| 摘要 |
NEW MATERIAL:An azetidinone derivative of formula I: (R<1> is protected amino group; R<2> is 3-6C alkyl, 5-6C cycloalkyl or lower alkoxycarbonylmethyl group; R<3> is H or OH-protecting group). EXAMPLE:(3S)-1-(1<1>-n-Butylaminocarbonyl-p-hydroxybenzyl)-3-t-butoxyc arbonylamino-2-azetidinone. USE:An intermediate for the synthesis of nocardin or its derivative. PROCESS:An 3- amino-2-protected amino-propionic acid of formula II is reacted with a hydroxybenzaldehyde of formula III in the presence of an alkali in an inert solvent at 60-80 deg.C, and neutralized with a mineral acid, then reacted with an isonitrile of formula IV to give the objective compound of formula I. Alternatively, the compounds of formulas II, III, and IV are reacted in an organic solvent, e.g. a lower aliphatic alcohol, with stirring. |
