5043-29-8

Upstream product

• 1608-42-0 benzenedizolium-2-carboxylate 
• 42933-07-3 methyl 3-bromo-2-oxo-2H-pyran-5-carboxylate 
• 118-92-3 anthranilic acid 
• 67-56-1 methanol 
• 1013-80-5 4-bromo-2-naphthoic acid 
• 5959-52-4 2-Amino-3-naphthoic acid 
• 5043-27-6 3-amino-4-bromo-2-naphthoic acid 
• 110-71-4 1,2-dimethoxyethane 
• 110-46-3 isopentyl nitrite 

Relevant academic research and scientific papers

CARBOXY SUBSTITUTED (HETERO) AROMATIC RING DERIVATIVES AND PREPARATION METHOD AND USES THEREOF

Carboxy-substituted (hetero)aryl derivatives, pharmaceutical compositions comprising these compounds, and methods of preparing such compounds and compositions are provided. The compounds or compositions are useful in inhibiting xanthine oxidase and urate anion transporter 1, and also can be used in the treatment or prevention of diseases associated with high blood uric acid level in mammals, especially humans.

HETEROCYCLIC COMPOUNDS AS ANTIBIOTIC POTENTIATORS

The invention relates to heterocyclic compounds and their use as antibiotics and/or as antibiotic potentiators. The compounds may act as colistin potentiators and SOS inhibitors.

THIAZOLE DERIVATIVES AS SGLT2 INHIBITORS AND PHARMACEUTICAL COMPOSITION COMPRISING SAME

The present invention relates to a novel compound with thiazole ring having an inhibitory activity against sodium-dependent glucose cotransporter 2 (SGLT2) being present in the intestine and kidney, and a pharmaceutical composition comprising the same as an active ingredient, which is useful for preventing or treating metabolic disorders, particularly diabetes.

A PROCESS FOR THE PREPARATION OF 3-CYANO-1-NAPHTHOIC ACID AND SOME ANALOGUES THEREOF

The present invention is related to a process for the preparation of 3-cyano-1-naphthoic acid and some analogues thereof of formula (1), the intermediate 1-halo-3-cyano naphthalene and some analogues thereof used in this process and a process for the preparation of said intermediate.

A new route for manufacture of 3-cyano-1-naphthalenecarboxylic acid

3-Cyano-1-naphthalenecarboxylic acid is an intermediate required for manufacture of tachykinin receptor antagonists. The 1,3-disubstitution pattern on the naphthalene skeleton complicates the synthesis of this cyano acid. Previous literature-based chemistry is unattractive for large-scale manufacture due to stoichiometric use of mercury salts, low yield, and other operational difficulties. An attractive new route has been developed by establishing the 1,3-substitution on the carbon atoms destined for only one-half of the naphthalene 2-ring system, via 3-bromocoumalate, and then building up the rest of the naphthalene ring system by Diels-Alder addition of 3-bromocoumalate to in situ-generated benzyne. The resulting 4-bromo-2-naphthoate was converted to the required cyanoacid by transformation of ester to nitrile followed by carbonylation of the bromo substituent. The new route has been scaled up successfully and offers significant advantages over previous literature chemistry in terms of improved process environmental implications, improved yield, lower cost, and improved robustness and ease of operation at larger scales of operation.

[4+2] Cycloadditions between 2-pyrones and benzyne. Application to the synthesis of binaphthyls

Cycloaddition of benzyne to 2-pyrones affords the corresponding naphthalene derivatives, the intermediate bicyclic adduct not being detected. Benzopyrones do not react with benzyne under similar conditions probably because this would require the fused aromatic ring to lose aromaticity in the Diels-Alder transition state, which is therefore destabilized. 4-Bromo-2-naphthoic acid methyl ester (obtained by cycloaddition of benzyne to 3-bromo-5-carboxymethylpyran-2-one) can be transformed into 3,3'-dicarboxymethyl-1,1'-binaphthyl by Ni-mediated dimerization.