- Continuous Platform to Generate Nitroalkanes On-Demand (in Situ) Using Peracetic Acid-Mediated Oxidation in a PFA Pipes-in-Series Reactor
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The synthetic utility of the aza-Henry reaction can be diminished on scale by potential hazards associated with the use of peracid to prepare nitroalkane substrates and the nitroalkanes themselves. In response, a continuous and scalable chemistry platform to prepare aliphatic nitroalkanes on-demand using the oxidation of oximes with peracetic acid and direct reaction of the nitroalkane intermediate in an aza-Henry reaction is reported. A uniquely designed pipes-in-series plug-flow tube reactor addresses a range of process challenges, including stability and safe handling of peroxides and nitroalkanes. The subsequent continuous extraction generates a solution of purified nitroalkane, which can be directly used in the following enantioselective aza-Henry chemistry to furnish valuable chiral diamine precursors with high selectivity, thus completely avoiding isolation of the potentially unsafe low-molecular-weight nitroalkane intermediate. A continuous campaign (16 h) established that these conditions were effective in processing 100 g of the oxime and furnishing 1.4 L of nitroalkane solution.
- Tsukanov, Sergey V.,Johnson, Martin D.,May, Scott A.,Kolis, Stanley P.,Yates, Matthew H.,Johnston, Jeffrey N.
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supporting information
p. 971 - 977
(2018/08/28)
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- Inhibitors of Src and Lck protein kinases
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The present invention provides compounds of formula I: or a pharmaceutically acceptable derivative thereof, wherein A-B is N—O or O—N and G, R1, R2, R3, and R4 are as described in the specification. These compou
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- Highly efficient and catalytic conversion of aldoximes to nitriles
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(Matrix Presented) Catalytic dehydration of aldoximes can be performed highly efficiently with a catalyst system of [RuCl2(p-cymene)]2/molecular sieves under essentially neutral and mild conditions, and various types of cyano compounds are produced in good to excellent yields.
- Yang, Soon Ha,Chang, Sukbok
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p. 4209 - 4211
(2007/10/03)
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- CYCLOALKYL N-HYDROXY DERIVATIVES HAVING LIPOXYGENASE INHIBITORY ACTIVITY
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Where M is hydrogen, a pharmaceutically acceptable cation or metabolically cleavable group, R is alkyl, cycloalkyl, or NR'R2, where R1 and R2 are hydrogen, alkyl, cycloalkyl alkonyl, or carbocyclic aryl, Y is alkylene, alkenylene, or cyclopropyl, and A is
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