| 摘要 |
PURPOSE: A process for preparing alpha-methylated peptidomimetic derivatives using a solution phase reaction is provided, thereby preparing the high purity alpha-methylated peptidomimetic compounds in higher yield. CONSTITUTION: A process for preparing alpha-methylated peptidomimetic derivatives of the formula(1) using a solution phase reaction comprises the steps of: reacting (i) amino acid derivatives or typical acid derivatives having R1 group, (ii) amine derivatives or ammonium chloride compounds having R2 group, (iii) ketone derivatives having R3 group, and (iv) isocyanide compounds having R4 group in solution phase at room temperature; removing excess solvent; treating the reaction products with acid and base to remove excess acidic and basic compounds; separating remaining ketone and isocyanide compounds, wherein R1 is various amino acid derivatives or typical acid derivatives, alkyl or sulfur substituted alkyl, aryl, alkoxy aryl or hydroxy aryl, or hetero aryl; R2 is derived from amine compounds, hydrogen or alkyl, aryl, alkoxy aryl, or heteroaryl; R3 is derived from ketone compounds, hydroxybenzyl, halogen substituted benzyl, or alkoxy substituted benzyl; and R4 is compounds derived from isocyanide, benzyl, methylester, ethylester, or various methyl ester or ethyl ester derived from amino acids.
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