18761-31-4Relevant academic research and scientific papers
VEGFR INHIBITORS CONTAINING A ZINC BINDING MOIETY
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Page/Page column 25, (2009/04/24)
The present invention relates to VEGFR inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The said derivatives may further act as HDAC inhibitors.
SUBSTITUTED TRIAZOLE DERIVATIVES AS OXYTOCIN ANTAGONISTS
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Page/Page column 96-97, (2010/02/13)
The present invention relates to a class of substituted triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.).
An isomerization-ring-closing metathesis strategy for the synthesis of substituted benzofurans
Van Otterlo, Willem A.L.,Morgans, Garreth L.,Madeley, Lee G.,Kuzvidza, Samuel,Moleele, Simon S.,Thornton, Natalie,De Koning, Charles B.
, p. 7746 - 7755 (2007/10/03)
Twelve substituted benzofurans were synthesized from their corresponding substituted 1-allyl-2-allyloxybenzenes using ruthenium-mediated C- and O-allyl isomerization followed by ring-closing metathesis.
Vanilloid receptor ligands and their use in treatments
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, (2008/06/13)
Compounds having the general structure and compositions containing them, for the treatment of acute, inflammatory and neuropathic pain, dental pain, general headache, migraine, cluster headache, mixed-vascular and non-vascular syndromes, tension headache, general inflammation, arthritis, rheumatic diseases, osteoarthritis, inflammatory bowel disorders, inflammatory eye disorders, inflammatory or unstable bladder disorders, psoriasis, skin complaints with inflammatory components, chronic inflammatory conditions, inflammatory pain and associated hyperalgesia and allodynia, neuropathic pain and associated hyperalgesia and allodynia, diabetic neuropathy pain, causalgia, sympathetically maintained pain, deafferentation syndromes, asthma, epithelial tissue damage or dysfunction, herpes simplex, disturbances of visceral motility at respiratory, genitourinary, gastrointestinal or vascular regions, wounds, burns, allergic skin reactions, pruritis, vitiligo, general gastrointestinal disorders, gastric ulceration, duodenal ulcers, diarrhea, gastric lesions induced by necrotising agents, hair growth, vasomotor or allergic rhinitis, bronchial disorders or bladder disorders.
Synthesis of fused furans by gas-phase pyrolysis of 2-allyloxyaryl-propenoic esters
Black, Michael,Cadogan,McNab, Hamish,MacPherson, Andrew D.,Roddam, V. Peter,Smith, Carol,Swenson, Helen R.
, p. 2483 - 2493 (2007/10/03)
Flash vacuum pyrolysis of 2-allyloxypropenoic esters (e.g. 7) gives benzo[b]furans (e.g. 32) in synthetically useful yields by sequential generation of a phenoxyl radical, cyclisation and ejection of the carboxylic ester function as a free radical leaving group. The method is compatible with a range of substituents on either the benzene ring or the propenoate chain, and is particularly effective for 2-substituted benzo[b]furans. The natural products 5-methoxybenzo[b]furan 1 and angelicin 2 have been synthesised in three and four steps respectively from commercially available starting materials by this route. Related cyclisations to give naphtho[2,1-b]furan 40 were complicated by competitive formation of naphtho[2,1-b]pyran-3-ones (e.g. 41 and 42), but the yield of the required product could be optimised by the choice of the radical precursor. Annelation of a furan ring onto a thlophene is also possible by this method, but lower yields are obtained in such pyrolyses.
SELECTIVE PREPARATION AND CYCLIZATION OF 2-(2-HYDROXYPHENYL)-2-(ISOPROPYLTHIO)ETHANOLS. NEW SYNTHESIS OF 1-BENZOFURANS
Ota, Tomomi,Hasegawa, Shun,Inoue, Seiichi,Sato, Kikumasa
, p. 3029 - 3036 (2007/10/02)
Reaction of phenols with 2-(isopropylthio)ethyl acetate activated by sulphuryl chloride afforded 2-phenols regioselectively, via sigmatropic rearrangement of phenoxysulphonium ylides.The ortho-alkylated phenols thus obtained have been cyclized with conc. hydrochloric acid in 2-methoxyethanol to 1-benzofurans. 2-Methyl- and 2-phenyl-1-benzofurans have been prepared similarly.
BENZOFURAN DERIVATIVES. I. ON THE EFFECTS OF SUBSTITUENTS IN BENZOFURAN SYNTHESES.
Suzuki,Horaguchi,Shimizu,Abe
, p. 2762 - 2767 (2007/10/02)
The Roessing's reaction of 4-substituted 2-acylphenoxyacetic acids give a mixture of benzofurans and 2-benzofurancarboxylic acids. The relative yields of benzofurans and 2-benzofurancarboxylic acids depend on the substituents on the benzene ring of the 2-acylphenoxyacetic acids. Electron-withdrawing substituents such as nitro groups favor the formation of 2-benzofurancarboxylic acids. On the other hand, the formation of benzofurans is favored by the steric hindrance of 2-acyl groups in the reaction of 2-acyl-4-nitrophenoxyacetic acids with anhydrous sodium acetate and acetic anhydride.
