40473-60-7Relevant academic research and scientific papers
A Simple Synthesis of Densely Substituted Benzofurans by Domino Reaction of 2-Hydroxybenzyl Alcohols with 2-Substituted Furans
Abaev, Vladimir T.,Chalikidi, Petrakis N.,Kekhvaeva, Anna E.,Makarov, Anton S.,Trushkov, Igor V.,Uchuskin, Maxim G.
, p. 3747 - 3757 (2019/09/30)
The Br?nsted acid-catalyzed cascade synthesis of densely substituted benzofurans from easily available salicyl alcohols and biomass-derived furans has been developed. The disclosed sequence includes the intermediate formation of 2-(2-hydroxybenzyl)furans
Organocatalytic Phosphonylation of in Situ Formed o-Quinone Methides
Huang, Hai,Kang, Jun Yong
supporting information, p. 5988 - 5991 (2017/11/10)
A new class of Br?nsted acid catalysts based on N-heterocyclic phosphorodiamidic acids (NHPAs) has been developed. The NHPA catalyst promotes phospha-Michael addition reaction of trialkylphosphites to in situ generated ortho-quinone methides (o-QMs) for t
Targeting the gatekeeper residue in phosphoinositide 3-kinases
Alaimo, Peter J.,Knight, Zachary A.,Shokat, Kevan M.
, p. 2825 - 2836 (2007/10/03)
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.
Cadmium-mediated carbonyl benzylation in tap water
Zhou, Cunliu,Wang, Zhiyong
, p. 1649 - 1655 (2007/10/03)
Zn/CdCl2 has been developed as a mediator in the benzylation of various aldehydes in tap water affording the corresponding alcohols in moderate to good yields. The addition of a catalytic amount of InCl3 increases the yield of benzylation product significantly. It can selectively mediate the benzylation of aldehydes in the presence of ketones. A mechanism involving the formation of a cation π-complex is proposed based on the experimental facts. Georg Thieme Verlag Stuttgart.
Silver catalyzed zinc Barbier reaction of benzylic halides in water
Bieber, Lothar W.,Storch, Elisabeth C.,Malvestiti, Ivani,Da Silva, Margarete F.
, p. 9393 - 9396 (2007/10/03)
Benzylic chlorides react in aqueous dibasic potassium phosphate under silver catalysis with aromatic aldehydes in the presence of zinc dust to give 1,2-diaryl alcohols in moderate to good yields. Dimerization to bibenzyls and reduction of the halide are important side reactions. A wide range of substituted aromatic and heteroaromatic aldehydes and of substituted benzylic chlorides can be used. Aliphatic aldehydes and ketones are unreactive. A mechanism of two SET on the metal surface is discussed.
Substituted (ω-aminoalkoxy)stilbene derivatives as a new class of anticonvulsants
Kikumoto,Tobe,Fukami,Ninomiya,Egawa
, p. 645 - 649 (2007/10/02)
A series of substituted (ω-aminoalkoxy)stilbene derivatives has been synthesized and screened for anticonvulsant activity. The effect of structural modification of these molecules on the activities has been systematically examined. Potent anticonvulsant activity was displayed by 2-[4-(4-methyl-1-piperazinyl)butoxy]stilbene and some 2-[4-(3-alkoxy-1-piperidino)butoxy]stilbene derivatives, as determined by maximal electroshock seizure (MES) and pentylenetetrazol-induced convulsion tests in mice. One of these derivatives exhibited more potent anti-MES activity than diphenylhydantoin and carbamazepine in further pharmacological tests in rats, and its therapeutic index was superior to those of two antiepileptic drugs.
