- Preliminary structure-activity relationship (SAR) of a novel series of pyrazole SKF-96365 analogues as potential store-operated calcium entry (SOCE) inhibitors
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From a series of (1R, 1S)-1[β-(phenylalkoxy)-(phenetyl)]-1H-pyrazolium hydrochloride as new analogues of SKF-96365, one has an interesting effect for endoplasmic reticulum (ER) Ca2+ release and store-operated Ca2+ entry (SOCE) (ICsu
- Dago, Camille D.,Le Maux, Paul,Roisnel, Thierry,Brigaudeau, Christophe,Bekro, Yves-Alain,Mignen, Olivier,Bazureau, Jean-Pierre
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- Y(NO3)3·6H2O catalyzed regioselective ring opening of epoxides with aliphatic, aromatic, and heteroaromatic amines
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Yttrium nitrate hexahydrate [Y(NO3)3·6H2O] was found to be an efficient catalyst for selective ring opening of epoxides with aliphatic, aromatic, and heteroaromatic amines at room temperature under solvent-free conditions. The system tolerated a variety of hindered and functionalized epoxides/amines and afforded the desired β-amino alcohols at low catalyst concentration.
- Bhanushali, Mayur J.,Nandurkar, Nitin S.,Bhor, Malhari D.,Bhanage, Bhalchandra M.
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p. 3672 - 3676
(2008/09/19)
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- An efficient synthesis of β-hydroxyethylpyrazoles from propylene and styrene oxide using Cs2CO3
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Bases such as caesium carbonate efficiently catalyze the regioselective ring opening of propylene and styrene oxide with various substituted pyrazoles.
- Duprez, Virginie,Heumann, Andreas
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p. 5697 - 5701
(2007/10/03)
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- Ytterbium triflate catalyzed reactions of epoxide with nitrogen heterocycles under solvent-free condition
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Ytterbium triflate was found to effectively catalyze the reaction of epoxides with nitrogen heterocycles. The reactions afforded hydroxyl alkylated products in high yields.
- Luo, Sanzhong,Zhang, Baolian,Wang, Peng G.,Cheng, Jin-Pei
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p. 2989 - 2994
(2007/10/03)
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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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- High-pressure organic chemistry. 19. High-pressure-promoted, silica gel-catalyzed reaction of epoxides with nitrogen heterocycles
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The reaction of epoxides with nitrogen heterocycles such as indoles, pyrroles, imidazoles, and pyrazoles was studied under both high-pressure and silica gel-catalyzed conditions. Whereas it has been reported that the treatment of indole with styrene oxide
- Kotsuki, Hiyoshizo,Hayashida, Katsunori,Shimanouchi, Tomoyasu,Nishizawa, Hitoshi
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p. 984 - 990
(2007/10/03)
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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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