| 摘要 |
<p>PURPOSE: To obtain the subject compounds useful as synthetic intermediates for medicines, agrichemicals, etc., or as optical resolving agents under mild conditions by a new one step method comprising directly reacting anα-amino acid derivative with an excessive amount of a Grignard reagent. CONSTITUTION: One mole of anα-amino acid derivative of formula I (R<1> is alkyl, amino-protecting group; R<2> is 1-8C alkyl, aryl, etc.; C* is asymmetric carbon atom) is reacted with five or more moles of a Grignard reagent of formula: R<3> MgX (R<3> is 6-20C hydrocarbon; X is halogen) usually in a solution below the refluxing temperature of the solution, preferably at 15-50 deg.C, to obtain the objective compound of formula II. The reaction solvent is preferably THF. When e.g. N-benzyloxycarbonyl-L-serine and phenylmagnesium bromide are used as the starting raw material of formula I and as the Grignard reagent, respectively, (2S)-2-benzyloxycarbonylamino-3-hydroxy-1-phenylpropane is obtained as the compound of formula II.</p> |
