- Visible-light-induced aerobic oxidative desulfurization of 2-mercaptobenzimidazolesviaa sulfinyl radical
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A mild transition-metal-free non-toxic aerobic photoredox system was found to enable highly efficient desulfurization of 2-mercaptobenzimidazoles. This viable catalytic system includes Rose Bengal in a low catalyst loading as a photosensitizer and cheap, non-toxic NaCl in a catalytic amount as an additive, combined with an oxygen atmosphere. This protocol provides an important alternative access to a broad range of benzimidazole and deuterated benzimidazole products in generally high yields with good tolerance of various synthetically and pharmaceutically useful functionalities. The mechanistic studies reveal that both single electron transfer and energy transfer probably occur in the initial step and a sulfinyl radical intermediate is involved in the key desulfurization process.
- Deng, Guo-Jun,Fu, Mei,Huang, Huawen,Ji, Xiaochen,Li, Yongtong
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supporting information
p. 5594 - 5598
(2020/09/21)
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- SHIP1 MODULATORS AND METHODS RELATED THERETO
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Compounds of formula (I): where R1, R2, R3, R4a, R4b, R5, R6 and R7 are defined herein, or stereoisomers or pharmaceutically acceptable salts thereof, are described herein. Such compounds have activity as SHIP1 modulators, and thus may be used to treat any of a variety of diseases, disorders or conditions that would benefit from SHIP1 modulation. Compositions comprising a compound of formula (I) in combination with a pharmaceutically acceptable carrier or diluent are also disclosed, as are methods of SHIP1 modulation by administration of such compounds to an animal in need thereof.
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Page/Page column 119
(2014/09/29)
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- 5-benzyl-octahydroindole and 6-benzyl-decahydroquinoline NMDA/NR2B antagonists
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Novel 5-benzyl-octahydroindoles and 6-benzyl-decahydroquinolines substituted in the 1-position are effective as NMDA NR2B antagonists useful for relieving pain.
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- 8-aza-bicyclo[3.2.1]octane NMDA/NR2B antagonists
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Novel 3-substituted 8-aza-bicyclo[3.2.1]octanes (commonly known as “tropanes”) substituted in the 8-position are effective as NMDA NR2B antagonists useful for relieving pain.
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- 2-aza-bicyclo[2.2.2]octane NMDA/NR2B antigonists
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Novel 2-aza-bicyclo[2.2.2]octanes substituted in the 2-position are effective as NMDA NR2B antagonists useful for relieving pain.
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- Synthesis and SAR of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity
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A series of 4-(1H-benzimidazole-2-carbonyl)piperidines with dual histamine H1/tachykinin NK1 receptor antagonist activity has been prepared. Factors affecting receptor binding affinities and oral activity in this series are described
- Maynard, George D.,Bratton, Larry D.,Kane, John M.,Burkholder, Timothy P.,Santiago, Braulio,Stewart, Kenneth T.,Kudlacz, Elizabeth M.,Shatzer, Scott A.,Knippenberg, Robert W.,Farrell, Amy M.,Logan, Deborah E.
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p. 2819 - 2824
(2007/10/03)
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