Hydrochloric Acid → Amphotericin B Calcium Succinic Acid

Participants

Reaction Steps

10.66 g amphotericin B (938γ/mg of activity-equivalent to 10 g of chemical activity) suspended in 2.5 liters of anhydrous methanol containing 11.1 ml of 5% CaCl2 in methanol (equivalent to 200 mg Ca ion) is solubilized by means of 1.8 ml of 5.8 N HCl (pH 3.9). To the resulting solution are added 100 ml of methanol containing 10 g of reagent grade succinic acid to form a mixture of pH 3.2. The pH of the mixture is adjusted to about 7 by the addition of 7.7 ml concentrated NH 4 OH. The mixture is then heated to 45°-50° C and slurried for one hour and thereafter is cooled to room temperature, filtered and the wet cake dried overnight under vacuum at 45° C to yield 9.1 g of crystalline complex.

Provenance & Evidence