Emtricitabine → HCID 131725250, compound

Participants

Reaction Steps

The following example illustrates the state of the art using high amounts of enzyme catalysts in a of homogeneous system. To a solution of 1 ml of Altus PLE solution 650 units/ml from Altus Biologics, Inc. in 39 ml of 0.3 M phosphate buffer (pH 7.5) was added 10 ml of 10% FTC butyrate in isopropanol. The resulting mixture was stirred 24˜26° C. and the reaction progress was monitored by HPLC. The conversion reached 51% and the optical purity of the remaining chiral nonracemic ester compound was greater than 99% (48% chemical yield) after a 22 h reaction. These results are based on HPLC analysis of the remaining chiral nonracemic ester compound. The aqueous layer included hydrolyzed products (+)-FTC and (−)-FTC. The ratio of (+)-FTC and (−)-FTC was 96.6 to 3.4. The organic layer was evaporated to give 0.457 g of (−)-FTC butyrate.

Provenance & Evidence