CAS: 5400-79-3; Ethyl 3-Oxocyclopentanecarboxylate

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98-78-2 13012-38-9 71830-06-3

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环戊烯-1-羧酸甲酯置于chromium(Vi) Oxide,硫酸,Palladium On Activated Charcoal,氢气,乙酸酐体系中,用 二氯甲烷,溶剂黄146,乙酸乙酯 作为反应溶剂,化学反应生成 3-氧代环戊烷甲酸乙酯
参考文献:连续c-h羟基化,醇氧化和烯烃还原的生物催化合成手性环状γ-氧酸酯
标题:连续c-h羟基化,醇氧化和烯烃还原的生物催化合成手性环状γ-氧酸酯
摘要:描述了一种三步生物催化程序,用于将甲基和乙基环戊烯-和环己烯羧酸酯转化为相应的手性3-氧代酯的两种对映异构体,它们是合成活性药物成分的有用组成部分.起始环烯基羧酸酯的烯丙基羟基化反应通过使用米曲霉进行的.在25oc的乙酸盐缓冲溶液中,将静止的细胞截留在藻酸盐珠中.由漆酶/ Tempo系统进行的中间烯丙醇氧化为不饱和酮,以及烯键还原酶介导的烯烃键氢化反应是在同一反应容器中于30oc的连续模式下进行的.与报道的化学方法相比,我们的多步方法完全具有生物催化性,在选择性和环境影响方面具有相当大的优势.
DOI:10.1039/c7Gc02215H

专利信息

专利号:US-9861636-B2
优先权日:2014-04-29
标题 :Polyfluorinated compounds acting as bruton tyrosine kinase inhibitors
发明人：HE WEI
权利人:HE WEI; ZHEJIANG DTRM BIOPHARMA CO LTD
摘要:Described herein is a novel series of multi-fluoro-substituted pyrazolopyrimidine compounds or salts thereof. These compounds are Bruton's tyrosine kinase (BTK) inhibitors. These compounds may possess better BTK inhibition selectivity and pharmacokinetic properties. Disclosed herein are the synthesis methods of these compounds. Disclosed herein are novel synthesis methods of the multi-fluoro-substituted benzophenone and substituted phenoxy benzene. Also disclosed are pharmaceutical compositions comprising the BTK inhibitors described herein. The present invention also relates to pharmaceutical formulations comprising the compounds described herein as active ingredients. The present invention also includes the therapeutic methods by administering the BTK inhibitors and their formulations to treat and inhibit autoimmune disease, hypersensitivity disease, inflammatory diseases and cancer.