Trifluoroacetic acid → HCID 178461862, compound

Participants

Reaction Steps

7 g of the product of Example 3 were suspended in 140 ml of methylene chloride and 70 ml of trifluoroacetic acid were slowly added with the temperature falling to 15° C. Contact was maintained for 4 hours and then, after concentrating to dryness under reduced pressure, the residue was taken up in 100 ml of ether. The crystals were separated by filtration and the product was slowly added to 50 ml of a 10% aqueous solution of sodium bicarbonate. After stirring, filtration, and washing with water, the crude product was treated at reflux with 300 ml of methanol without complete solution and after cooling and concentrating to 50 ml, 2.3 g of 2-[(R) 1-aminoethyl]-4-hydroxy-N-(2-thiazolyl)-8-trifluoromethyl-3-quinoline-carboxamide melting at 265° C. and with a specific rotation of [α]D =-72°±2.5° (c=0.5% in CH3COOH) were obtained.

Provenance & Evidence