| 摘要 |
<p>NEW MATERIAL:The compound of formula I [R<1> is (protected) amino or mono- or dialkylamino; R<2> is (protected) carboxy, carbamoyl, (substituted) phenyl, (3-7C cycloalkyl-substituted) alkyl or R<1>] and its salt. EXAMPLE:(2S,3R,4S)-4-benzyloxycarbonylamino-6-methyl-2,3-epoxyheptanol. USE:An important synthetic intermediate for statine or its analog which is a constituent amino acid of pepstatine having excellent pepsin inhibiting activity. PREPARATION:For example, the compound of formula II (R<3> is H or OH- protecting group; R<1>' is protected amino; R<2>' is R<2> except for mono- or dialkylamino) is made to react with an organic peroxide in a solvent to effect cis-epoxidization and optionally the R<3>-protecting group is removed to obtain the corresponding compound of formula I.</p> |
