| 摘要 |
Disclosed is a method for synthesizing an optically active 2-(2-arylmorpholin-4-yl)-1-methyl-1H-[4,4']bipyrimidinyl-6-one represented by the formula (I) wherein R is an aryl or a heteroaryl) and a carbon atom marked with * is an asymmetric carbon atom; which comprises Step (1) or Step (2): Step (1) synthesizing an optically active compound represented by the amine 5: wherein R is an aryl or a heteroaryl, X1 is a halogen, and R1 is an alkyl, an aralkyl or an alkenyl; reacting a compound of the formula 1 with a borane or complex thereof in a solvent in the presence of (S)-2-methyl-CBS-oxazaborolidine to give a alcohol 2, reacting the alcohol of the formula 2 with a base in a solvent to give a epoxide of the formula 3, and reacting the epoxide of the formula 3 with an amine of the formula 4 to give the aminoalcohol of the formula 5. Step (2) synthesizing an optically active amino alcohol represented by the formula 25, wherein R is an aryl or a heteroaryl, X1 is a halogen, and R1 is an alkyl, an aralkyl or an alkenyl, reacting a ketone of the formula 21 with a borane or complex thereof in a solvent in the presence of (R)-2-methyl-CBS-oxazaborolidine to give a alcohol of the formula 22, reacting the alcohol of the formula 22 with a base in a solvent to give a epoxide of the formula 23, and reacting the epoxide of the formula 23 with an amine of the formula 24 to give a amino alcohol of the formula 25.
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