| 摘要 |
PROBLEM TO BE SOLVED: To efficiently obtain the subject amino acid amide that is useful as a synthetic intermediate for pharmaceuticals by reaction of a specific aminonitrile with a ketone. SOLUTION: An α,α-dialkyl-substituted aminonitrile of formula I (R<1> and R<2> are each a lower alkyl, an alkylene), for example, α-amino-α- methylpropionitrile or the like is allowed to react with a ketone of the formula: R<3> -CO-R<4> (R<3> and R<4> are each a lower alkyl or an alkylene), for example, acetone in the presence of a strong base substance, for example, sodium hydroxide or the like to produce an oxazolidine of formula II. The resultant oxazolidine product is hydrolyzed to give the objective amide, for example, α-amino-α- methylpropionamide. In a preferred embodiment, the hydrolysis is carried out by using hydrochloric acid or the like to keep the reaction medium neutral or acidic and the reaction system is held at the reaction temperature of from 0 to about 50 deg.C for about 1-5 hours. |
