280571-34-8

Upstream product

• 1192-62-7 1-(2-furyl)-1-ethanone 
• 352-11-4 1-chloromethyl-4-fluorobenzene 
• 280571-32-6 5-(4-fluorobenzyl)-furan-2-carboxylic acid 

Downstream Products

• 311983-91-2 1-[5-(4-fluorobenzyl)furan-2-yl]-3-hydroxy-3-[1-(tetrahydropyran-2-yl)-1,2,4-triazole-3-yl]propenone 

Relevant academic research and scientific papers

One-step synthesis of 5-(4-fluorobenzyl)-2-furyl methyl ketone: A key intermediate of HIV-integrase inhibitor S-1360

Practical one-step synthesis of 5-(4-fluorobenzyl)-2-furyl methyl ketone was accomplished by Friedel-Crafts benzylation of 2-furyl methyl ketone with 4-fluorobenzyl chloride hi the presence of ZnCl2. Two reaction conditions and their work-up pr

Development of HIV-integrase inhibitor S-1360: Selection of the protecting group on the 1,2,4-triazole ring

HIV-integrase inhibitor S-1360 was synthesized by Claisen-type reaction of 5-(4-fluorobenzyl)-2-furyl methyl ketone with N-protected 1H-1,2,4-triazole-3- carboxylate. The protecting group on the triazole ring is essential for the reaction to proceed. Tetr

Palladium-catalyzed benzylation of heterocyclic aromatic compounds

Broadly applicable palladium-catalyzed heteroarene benzylation reactions are described with a focus on the most challenging heterocyclic classes under traditional benzylation techniques such as sulfur-containing heterocycles and those bearing functional groups that would be incompatible with reactions requiring Lewis acids and/or strong bases.

Medicinal compositions containing propenone derivatives

A combination of an integrate inhibitor with an anti-retrovirus active substance and medical compositions containing the same as the active ingredients are found.

Aromatic heterocycle compounds having HIV integrase inhibiting activities

A compound of the formula (I): wherein X is hydroxy, protected hydroxy or optionally substituted amino; Y is —COORAwherein RAis hydrogen or ester residue, —CONRBRCwherein RBand RCeach is independently hydrogen or amide residue, optionally substituted aryl or optionally substituted heteroaryl; and A1is optionally substituted heteroaryl; provided that a compound wherein Y and/or A1is optionally substituted indol-3-yl is excluded, a tautomer, a prodrug, a pharmaceutically acceptable salt or a hydrate thereof has an inhibitory activity against an integrase.

INHIBITOR FOR ENZYME HAVING TWO DIVALENT METAL IONS AS ACTIVE CENTERS

A pharmaceutical composition for use as an inhibitor of an enzyme having two divalent metal ions as an active center was found. It is possible to inhibit the activity of an enzyme by a compound capable of chelating both of the two divalent metal ions.

NOVEL PROCESSES FOR THE PREPARATION OF SUBSTITUTED PROPENONE DERIVATIVES

The present invention provides industrial and commercial processes for the preparation of 2-acyl-5-benzylfuran derivatives, 1,2,4-triazole-3-carboxylic acid ester derivatives and propenone derivatives having anti-HIV activities and usuful crystals thereof. wherein R1, R2 and R4 each is independently hydrogen or the like; A is CR6 or N; R6 is hydrogen or the like; Q is a protecting group; and L is a leaving group.