Camptothecin → HCID 4442037, compound

Participants

Reaction Conditions

Reaction Steps

Sodium borohydride (14 g, 370 mmol) is added in portions to a suspension of (S)-(+)-camptothecin (14 g, 40 mmol, that may be obtained using different commercial sources such as Aldrich Chemical Co. (Milwaukee, Wis.)), in methanol (750 ml) and the resulting mixture is heated slowly to 55° C. so as to obtain a clear solution that is then agitated for 16 hours at ambient temperature. The solvent is then evaporated under reduced pressure, the residue is recovered in water (250 ml), neutralized by the addition of acetic acid (21 ml) and left alone for 2 hours at 4° C. The resulting suspension is filtered and washed successively with cold water, acetone and diethyl ether, which, after drying under reduced pressure, permits obtaining the sought compound in the form of a white solid, m.p. 280° C.

Provenance & Evidence