A method for removing excess amine substrate in S-35 labeled radioligand preparations using fluorous scavengers has been developed in an effort to simplify purification. The fluorous scavenging methodology has been shown effective at removing a variety of amines from sulfonylation reaction mixtures. In many cases, this results in lessened semi-preparative HPLC purification and thus in higher radiochemical yield and time saving. This methodology was compared to the use of a solid phase resin (PS-Isocyanate) and determined to be approximately equal in the recovery of radioactivity. However, the reaction with the solid phase resin required 24 hours with 10 equivalents of resin while the reaction of fluorous scavenger required only 3 equivalents of electrophile and was complete in 1 hour.
展开▼
