Rapid preparation of new or known fluorinated sugar derivatives, for use in vivo pharmacokinetic studies, by reacting pentose or hexose with fluoropyruvate using aldolase

摘要

Preparation of organic fluoro compounds (I), for use in vivo pharmacokinetic studies, involves reacting a pentose or hexose with fluoropyruvate using an aldolase. An Independent claim is included for the following 3-deoxy-3-fluoro-nonulopyranosonic or -octopyranosonic acid derivatives as new compounds (specifically where the 3-fluoro atom is in axial configuration and/or is an 18F atom): 3,5-didesoxy-3-fluoro-D-arabino-D-glycero-nonulosonic acid (Ia), 3-desoxy-3-fluoro-D-glycero-D-galacto-nonulosonic acid, 3,5-didesoxy-3-fluoro-D-lyxo-D-glycero-nonulosonic acid, 3-desoxy-3-fluoro-D-galacto-octulosonic acid, 3-desoxy-3-fluoro-D-glycero-L-altro-nonulosonic acid, 3,9-didesoxy-3-fluoro-L-glycero-D-talo-nonulosonic acid, 3-desoxy-3-fluoro-D-manno-octulosonic acid, 3-desoxy-3-fluoro-D-gluco-octulosonic acid, 3-desoxy-3-fluoro-L-gulo-octulosonic acid, 3-desoxy-3-fluoro-L-ido-octulosonic acid, 3,9-didesoxy-3-fluoro-D-glycero-L-manno-nonulosonic acid, 3-desoxy-3-fluoro-D-glycero-L-manno-nonulosonic acid, 3-desoxy-3-fluoro-D-altro-octulosonic acid and 3-desoxy-3-fluoro-D-allo-octulosonic acid.