Lithium Chloride → HCID 13650110, compound

Participants

Reaction Steps

247 mg. (1 mmol) methyl 5-[(2-cyano-1-aziridinyl)-methyl]-6-methoxypyridine-2-carboxylate (see Example 1) are dissolved in 10 ml. of anhydrous tetrahydrofuran and the solution is mixed with 74 mg. (2 mmol) sodium borohydride and 84 mg. (2 mmol) lithium chloride. After stirring for 12 hours at ambient temperature, the same amounts of sodium borohydride and lithium chloride are again added and, after a further 12 hours, the reaction mixture is mixed with 5 ml. water, evaporated and the residue taken up in ethanol and filtered. The filtrate is evaporated, the residue is taken up in acetone, filtered and evaporated. The residue is purified over a silica gel column (elution agent: acetone/toluene 1:3 v/v) (Rf value about 0.3) to give 120 mg. (55% of theory) of the desired product; m.p. 68°-70° C.

Provenance & Evidence