Dichloromethane → Diisopropylethylamine

Participants

Reaction Steps

A tricyclic benzodiazepine of formula (1) is treated with an appropriately substituted haloaroyl (heteroaroyl) halide, preferably a fluoro aroyl or a fluoro (or chloro) heteroaroyl chloride of formula (29), in the presence of a base such as triethylamine or diisopropylethylamine in an aprotic organic solvent such as dichloromethane or tetrahydrofuran at temperatures from 40° C. to the reflux temperature of the solvent to yield the acylated derivative (30).

Provenance & Evidence