1154060-54-4

Upstream product

• 536-74-3 phenylacetylene 
• 157942-12-6 methyl 3-hydroxy-4-iodobenzoate 
• 98-80-6 phenylboronic acid 
• 619-12-5 4-formyl-3-hydroxybenzoic acid 
• 108-86-1 bromobenzene 

Downstream Products

• 1154060-53-3 2-phenylbenzofuran-6-carboxylic acid 

Relevant academic research and scientific papers

De Novo Synthesis of Benzannelated Heterocycles

Benzannelated heterocycles such as indoles and indazoles are prominent structural motifs found in natural products, pharmaceuticals and agrochemicals. For their synthesis, chemists traditionally either functionalize commercially available heterocycles or resort to transformations that make use of benzene-derived building blocks. Here, we report a powerful cascade reaction that enables the de novo construction of variously substituted indoles, indazoles, benzofurans and benzothiophenes from readily available bicyclo[3.1.0]hexan-2-ones. The transformation can be conducted under mild, non-anhydrous conditions. For the synthesis of indoles, mechanistic studies revealed that the electrocyclic ring-opening of the bicyclic ring-system and aromatization precedes the 3,3-sigmatropic rearrangement.

BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY

A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.

Tandem Sonogashira-Hagihara coupling/cycloisomerization reactions of ethynylboronic acid MIDA ester to afford 2-heterocyclic boronic acid MIDA esters: A concise route to benzofurans, indoles, furopyridines and pyrrolopyridines

A one-pot process that provides direct access to 2-heterocyclic MIDA (N-methyliminodiacetic acid) boronates has been developed. The reaction of 2-iodophenols or 2-iodoanilines with ethynylboronic acid MIDA ester readily afforded 2-substituted heterocyclic compounds. Amidine and phosphazene bases, especially TMG (1,1,3,3-tetramethylguanidine) assumed an important role in the tandem Sonogashira-Hagihara coupling/cycloisomerization reactions.

BIS-(SULFONYLAMINO) DERIVATIVES IN THERAPY 065

The invention provides compounds of formula wherein R1, R2, R3, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1

BIS-(SULFONYLAMINO) DERIVATIVES IN THERAPY 066

The invention provides compounds of formula wherein R1, R3, L1, L2, G1, G2, A and m are as defined in the specification and optical isomers, racemates and tautomers thereof, and pharmaceutically acceptable salts thereof; together with processes for their preparation, pharmaceutical compositions containing them and their use in therapy. The compounds are inhibitors of microsomal prostaglandin E synthase-1.