125629-39-2

Upstream product

• 125629-28-9 (2-fluorophenyl)(3-methoxy-4-benzyloxyphenyl)methanol 
• 125629-29-0 2-fluorophenyl 3-methoxy-4-benzyloxyphenyl ketone 
• 125629-31-4 2-fluorophenyl 4-hydroxy-3-methoxy-5-nitrophenyl ketone 
• 125629-30-3 2-fluorophenyl 4-hydroxy-3-methoxyphenyl ketone 
• 2426-87-1 3-methoxy-4-(phenylmethoxy)benzaldehyde 
• 1072-85-1 o-fluorobromobenzene 
• 125628-97-9 Ro 41-0960 
• 77-78-1 dimethyl sulfate 

Downstream Products

• 125629-41-6 5-(2-fluorobenzoyl)-2,3-dimethoxybenzonitrile 
• 125629-40-5 3-amino-2'-fluoro-4,5-dimethoxybenzophenone 

Relevant academic research and scientific papers

Synthesis of [18F]Ro41-0960, a potent catechol-O-methyltransferase inhibitor, for PET studies

Ro41-0960 (3,4-dihydroxy-5-nitro-2'-fluorobenzophenone is a potent, fluorine containing COMT inhibitor. In order to map catechol-O-methyltransferase (COMT) in vivo with PET, no-carrier-added [18F]Ro41-0960 was synthesized by the nucleophilic aromatic substitution of [18F]fluoride for 2'-nitro on 3,4-dimethoxy-5,2'-dinitrobenzophenone, followed by hydrolysis with HBr. During the course of this study it was found that [18F]fluoromethane ([18F]CH3F) was generated as the side product of nucleophilic aromatic substitution reaction. Various precursors with different hydroxyl protecting groups were then investigated for the effects on this side reaction.

Catechol derivatives

Catechol derivatives of the formula STR1 wherein Ra, Rb and Rc have the significance given herein, the ester and ether derivatives thereof which are hydrolyzable under physiological conditions and the pharmaceutically acceptable salts thereof are described and possess valuable pharmacological properties. In particular, they inhibit the enzyme catechol-O-methyltransferase (COMT), a soluble, magnesium-dependent enzyme which catalyses the transference of the methyl group of S-adensoylmethionine to a catechol substrate, whereby the corresponding methyl ethers are formed. Suitable substrates which can be O-methylated by COMT and which can thus be deactivated are, for example, extraneuornal catecholamines and exogeneously-administered therapeutically active substances having a catechol structure. Formula Ia above embraces not only compounds which form part of the invention, but also known compounds; the compounds which form part of the invention can be prepared according to known methods.