| 摘要 |
<p>PURPOSE:To produce the titled compound having antitumor activity, etc., and modifiable easily by the introduction of functional group, economically in short step, by reacting a specific olefin compound with aziridine, and treating the resultant pyrrolidine derivative in the presence of a base. CONSTITUTION:The objective compound of formula IV can be produced by reacting the olefin compound of formula I (X is halogen, -OTs or -OMs; R1-R4 is electron attracting functional group, H, OH, OH-protecting group, derivative of OH, ketone group or ketone-protecting group) e.g. ethyl-6-chloro-2-hexenoate) with aziridine of formula II, and reacting the resultant pyrrolidine derivative of formula III [e.g. ethyl-N-(beta-chloroethyl)-2-pyrrolidine acetate, etc.] with a base such as lithium diisopropylamide in a solvent such as THF.</p> |
