New tetrahydro-pyran compounds useful to prepare 2-desoxy-2-(F-18)fluoroglucosyl-1-azide, which is useful for F-18-glycosylation of bioactive alkynyl or ethinyl derivatized molecule to form conjugated tetrahydro-pyran biomolecule

摘要

Tetrahydro-pyran compounds (I) are new. Tetrahydro-pyran compounds of formula (I) are new. 3 of R 1-R 4= a leaving group comprising OAc and the other is OSO 2R', and R'= methyl, trifluoromethyl or nitrophenyl. Independent claims are included for: (1) the preparation of (I); (2) the preparation of 2-desoxy-2-[ 18>F]fluoroglucosyl-1-azide (V) comprising reacting (I) with acetic acid 4-acetoxy-2-acetoxymethyl-6-azido-5-[ 18>F]-tetrahydro-pyran-3-yl ester (IV) and removing the acetyl group in a base; and (3) use of (V) for 18>F-glycosylation of a bioactive alkynyl or ethinyl derivatized molecule to obtain a conjugated 2-hydroxymethyl-6-[1,2,3]triazol-1-yl-tetrahydro-pyran-3,4-diol biomolecule of formula (VI). R1a : biomolecule. [Image] [Image].