193687-89-7

Upstream product

• 3780-33-4 2,3-dihydro-2,2-dimethylbenzo[b]pyran-4-one 
• 89-95-2 2-methyl-benzyl alcohol 
• 926-62-5 isobutylmagnesium bromide 

Downstream Products

• 19019-21-7 1-(2-hydroxyphenyl)-3-methylbutan-1-one 

Relevant academic research and scientific papers

Targeting the gatekeeper residue in phosphoinositide 3-kinases

A single residue in the ATP binding pocket of protein kinases-termed the gatekeeper-has been shown to control sensitivity to a wide range of small molecule inhibitors (Chem. Biol. 2004, 11, 691; Chem. Biol. 1999, 6, 671). Kinases that possess a small side chain at this position (Thr, Ala, or Gly) are readily targeted by structurally diverse classes of inhibitors, whereas kinases that possess a larger residue at this position are broadly resistant. Recently, lipid kinases of the phosphoinositide 3-kinase (PI3-K) family have become the focus of intense research interest as potential drug targets (Chem. Biol. 2003, 10, 207; Curr. Opin. Pharmacol. 2003, 3, 426). In this study, we identify the residue that corresponds structurally to the gatekeeper in PI3-Ks, and explore its importance in controlling enzyme activity and small molecule sensitivity. Isoleucine 848 of p110α was mutated to alanine and glycine, but the mutated kinase was found to have severely impaired enzymatic activity. A structural bioinformatic comparison of this kinase with its yeast orthologs identified second site mutations that rescued the enzymatic activity of the I848A kinase. To probe the dimensions of the gatekeeper pocket, a focused panel of analogs of the PI3-K inhibitor LY294002 was synthesized and its activity against gatekeeper mutated and wild-type p110α was assessed.

Synthesis of 2,3-disubstituted benzofurans from ortho-acylphenols

2,3-Disubstituted benzofuran derivatives were synthesized from ortho-acylphenols in two steps. The β-aryloxyacrylates prepared from the ortho-acylphenols were treated with n-Bu3SnH/ AIBN and then with 5% HCl-EtOH to afford 2,3-disubstituted benzofurans. Georg Thieme Verlag Stuttgart.

Chromenes and chromanones. Part IV.1 The Birch reduction of 2,2-dimethyl-4-chromanone and its 7-substituted analogues

2,2-Dimethyl-4-chromanone (1a), 2,2,7-trimethyl-4-chromanone (1b) and 7-methoxy-2,2-dimethyl-4-chromanone (1c) have been reduced by sodium or lithium in liquid ammonia with the presence or without of proton donor. The bicyclic or phenolic products were obtained. Products with reduced benzene ring only were also observed. The possible mechanisms of reductions are considered.