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Seven‐Step Continuous Flow Synthesis of Linezolid Without Intermediate Purification
Author(s) -
Russell M. Grace,
Jamison Timothy F.
Publication year - 2019
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/anie.201901814
Subject(s) - linezolid , continuous flow , yield (engineering) , residence time (fluid dynamics) , chemistry , flow chemistry , combinatorial chemistry , solvent , sequence (biology) , organic chemistry , materials science , bacteria , biochemical engineering , biochemistry , staphylococcus aureus , biology , geotechnical engineering , vancomycin , engineering , metallurgy , genetics
Herein, the blockbuster antibacterial drug linezolid is synthesized from simple starting blocks by a convergent continuous flow sequence involving seven (7) chemical transformations. This is the highest total number of distinct reaction steps ever performed in continuous flow without conducting solvent exchanges or intermediate purification. Linezolid was obtained in 73 % isolated yield in a total residence time of 27 minutes, corresponding to a throughput of 816 mg h −1 .