| 摘要 |
Disclosed is a method of preparing a rapamycin derivative zotarolimus molecule of formula I comprising: (a) reacting a molecule of formula II: with triflic anhydride to produce a molecule of the triflate and (b) reacting the molecule of the triflate with a molecule of formula IV: wherein R1 is selected from the group consisting of =O, and (H, OH); R2 and R5 are independently selected from the group consisting of H, -C(=O)R6, -C(=O)OR6, -C(=O) NHR6 and -C(=S)OR6; R3 is selected from the group consisting of =O and OR5; or R2 and R3 can be taken together to form moiety of formula A -C(R7)(R8) -O-B, where A is a bond to oxygen bonded to carbon 28 and B is a bond bonded to carbon 26 as defined above; R4 is selected from the group consisting of H and alkyl; R6 is selected from the group consisting of alkyl, cycloalkyl, aryl groups, and heterocyclic groups; R7 and R8 are independently selected from the group consisting of H, alkyl, or R7 and R8 taken together are =O R9 and R10 are independently selected from the group consisting of H, alkenyl, alkenylcycloalkenyl, alkenylcycloalkyl, alkyl, alkylcycloalkenyl, alkylcycloalkyl, alkynyl, aralkyl, aryl, cycloalkenyl, cycloalkyl, cycloalkylalkyl, cycloalkylcycloalkyl, cycloalkenylalkyl, heterocyclyl, and combinations thereof, wherein the reactions are performed in a single pot.
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