- An Expeditious One-Pot Synthesis of N-Substituted 6-Nitroindoles from Indolines
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This paper reports an one-pot method for the concomitant alkylation - oxidation (aromatization) of indolines, particularly effective to get easy access to N-alkyl-6-nitroindoles, which are useful platforms in medicinal chemistry. N-alkyl-6-nitroindoles are obtained in good yield (64-91%) by reaction at room temperature in non-degassed DMF of 6-nitroindoline, an alkyl halide, and NaH as base. The presence of NaH appears to be essential for a high yield conversion.
- Laconde, Guillaume,Carato, Pascal,Poupaert, Jacques H.,Berthelot, Pascal,Depreux, Patrick,Henichart, Jean-Pierre
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- COMPOUNDS AND THERAPEUTIC USES THEREOF
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The invention relates to compounds, pharmaceutical compositions and methods useful for treating cancer, systemic or chronic inflammation, rheumatoid arthritis, diabetes, obesity, T-cell mediated autoimmune disease, ischemia, and complications associated w
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Page/Page column 102-103
(2013/02/28)
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- NOVEL FUSED PYRROLE DERIVATIVE
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Disclosed is a compound represented by the formula (1) below which is useful as a glucocorticoid receptor function regulating agent, an anti-inflammatory drug or an antidiabetic drug, or a pharmaceutically acceptable salt thereof. (1) [In the formula, R1 represents an aralkyl group or the like; R2 represents a hydrogen atom or the like; -W4=W5-W6=W7- represents a group expressed as the following formula: -CR4=CR5-CR6=CR7- (wherein R4, R5, R6 and R7 independently represent a group expressed as the following formula: -E-A (wherein E represents a single bond and A represents a hydrogen atom, a nitro group or the like)) or the like; R8 represents a group expressed as the following formula: -OR11 (wherein R11 represents a hydrogen atom or the like) or the like; R9 represents a trifluoromethyl group or the like; and R10 represents a group expressed as the following formula: -[C(R13)R14]n-R15 (wherein R13 and R14 independently represent a hydrogen atom or the like, n represents an integer of 0-10, and R15 represents a group expressed as the following formula: -N(R18)R19 (wherein R18 and R19 represent a monocyclic nitrogen-containing heterocyclic ring or the like together with a nitrogen atom to which they are bonded) or the like).]
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Page/Page column 71-72
(2010/11/26)
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- Substituted indole compounds having NOS inhibitory activity
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The present invention features inhibitors of nitric oxide synthase (NOS), particularly those that selectively inhibit neuronal nitric oxide synthase (nNOS) in preference to other NOS isoforms. The NOS inhibitors of the invention, alone or in combination w
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Page/Page column 83; 84
(2010/11/24)
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- N-ARYLPHENYLACETAMIDE DERIVATIVES AND MEDICINAL COMPOSITIONS CONTAINING THE SAME
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N-Arylphenylacetamide derivatives represented by the following formula [I]: (wherein R1 is C1-6 alkoxy, etc.; R2 is hydrogen, -(CH2)m-N(R6)(R7) (m is an integer of from 1 to 4; R
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- Synthesis and reactions of N-protected 3-nitroindoles
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Treatment of N-protected indoles 3 with acetyl nitrate generated in situ at low temperatures affords the corresponding 3-nitroindoles 2 in good to excellent yields. Deprotection of 1-acetyl-3-nitroindole (2h) with DBU gives 3-nitroindole (1). Reaction of
- Pelkey,Gribble
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p. 1117 - 1122
(2007/10/03)
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