing reports of successful examples about multistep total synthesis of active pharmaceutical ingredients (APIs). Different proc-ess categorizations are emphasized with many API syntheses to demonstrate the up-to-date progress of this topic, after a brief introduction of the advantages, existing challenges and the corresponding solutions for flow chemistry. Keywords flow chemistry; microreactor; microreaction technology; API synthesis; multistep flow synthesis; process catego-rization [1a] 自从20 世纪90年代初Manz等首次提出了微全分析系统(miniaturized total analysis systems, μ-TAS)的概念以来, 微反应技术(Microreaction technolog/doc/6ecdc8126bd97f192279e9c