| abstract |
Disclosed herein is a process for production of annO-alkylrapamycin derivative represented by the generalnformula (1) below by reaction between rapamycin and alkylntriflate in an organic solvent, characterized in that thenreaction is carried out in the presence of trialkylamine.n n(where R denotes alkyl, arylalkyl, hydroxyalkyl,nalkoxyalkyl, acyloxyalkyl, aminoalkyl, alkylaminoalkyl,nalkoxycarbonylaminoalkyl, acylaminoalkyl, or aryl.) n This process is capable of producing O-alkylrapamycinnderivative efficiently owing tonimprovement in reaction yields for O-alkylation. |