反応 #73087

反応方程式

3-morpholinecarboxylic acid

methylmorpholine-3-carboxylate

2,4-dichloro-5-nitropyrimidine

compound II

(R)-methyl 2-aminobutanoate

Intermediate A

(R)-Methyl 2-((2-chloro-5-nitropyrimidin-4-yl)(cyclopentyl)amino)butanoate

(R)-2-aminobutanoic acid

→

Intermediate I

2-Chloro-5-methyl-6a,7,9,10-tetrahydro-[1,4]oxazino[3,4-h]pteridin-6(5H)-one

反応条件

実験手順

Intermediate I was prepared in the same manner as Intermediate B, using 3-morpholinecarboxylic acid as the starting material instead of (R)-2-aminobutanoic acid. No reductive amination step, such as that used for the conversion of compound II to compound III, was required. Rather, methylmorpholine-3-carboxylate was reacted directly with 2,4-dichloro-5-nitropyrimidine in the same manner as is described for the conversion of compound III to Intermediate A. LCMS: 254.9 m/z (M+H)+.

出典