- INTRAMOLECULAR FORMATION OF OXAZOLIUM SALTS AND THEIR REACTION WITH N- AND C-NUCLEOPHILES
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We report the first intramolecular formation of an oxazolium salt and its reaction with N- and C-nucleophiles, leading to isolation of piperidine derivatives via azomethine ylides.Trapping of the latter produced tetrahydroindolizines.
- Hassner, Alfred,Fischer, Bilha
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- INDOLE COMPOUNDS AND PHARMACEUTICAL USE THEREOF
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Provided is an agent for the treatment or prophylaxis of inflammatory diseases, allergic diseases, autoimmune diseases, transplant rejection or the like. A compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, or a solvate thereof: wherein each symbol is as described in the specification.
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Page/Page column 38
(2012/01/03)
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- NK1 and NK3 antagonists
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The invention is to a compound exhibiting neurokinin inhibitory properties, a pharmaceutical composition comprising same and a method of treatment for neurokinin-mediated conditions.
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Page/Page column 28
(2010/02/14)
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- 1,3-Dipolar cycloadditions of new mesoionic compounds. Synthesis of 1H-pyrrolo[1,2-c]thiazoles, pyrrolizines and 5,6,7,8-tetrahydroindolizines
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We studied the 1,3-dipolar cycloaddition reactions between alkyne dipolarophiles and the new mesoionic compounds 2H,5H,7H-thiazolo[4,3-b]oxazol-2-one (12), 2H,5H,7H-pyrrolo[2,1-b]oxazol-2-one (13) and 2H,5H,7H-oxazolo[3,2-a]pyridin-2-one (14). These 1,3-dipoles were prepared in situ by means of cyclodehydration with acetic anhydride of the corresponding α-substituted 4-oxo-3-thiazolidine- (9), 2-oxo-1-pyrrolidine- (10) and 2-oxo-1-piperidineacetic acids (11). The cycloaddition reactions with alkyne dipolarophiles afforded single 1H-pyrrolo[1,2-c]thiazole, pyrrolizine and 5,6,7,8-tetrahydroindolizine derivatives, or a mixture of the two possible regioisomers, depending on whether symmetrical or unsymmetrical alkynes.
- Dalla Croce, Piero,La Rosa, Concetta
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p. 1843 - 1857
(2007/10/03)
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- Novel arylpiperazines as selective α1-adrenergic receptor antagonists
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A novel series of arylpiperazines has been synthesized and identified as antagonists of α(1a) adrenergic receptor (α(1a)-AR) implicated in benign prostatic hyperplasia. These compounds selectively bind to membrane bound α(1a)-AR with K(i)s as low as 0.66 nM. As such, these potentially represent a viable treatment for BPH without the side effects associated with known α1-adrenergic antagonists. (C) 2000 Elsevier Science Ltd. All rights reserved.
- Li, Xiaobing,Murray, William V.,Jolliffe, Linda,Pulito, Virginia
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p. 1093 - 1096
(2007/10/03)
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- Multipath Reactions between Intramolecularly Formed Oxazolium Salts and Nucleophiles
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Reaction of 2-(4'-bromobutyl-5-ethoxyoxazole (1) with nucleophiles led either to SN2 substitution products or to products with a piperidine skeleton.The latter were shown to arise from an intramolecular ring closure to an oxazolium salt 7, whic
- Hassner, Alfred,Fischer, Bilha
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p. 3070 - 3075
(2007/10/02)
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