| 摘要 |
<p>A method of preparation of oxabispidine compounds that bear an N-2- (alkoxycarbonylamino) ethyl substituent is described. In particular, a process for the preparation of a compound of formula I is disclosed wherein R1 represents H, an amino protective group or a structural fragment of formula Ia. The process comprises reaction of a compound of formula II with either a compound of formula III or acrylaminde, followed by reaction of the resulting intermediate of formula IV with an alcohol of formla R2-OH and an agent that promotes, or agents that in combination promote, rearrangement and oxidation of the compound of formula IV to an intermediate isocyanate, which may then react with the alcohol of formula R2-OH.</p> |
