- METHYL-1H-PYRAZOLE ALKYLAMINE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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The present invention relates to compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor and more particularly to methyl-1H-pyrazole alkylamine compounds having this pharmacological activity, to process
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Page/Page column 122; 123
(2016/07/05)
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- 1-METHYLPYRAZOLE-PIPERAZINE COMPOUNDS HAVING MULTIMODAL ACTIVITY AGAINST PAIN
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The present invention relates to 1-methylpyrazole-piperazine compounds having dual pharmacological activity towards both the sigma (σ) receptor, and the μ-opiod receptor, to processes of preparation of such compounds, to pharmaceutical compositions compri
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Page/Page column 106; 107
(2016/07/05)
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- 1-METHYLPYRAZOLE MODULATORS OF SUBSTANCE P, CALCITONIN GENE-RELATED PEPTIDE, ADRENERGIC RECEPTOR, AND/OR 5-HT RECEPTOR
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The present invention relates to new 1-methylpyrazole modulators of substance P release, calcitonin gene-related peptide activity, adrenergic receptor activity, and/or 5 -HT receptor activity, pharmaceutical compositions thereof, and methods of use thereof.
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Page/Page column 33
(2010/11/05)
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- Effects of base, electrophile, and substrate on the selective alkylation of heteroaromatic systems
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Several heteroaromatic systems, including oxazoles, pyrazoles, and thiophenes, are regioselectively alkylated using lithium diethylamide. Effects of substrate, base, and electrophile on the selectivity of this process are surveyed and interpreted.
- Smith, Thomas E.,Mourad, Michelle S.,Velander, Alan J.
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p. 1211 - 1217
(2007/10/03)
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- Process for separating carbinols
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A method for predominantly preparing the enantiomer (R)-(+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole, (R)-(+)-1, by separating the racemate (+)-5-(phenyl)hydroxymethyl-1-methyl-1H-pyrazole of formula (1), comprising the series of steps of using a lipa
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- Regioselective Halo- and Carbodesilylation of (Trimethylsilyl)-1-methylpyrazoles
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The isomeric 3-, 4-, and 5-(trimethylsilyl)- as well as the 3,4-, 3,5-, and 4,5-bis(trimethylsilyl)-1-methylpyrazoles (2, 7, 3, 5, 9, and 10, respectively) are obtained by methylation of the corresponding (trimethylsilyl)-1H-pyrazoles or by silylation of Grignard or lithio derivatives of appropriate 1-methylpyrazoles with chlorotrimethylsilane. 5 and 10 are halodesilylated regioselectively by Br2 or ICl in the 4-position, yielding 13 and 15.With addditional bromine, these monobromo compounds suffer exclusively bromodesilylation to give 3,4- and 4,5-dibromo-1-methylpyrazole (14 and 16, respectively).These findings are in accord with the electrophilic substitution reactivity indices for 1-methylpyrazole (8) and with ipso-directing influence of the Me3Si group.The reaction of 5 with I2, unexpectedly, attacks preferentially at the 3-position.Regioselective carbodesilylation in the 5-position is observed in the fluoride-catalyzed reactions of 3, 9, and 10 with carbon electrophiles.The high regiospecificity of this reaction is rationalized in terms of carbanion stabilization at the individual pyrazole positions.
- Effenberger, Franz,Krebs, Andreas
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p. 4687 - 4695
(2007/10/02)
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- ALPHA-LITHIATION OF N-ALKYL GROUPS IN PYRAZOLES
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1,3,5-Trimethylpyrazole and 1-ethyl-3,5-dimethylpyrazole undergo lithiation exclusively at the α-position of the N-alkyl group. 1-Benzylpyrazole is metallated under kinetic control at -78 deg C at the CH2 group, but the metallorganic intermediate rearrang
- Katritzky, Alan R.,Jayaram, Chandra,Vassilatos, Socrates N.
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p. 2023 - 2029
(2007/10/02)
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