Hagelin G, Laland S G, Undheim K
Department of Chemistry, Nycomed AS, Oslo, Norway.
Acta Chem Scand (Cph). 1992 Dec;46(12):1204-7. doi: 10.3891/acta.chem.scand.46-1204.
The parent methyl ester of the N-1 substituted 5-chloropyrimidinone is hydrolysed by pig liver esterase to the corresponding carboxylic acid. The acid chloride was made with PCl5 in toluene, and coupling with benzyl and methyl esters of selected L-amino acids to the corresponding amides was done in dichloromethane in the presence of triethylamine. The benzyl and methyl ester protecting groups were hydrolysed with pancreas lipase or esterase in a pH-stat to yield the corresponding carboxylic acids.
N-1取代的5-氯嘧啶酮的母体甲酯被猪肝酯酶水解为相应的羧酸。用五氯化磷在甲苯中制备酰氯，并在三乙胺存在下于二氯甲烷中使所选L-氨基酸的苄酯和甲酯与相应的酰胺偶联。苄基和甲酯保护基在pH计中用胰脂肪酶或酯酶水解，得到相应的羧酸。
