125629-01-8

Upstream product

• 67-56-1 methanol 
• 84211-30-3 3,4-dihydroxy-5-nitrobenzoic acid 
• 3943-74-6 4-hydroxy-3-methoxybenzoic acid methyl ester 
• 116313-85-0 3,4-dihydroxy-5-nitrobenzaldehyde 
• 15785-54-3 5-nitrovanillic acid 
• 42590-00-1 4-hydroxy-3-methoxy-5-nitrobenzoic acid methyl ester 

Downstream Products

• 438547-21-8 3-Benzyloxy-4-hydroxy-5-nitro-benzoic acid methyl ester 
• 1391712-04-1 C₂₂H₁₉NO₆ 
• 163495-26-9 3-Benzyloxy-4-iodo-5-nitroso-benzoic acid methyl ester 
• 163495-25-8 3-Benzyloxy-4-iodo-5-nitro-benzoic acid methyl ester 
• 438547-22-9 3-Benzyloxy-5-nitro-4-trifluoromethanesulfonyloxy-benzoic acid methyl ester 
• 163495-28-1 3-Benzyloxy-5-(6-hydroxymethyl-6-methoxymethoxy-3,6-dihydro-[1,2]oxazin-2-yl)-4-iodo-benzoic acid methyl ester 
• 163495-29-2 3-(6-Acetoxymethyl-6-methoxymethoxy-3,6-dihydro-[1,2]oxazin-2-yl)-5-benzyloxy-4-iodo-benzoic acid methyl ester 
• 180031-12-3 4-chloro-3-hydroxy-5-nitrobenzoic acid methyl ester 
• 955886-81-4 methyl 3-amino-4,5-dihydroxybenzoate hydrochloride 
• 148546-84-3 methyl 3,4-dimethoxy-5-nitrobenzoate 
• 148546-85-4 methyl 3-amino-4,5-dimethoxybenzoate 

Relevant academic research and scientific papers

Synthesis of proposed structure of aaptoline a, a marine sponge-derived 7,8-dihydroxyquinoline, and its neuroprotective properties in c. Elegans

A concise and efficient synthesis of the proposed structure of aaptoline A, a 7,8-dihy-droxyquinoline derived from a marine sponge, was accomplished in seven steps with a 52% overall yield. A key feature of the synthesis is the high-yielding Ag(I)-catalyz

DUOCARMYCIN ANALOGUES

The invention relates to 2-methylbenzoxazole compounds of formula I which are analogues of the DNA alkylating subunit of the duocarmycins. Compounds of formula I can be used in the synthesis of DNA alkylating agents and antibody-drug conjugates and relate

Discovery of a long-acting, peripherally selective inhibitor of catechol- O -methyltransferase

Novel nitrocatechol-substituted heterocycles were designed and evaluated for their ability to inhibit catechol-O-methyltransferase (COMT). Replacement of the pyrazole core of the initial hit 4 with a 1,2,4-oxadiazole ring resulted in a series of compounds endowed with longer duration of COMT inhibition. Incorporation of a pyridine N-oxide residue at position 3 of the 1,2,4-oxadiazole ring led to analogue 37f, which was found to possess activity comparable to entacapone and lower toxicity in comparison to tolcapone. Lead structure 37f was systematically modified in order to improve selectivity and duration of COMT inhibition as well as to minimize toxicity. Oxadiazole 37d (2,5-dichloro-3-(5-(3,4-dihydroxy-5-nitrophenyl)-1,2,4-oxadiazol-3-yl)-4, 6-dimethylpyridine 1-oxide (BIA 9-1067)) was identified as a long-acting, purely peripheral inhibitor, which is currently under clinical evaluation as an adjunct to l-Dopa therapy of Parkinson's disease.

Oxadiazole derivatives as COMT inhibitors

This invention relates to novel substituted [1,2,4]-oxadiazoles, their use in the treatment of some central and peripheral nervous system disorders, methods for their preparation and pharmaceutical compositions containing them.

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.