Haloacetylated enol ethers: 12 [18]. Regiospecific synthesis and structural determination of stable 5-hydroxy-1H-pyrazolines
TL;DR: In this article, a series of twelve 3-aryl[alkyl]-5-hydroxy-5-trichloromethyl-4, 5-dihydro-1H-pyrazole-1-carboxyamides and analogous 1-thiocarboxy-amides is reported.
About: This article is published in Tetrahedron.The article was published on 1999-01-08. It has received 49 citations till now. The article focuses on the topics: Enol & Alkyl.
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TL;DR: Ionic Liquids Presented in This Review 2020 3.1.
Abstract: 2.5. Ionic Liquids Presented in This Review 2020 3. Cyclocondensation Reactions 2020 4. Synthesis of Three-Membered Heterocycles 2022 4.1. Aziridines 2022 5. Synthesis of Five-Membered Heterocycles 2022 5.1. Pyrroles 2022 5.2. Furans 2022 5.3. Thiophenes 2023 5.4. Pyrazoles 2024 5.5. Imidazoles 2025 5.6. Isoxazoles 2027 5.7. Oxazoles, Oxazolines, and Oxazolidinones 2027 5.8. Thiazoles and Thiazolidinones 2028 6. Synthesis of Six-Membered Heterocycles 2030 6.1. Pyridines 2030 6.2. Quinolines 2031 6.3. Acridines 2033 6.4. Pyrans 2033 6.5. Flavones 2035 6.6. Pyrimidines and Pyrimidinones 2035 6.7. Quinazolines 2037 6.8. -Carbolines 2038 6.9. Dioxanes 2039 6.10. Oxazines 2039 6.11. Benzothiazines 2040 6.12. Triazines 2040 7. Synthesis of Seven-Membered Heterocycles: Diazepines 2041
631 citations
TL;DR: It is suggested that MPCA and PPCA cause antipyresis, which is similar to that caused by dipyrone, and may be useful antipyretic agents.
128 citations
98 citations
TL;DR: An animal model of fever that is not only advantageous from the economical and technical point of view, but also bears ethical concerns is described, which ultimately causes a significant reduction in the number of animals necessary for antipyretic evaluation.
77 citations
TL;DR: The reaction between aryl or hetero-hydrazines with fluorinated β-diketones (CF3COCH2COR) yields a variety of 3-, 5-, and 3,5-trifluoromethylpyrazoles and 5-trifehyl-5-hydroxy-Δ2-pyrazoli.
Abstract: The reaction between aryl or heteroarylhydrazines with fluorinated β-diketones (CF3COCH2COR) yields a variety of 3-, 5-, and 3,5-trifluoromethylpyrazoles and 5-trifluoromethyl-5-hydroxy-Δ2-pyrazoli...
77 citations
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30 Sep 1997
TL;DR: In this article, the CHEC III is organized in 15 volumes and closely follows the organization used in the previous edition: Volumes 1 and 2: Cover respectively three and four-membered heterocycles, together with all fused systems containing a three- or four-measured heterocyclic ring.
Abstract: CHEC III is organized in 15 Volumes and closely follows the organization used in the previous edition: Volumes 1 and 2: Cover respectively three- and four-membered heterocycles, together with all fused systems containing a three- or four-membered heterocyclic ring. Volume 3: Five-membered rings with one heteroatom together with their benzo- and other carbocyclic-fused derivatives. Volumes 4, 5 and 6: Cover five-membered rings with two heteroatoms, and three or more heteroatoms, respectively, each with their fused carbocyclic compounds. Volumes 7, 8 and 9: Dedicated to six-membered rings with one, two, and more than two heteroatoms, respectively, again with the corresponding fused carbocylic compounds. Volumes 10, 11 and 12: Cover systems containing at least two directly fused heterocyclic five- and/or six-membered rings: of these Volume 10 deals with bi-heterocyclic rings without a ring junction heteroatom, and Volume 11 deals with 5:5 and 5:6 fused rings systems with at least one ring junction nitrogen, while Volume 12 is devoted to all other systems of five and/or six-membered fused or spiro heterocyclic rings with ring junction heteroatoms. Volumes 13 and 14: Seven-membered and larger heterocyclic rings including all their fused derivatives (except those containing three- or four-membered heterocyclic rings which are included in Volume 1 and 2, respectively). Volume 15: Author, ring and subject indexes.
8,174 citations
TL;DR: Compound 14n, a new series of 5-(biphenyl-4-ylmethyl)pyrazoles as potent angiotensin II antagonists, shows high potency both in vitro and in vivo and is selection for clinical evaluation as an antihypertensive agent.
Abstract: The synthesis and pharmacological activity of a new series of 5-(biphenyl-4-ylmethyl)pyrazoles as potent angiotensin II antagonists both in vitro (binding of [3H]AII) and in vivo (iv, inhibition of AII-induced increase in blood pressure, pithed rats; po, furosemide-treated sodium-depleted rats) are reported. The various substituents of the pyrazole ring have been modified taking into account the receptor's requirements derived from related structure−activity relationship studies. A propyl or butyl group at position 1 as well as a carboxylic acid group at position 4 were shown to be essential for high affinity. Different groups at position 3 (H, small alkyl, phenyl, benzyl) provided good binding affinity, but oral activity was highly discriminating: bulky alkyl groups provided the highest potencies. Among the acidic isosteres tested in the biphenyl moiety, the tetrazole group proved to be the best. Compound 14n (3-tert-butyl-1-propyl-5-[[2‘-(1H-tetrazol-5-yl)-1,1‘-biphenyl-4-yl]methyl]-1H-pyrazole-4-carbo...
82 citations
TL;DR: In this paper, a pyrazole ring with a 5-trifluoromethyl substituent was constructed by reaction of 4-alkoxy-1,1, 1, 1-trifi-oro-3-alken-2-ones (1) and hydrazine, methylhydrazine and phenylhydrazines (2) in good yields.
69 citations
TL;DR: In this paper, the synthesis of a series of 5-and 6-substituted 4-trihalomethyl-2-methylthiopyrimidines, prepared from the cyclocondensation reaction of β-alkoxyvinyl tri[fluoro]chloromethsyl ketones with 2-methyl 2-thiopseudourea sulfate, is reported.
62 citations
TL;DR: In this paper, the results of the reaction of β-alkoxyvinyl trihalomethyl ketones 1, 2a-e, with guanidine hydrochloride are reported.
56 citations