81381-93-3

Usage

InChI:InChI=1/C21H22INO3/c22-18-8-6-17(7-9-18)21(25,16-4-2-1-3-5-16)20(24)26-19-14-23-12-10-15(19)11-13-23/h1-9,15,19,25H,10-14H2

Upstream product

• 81381-92-2 (RS)-1-azabicyclo<2.2.2>oct-3-yl (RS)-α-hydroxy-α-<4-<2-(3-methylpiperidin-1-yl)-1,2-diazaethylen-1-yl>phenyl>-α-phenylacetate 
• 1144-74-7 4-nitrobenzophenone 
• 31029-96-6 1-(4-aminophenyl)-2-phenylethane-1,2-dione 
• 1603-79-8 phenylglyoxylic acid ethyl ester 
• 81039-90-9 (RS)-1-azabicyclo<2.2.2>oct-3-yl (RS)-α-hydroxy-α-(4-aminophenyl)-α-phenylacetate 
• 81381-90-0 α-hydroxy-α-(4-aminophenyl)-α-phenylacetic acid 
• 88000-52-6 4-[(1-Aza-bicyclo[2.2.2]oct-3-yloxycarbonyl)-hydroxy-phenyl-methyl]-benzenediazonium; chloride 
• 81039-87-4 ethyl α-hydroxy-α-(4-nitrophenyl)-α-phenylacetate 
• 88000-53-7 α-hydroxy-4-nitro-α-phenylbenzeneacetonitrile 
• 81039-78-3 ethyl α-hydroxy-α-(4-aminophenyl)-α-phenylacetate 
• 88000-54-8 (R,S)-α-hydroxy-α-(4-nitrophenyl)-α-phenylacetic acid 
• 6581-06-2 quinuclidinyl benzilate 

Relevant academic research and scientific papers

A direct iodination method with iodine and silver triflate for the synthesis of SPECT and PET imaging agent precursors

A direct iodination method with iodine and silver triflate for the synthesis of SPECT and PET imaging agent precursors has been developed.

Synthesis and evaluation of radioiodinated derivatives of 1-azabicyclo[2.2.2]oct-3-yl α-hydroxy-α-(4-iodophenyl)-α-phenylacetate as potential radiopharmaceuticals

Two derivatives of (RS)-1-azabicyclo[2.2.2]oct-3-yl (RS)-α-hydroxy-α-(4-iodophenyl)-α-phenylacetate and three partially resolved (R)- or (S)-1-azabicyclo[2.2.2]oct-3-yl (RS)-α-hydroxy-α-(4-iodophenyl)-α-phenylacetates labeled with no carrier added iodine-125 and iodine-123 were synthesized by the Wallach triazene approach. We have found that this approach is necessary to obtain no carrier added labeling and gives far better results than the direct electrophilic iodination. The obtained yields were 7 to 18% when using iodine-123 (yield dependent on the source of iodide) and up to 17% for iodine-123 (yield dependent on the source of iodide) and up to to 17% for iodine-125 labeled compounds. Our preliminary distribution studies indicate that one derivative localizes in the organs known to have a large concentration of muscarinic receptors and that this localization is due to binding to those receptors.

Analogues of 3-Quinuclidinyl Benzilate

A number of analogues of 3-quinuclidinyl benzilate (QNB) have been synthesized and their affinities to muscarinic receptor from rat or dog ventricular muscle measured.We have determined that the muscarinic receptor can to a different degree accomodate either a halogen in the ortho, meta, or para position of one phenyl ring or the repalcement of one phenyl ring with an alkyl group.Our in vitro competition studies show that the affinities lie within a 270-fold range, from the highest affinity compound, 3-quinuclidinyl α-hydroxy-α-cyclopentylphenylacetate (2), to the lowest affinity compound, 3-quinuclidinyl α-hydroxy-α-2-propargylphenylacetate (11).