17953-46-7Relevant academic research and scientific papers
Hit-to-lead optimization of 2-(1H-pyrazol-1-yl)-thiazole derivatives as a novel class of EP1 receptor antagonists
Atobe, Masakazu,Naganuma, Kenji,Kawanishi, Masashi,Morimoto, Akifumi,Kasahara, Ken-Ichi,Ohashi, Shigeki,Suzuki, Hiroko,Hayashi, Takahiko,Miyoshi, Shiro
, p. 6064 - 6067 (2013/11/06)
We describe a medicinal chemistry approach to generate a series of 2-(1H-pyrazol-1-yl)thiazole compounds that act as selective EP1 receptor antagonists. The obtained results suggest that compound 12 provides the best EP1 receptor ant
DABCO-promoted synthesis of pyrazoles from tosylhydrazones and nitroalkenes
Tang, Meng,Zhang, Wen,Kong, Yuanfang
supporting information, p. 6250 - 6254 (2013/09/23)
An efficient synthesis of pyrazoles from tosylhydrazones and nitroalkenes was developed. In comparison with the previously reported 1,3-dipolar cycloaddition reaction of diazo compounds with electron-deficient alkenes or alkynes, this methodology proceeded with a sequential Baylis-Hillman/ intramolecular cyclization mechanism and a variety of reversed regioselectivity products were prepared in good yields.
Palladium-catalyzed carbonylative α-arylation for accessing 1,3-diketones
Gogsig, Thomas M.,Taaning, Rolf H.,Lindhardt, Anders T.,Skrydstrup, Troels
supporting information; experimental part, p. 798 - 801 (2012/03/09)
With a hint of CO: The first Pd-catalyzed carbonylative α-arylations of simple ketones with carbon monoxide is presented for the direct synthesis of 1,3-diketones (see scheme). The method uses only stoichiometric amounts of CO, and hence allows for the si
NITROGEN-CONTAINING HETEROCYCLIC COMPOUNDS
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Page/Page column 45, (2010/03/02)
Nitrogen-containing heterocyclic compounds represented by the following Formula (1) are provided. The compounds or salts thereof have a strong EP1 antagonistic activity when they are administered to a human or an animal, and they are useful as an effective component of a pharmaceutical agent for prophylaxis and/or treatment of an overactive bladder, for example. Furthermore, they are useful as an effective component of a pharmaceutical agent for the prophylaxis and/or treatment of symptoms including frequent urination, urinary urgency and urinary incontinence.
Isothiazoles. Part 3. Cycloadditions of Diazoalkanes to 3-Dialkylaminoisothiazole 1,1-Dioxides. Competitive Ring Cleavage in 3a,4-Dihydro-6aH-pyrazoloisothiazole 1,1-Dioxides: Formation of 2-Thia-3-azabicyclohex-3-ene 2,2-Dioxides and/or Pyrazoles
Clerici, Francesca,Ferrario, Tiziano,Gelmi, Maria Luisa,Marelli, Roberto
, p. 2533 - 2536 (2007/10/02)
3-Dialkylaminoisothiazole 1,1-dioxides 1 readily undergo cycloadditions with diazoalkanes 2.The reaction is characterized by high site- and regio-selectivity.Cycloadducts 3 and 4 were found to undergo straightforward thermolysis reactions at elevated temperature through two different paths characterized respectively by loss of nitrogen or sulfur dioxide and diethylcyanamide.The different transformations affording pyrazoles 6 and derivatives of the new heterocycle 2-thia-3-azabicyclohex-3-ene 2,2-dioxide 5 are discussed.
Catalytic dehydrogenation process for the preparation of 3,4,5-trisubstituted pyrazoles
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, (2008/06/13)
There is provided a process for the preparation of 3,5-disubstituted pyrazoles which involves: A. the reaction of a methyl ketone, such as acetophenone or an appropriate derivative thereof, with an appropriate aldehyde, such as benzaldehyde in the presence of base to form a 1,3-disubstituted α,β-unsaturated ketone, such as chalcone or a substituted chalcone, B. the acidification of said α,β-unsaturated ketone, followed by treatment of the acidified reaction mixture with hydrazine to form a disubstituted pyrazoline, and C. the catalytic dehydrogenation of said pyrazoline to yield the desired 3,5-disubstituted pyrazole.
