Hydrochloric Acid → Hydrochloric Acid

Participants

Reaction Steps

In addition, it is preferred that a compound of Formula (3-4), in which R41 is a 2,6-dichlorophenyl group and R42 is an isopropyl group, is reacted with a compound of Formula (2-4) in which R43′ is an N-formyl-N-methyl-aminomethyl group and R45 is an ethyl group to thus form Nα-(2,6-dichlorobenzoyl)-4-{2-ethoxycarbonyl-amino-5-(N-formyl-N-methylaminomethyl)benzoylamino}-L-phenylalanine isopropyl ester of Formula (4-4) in which R41 is a 2,6-dichlorophenyl group, R42 is an isopropyl group, R43′ is an N-formyl-N-methyl-aminomethyl group and R45 is an ethyl group; then the isopropyl ester of Formula (4-4) is reacted with potassium carbonate to thus convert the ester into Nα-(2,6-dichlorobenzoyl)-4-{6-(N-formyl-N-methyl-aminomethyl)quinazoline-2,4[1H,3H]-dion-3-yl}-L-phenylalanine isopropyl ester of Formula (5-4) in which R41 is a 2,6-dichlorophenyl group, R42 is an isopropyl group and R43′ is an N-formyl-N-methyl-aminomethyl group; subsequently the isopropyl ester is subjected to N-alkylation using methyl p-toluene-sulfonate to thus convert the ester into Nα-(2,6-dichlorobenzoyl)-4-{1-methyl-6-(N-formyl-N-methyl-aminomethyl)-quinazoline-2,4[1H,3H]-dion-3-yl}-L-phenylalanine isopropyl ester; and finally the formyl group of the resulting isopropyl ester is deprotected with hydrogen chloride to give Nα-(2,6-dichlorobenzoyl)-4-{1-methyl-6-(N-methyl-aminomethyl)-quinazoline-2,4[1H,3H]-dion-3-yl}-L-phenylalanine isopropyl ester or hydrochloride thereof, in which R41 is a 2,6-dichlorophenyl group, R42 is an isopropyl group, R43 is an N-methyl-aminomethyl group and R44 is a methyl group.

Provenance & Evidence