Novel preparation of (R,R)bromo-3-quinuclidinylbenzilate (Br-QNB), a precursor for the synthesis of (R,R)[125I]iodo-QNB
Radioiodinated QNB (3-quinuclidinylbenzilate)(IV) is a potential SPET-ligand with high affinity muscarinic receptor binding. The synthesis of the precursor BrQNB(III)((R)-(-)-azabicyclo[2.2.2]oct-3-yl-(R)-(+)-α-hydroxy-α-(4- bromophenyl)-α-phenylacetate)
Kaempfer, Ingrid,Heinicke, Jochen,Sorger, Dietlind,Schulze, Klaus,Schliebs, Reinhard,Knapp, Wolfram H.
p. 1047 - 1052
(2007/10/03)
Boronic acid adducts of rhenium dioxime and technetium-99m dioxime complexes containing a biochemically active group
Boronic acid adducts of technetium-99m and radioactive rhenium dioxime complexes, each of which include biochemically active groups, are useful as diagnostic and therapeutic agents, respectively.
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(2008/06/13)
Synthesis of the Four Stereoisomers of 1-Azabicyclooct-3-yl-α-hydroxy-α-(4-phenylboronic acid)-α-phenylacetae (QNB-Boronic acid), including a preparative HPLC method to separate diastereoisomeric mixtures with high optical purity
The four stereoisomers of 1-azabicyclooct-3-yl-α-hydroxy-α-(4-phenylboronic acid)-α-phenylacetate (QNB boronic acids, 1a-1d) were synthesized initially via 1-azabicyclooct-3-yl-α-hydroxy-α-(4-iodophenyl)-α-phenylacetate (iodo-QNBs, 6a-6d) using an adaptation of a published procedure.The number of steps involved were reducted substantially using a distinctly different approach.This involved the synthesis of diastereoisomers of QNB-boronic acid, followed by separation and isolation of enantiomers by preparative reversed-phase HPLC.An improved method of synthesis of α-hydroxy-α-(4-aminophenyl)-α-phenyl-acetic acid (3a and 3b) from α-hydroxy-α-(4-nitrophenyl)-α-phenylacetic acid (2a and 2b) is also described.
Nanjappan, P.,Ramalingam, K.,Nowotnik, D. P.
p. 1271 - 1282
(2007/10/02)
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