One-pot method to construct isoindolinones and its application to the synthesis of DWP205109 and intermediate of Lenalidomide

Transition metal-free advanced synthetic approaches for isoindolinones and their fused analogues

“…10 Herein, we are interested in the synthetic pathways for isoindolinones and their fused analogues from available starting materials that do not contain any isoindolinone scaffolds in the initial step. Although there is a greater number of reports available on transition-metal catalyzed reactions 11 a – g via the reduction of the number of reaction steps to obtain the most available isoindolinone-based structures, transition metal-free protocols 12–53 offer various advantages over transformations involving transition metal catalysts. Transition metal-catalyzed protocols have the following drawbacks: (a) most metals are very sensitive to air and moisture, (b) toxic metals can easily mixed with drainage water during work-up, and (c) the high cost of metal catalysts is another barrier in the pharmaceutical industry.…”

Measurement of the Thermal Conductivities of Methyl 2-Methyl-3-nitrobenzoate + Acetonitrile, N-Bromosuccinimide + Acetonitrile, and Methyl 2-Methyl-3-nitrobenzoate + N-Bromosuccinimide + Acetonitrile in the Temperature Range from 300 to 340 K

“…Therefore, it is urgent to reduce the fabrication costs of the drug to satisfy the demand of the public. In the prepared process of lenalidomide, methyl 2-bromomethyl-3-nitrobenzoate frequently used is one of the most important intermediates , whose production process is a bromination reaction with methyl 2-methyl-3-nitrobenzoate (MMN) and N -bromosuccinimide (NBS) as the raw material. , Accordingly, improving the yield of methyl 2-bromomethyl-3-nitrobenzoate, as well as reducing its reactive energy consumption, will be important methods to reduce costs.…”