Patent ID: 8227450
Filing Date: 2012-07-24
Classification: C07F

Abstract:
1. A process for synthesizing a compound of formula IIIA: the process comprising the step of acylating a compound of formula XIV: with a reactive amino acid having structure: wherein LG represents a leaving group and wherein n is 3 or 4, wherein X and Y, the same or different, are selected from the group consisting of H, a straight alkyl group of 1 to 6 carbon atoms, a branched alkyl group of 3 to 6 carbon atoms, a cycloalkyl group of 3 to 6 carbon atoms, F, Cl, Br, I, —CF wherein R a picolyl group selected from the group consisting of a picolyloxy group selected from the group consisting of a substituted pyridyl group selected from the group consisting of and a group of formula: wherein R 2 is selected from the group consisting of a diphenylmethyl group of formula IV: a naphthyl-1-CH 2 — group of formula V: a naphthyl-2-CH 2 — group of formula VI: wherein X′ and Y′, the same or different, are selected from the group consisting of H, a straight alkyl group of 1 to 6 carbon atoms, a branched alkyl group of 3 to 6 carbon atoms, a cycloalkyl group of 3 to 6 carbon atoms, F, Cl, Br, I, —CF 3 , —NO 2 , —NR 4 R 5 , —NHCOR 4 , —OR 4 , —SR 4 , —COOR 4 , —COR 4 and —CH 2 OH, wherein R 4 and R 5 , the same or different, are selected from the group consisting of H, a straight alkyl group of 1 to 6 carbon atoms, a branched alkyl group of 3 to 6 carbon atoms, a cycloalkyl group of 3 to 6 carbon atoms, and tert-butoxycarbonyl, and wherein R 6 is selected from the group consisting of a straight alkyl group of 1 to 6 carbon atoms, a branched alkyl group of 3 to 6 carbon atoms, a cycloalkylalkyl group having 3 to 6 carbon atoms in the cycloalkyl part thereof and 1 to 3 carbon atoms in the alkyl part thereof.