13196-10-6Relevant articles and documents
Synthetic models related to methoxalen and menthofuran-cytochrome P450 (CYP) 2A6 interactions. Benzofuran and coumarin derivatives as potent and selective inhibitors of CYP2A6
Yamaguchi, Yuki,Akimoto, Ichie,Motegi, Kyoko,Yoshimura, Teruki,Wada, Keiji,Nishizono, Naozumi,Oda, Kazuaki
, p. 997 - 1001 (2013)
Human microsomal cytochrome P450 (CYP) 2A6 contributes extensively to nicotine detoxication but also activates tobacco-specific procarcinogens to mutagenic products. We prepared a series of benzofuran and coumarin derivatives that have inhibitory effects on the activity of human CYP2A6. The reported compounds methoxalen and menthofuran had potent inhibitory effects on the activity of CYP2A6 with IC50 values of 0.47 μM and 1.27 μM, respectively. Synthetic benzofuran (4-methoxybenzofuran: IC50=2.20 μM) and coumarin (5-methoxycoumarin: IC50=0.13 μM and 6-methoxycoumarin: IC50=0.64 μM) derivatives, which have more selective effects than those of methoxalen and menthofuran, exhibited comparable activities against CYP2A6. These compounds can be used as a lead compounds in the design of CYP2A6 inhibitor drugs to reduce smoking and tobacco-related cancers.
Facile entry to 4- and 5-hydroxybenzofuran and to their amino derivatives
Bonini, Carlo,Cristiani, Graziella,Funicello, Maria,Viggiani, Licia
, p. 1983 - 1990 (2006)
An innovative one-step procedure for the synthesis of 4-hydroxybenzofuran and an improved synthesis of 5-hydroxybenzofuran is reported. Such compounds were also transformed into their amino derivatives via Smiles rearrangement with good to high overall yields. Copyright Taylor & Francis Group, LLC.
2-Nitrofurans as dienophiles in Diels-Alder reactions
Rosa, Claudia Della,Kneeteman, María N.,Mancini, Pedro M.E.
, p. 8711 - 8714 (2005)
α-Nitrofuran derivatives are studied in Diels-Alder reactions under thermal conditions. In contrast to α-acylfurans, they proved to be efficient dienophiles.
TRICYCLIC SUBSTITUTED PIPERIDINE DIONE COMPOUND
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Paragraph 0101-0102, (2021/07/17)
Disclosed is a series of tricyclic substituted piperidine dione compounds, and applications thereof in the preparation of medicines for treating diseases related to CRBN protein; specifically disclosed are the derivative compound represented by formula (I) or a pharmaceutically acceptable salt thereof.
Method suitable for large-scale production of B-RAF kinase dimer inhibitor
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Paragraph 0067-0068, (2020/08/18)
The invention relates to a method for large-scale production of a B-RAF kinase dimer inhibitor 1-((1S, 1aS, 6bS)-5-((7-oxo-5, 6, 7, 8-tetrahydro-1, 8-diazanaphthalene-4-yl) oxy)-1a, 6b-dihydro-1H-cyclopropyl [b] benzofuran-1-yl)-3-(2, 4, 5- trifluorophenyl) urea (hereinafter sometimes referred to as a compound 1). The method enables impurities or by-products to be controlled to 0.05% or less without the use of expensive column chromatography operations. Thus, the method greatly reduces cost and is suitable for large-scale production.