393-62-4

Upstream product

• 394-32-1 1-(5-fluoro-2-hydroxyphenyl)ethan-1-one 
• 459-60-9 1-fluoro-4-methoxybenzene 
• 496-69-5 2-bromo-4-fluoro-phenol 
• 480439-44-9 1-acetoxy-2-bromo-4-fluorobenzene 
• 75-36-5 acetyl chloride 
• 445-82-9 1-(5-fluoro-2-methoxyphenyl)ethanone 

Downstream Products

• 16167-61-6 1-(4-Acetamino-benzolsulfonylhydrazono)-1-(5-fluor-3-brom-2-hydroxy-phenyl)-ethan 
• 790710-81-5 ethyl 8-bromo-6-fluoro-4-oxo-4H-chromene-2-carboxylate 
• 790710-83-7 1-[5-fluoro-2-hydroxy-3-(4-methylpiperazin-1-yl)phenyl]ethanone 
• 66892-34-0 6-fluoro-4-chromanone 

Relevant academic research and scientific papers

ALLOSTERIC CHROMENONE INHIBITORS OF PHOSPHOINOSITIDE 3-KINASE (PI3K) FOR THE TREATMENT OF DISEASES ASSOCIATED WITH P13K MODULATION

The disclosure relates to compounds of Formula (I) as allosteric chromenone inhibitors of phosphoinositide 3-kinase (PI3K) useful in the treatment of diseases or disorders associated with PI3K modulation, Formula (I), or a prodrug, solvate, enantiomer, st

Redox-Neutral Coupling between Two C(sp3)?H Bonds Enabled by 1,4-Palladium Shift for the Synthesis of Fused Heterocycles

The intramolecular coupling of two C(sp3)?H bonds to forge a C(sp3)?C(sp3) bond is enabled by 1,4-Pd shift from a trisubstituted aryl bromide. Contrary to most C(sp3)?C(sp3) cross-dehydrogenative couplings, this reaction operates under redox-neutral conditions, with the C?Br bond acting as an internal oxidant. Furthermore, it allows the coupling between two moderately acidic primary or secondary C?H bonds, which are adjacent to an oxygen or nitrogen atom on one side, and benzylic or adjacent to a carbonyl group on the other side. A variety of valuable fused heterocycles were obtained from easily accessible ortho-bromophenol and aniline precursors. The second C?H bond cleavage was successfully replaced with carbonyl insertion to generate other types of C(sp3)-C(sp3) bonds.

NOVEL AMINATION PROCESS

Provided herein are novel processes for the preparation of intermediates that may be useful in the preparation of 5-Ht1b receptor antagonist useful in the treatment of depression, anxiety and other related diseases. The present processes may of

NOVEL PROCESS

Provided herein are novel processes for the preparation of intermediates that may be useful in the preparation of 5-Ht1b receptor antagonist useful in the treatment of depression, anxiety and other related diseases. The present processes may offer improve

Successful development and scale-up of a palladium-catalysed amination process in the manufacture of ZM549865

Key steps in the synthesis of ZM549865 (a 5-HT receptor antagonist) are the palladium-catalysed amination of ethyl 8-bromo-6-fluoro-4-oxo-4H-2- chromenecarboxylate and subsequent hydrolysis of the ester group. The development of a simple, robust process c