化学
卡托普利
流动化学
试剂
化学合成
组合化学
对映选择合成
猝灭(荧光)
立体选择性
催化作用
有机化学
连续流动
色谱法
微型反应器
作者
Valerio De Vitis,Federica Dall'Oglio,Andrea Pinto,Carlo De Micheli,Francesco Molinari,Paola Conti,Diego Romano,Lucia Tamborini
出处
期刊:ChemistryOpen
[Wiley]
日期:2017-10-01
卷期号:6 (5): 668-673
被引量:36
标识
DOI:10.1002/open.201700082
摘要
The chemoenzymatic flow synthesis of enantiomerically pure captopril, a widely used antihypertensive drug, is accomplished starting from simple, inexpensive, and readily available reagents. The first step is a heterogeneous biocatalyzed regio- and stereoselective oxidation of cheap prochiral 2-methyl-1,3-propandiol, performed in flow using immobilized whole cells of Acetobacter aceti MIM 2000/28, thus avoiding the use of aggressive and environmentally harmful chemical oxidants. The isolation of the highly hydrophilic intermediate (R)-3-hydroxy-2-methylpropanoic acid is achieved in-line by using a catch-and-release strategy. Then, three sequential high-throughput chemical steps lead to the isolation of captopril in only 75 min. In-line quenching and liquid–liquid separation enable breaks in the workflow and other manipulations to be avoided.
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