- Synthesis and reactions of 5-tributylstannyl-4-fluoro-1H-pyrazole
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The palladium-catalyzed cross-coupling reactions of 5-tributylstannyl-4-fluoro-1H-pyrazole with aryl iodides provided high yields of the corresponding 5-aryl-4-fluoro-1H-pyrazoles. Furthermore, these cross-coupling reactions proceeded smoothly under an atmosphere of carbon monoxide (CO) to afford the corresponding 5-acyl-4-fluoro-1H-pyrazoles as CO-insertion products.
- Hanamoto, Takeshi,Suetake, Takao,Koga, Yukinori,Kawanami, Toshio,Furuno, Hiroshi,Inanaga, Junji
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- Preparation method of 4-fluoro-1H-pyrazole
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The invention discloses a preparation method of 4-fluoro-1H-pyrazole, and particularly relates to an effective method for preparing the 4-fluoro-1H-pyrazole (compound I) by using a one-pot process. The method comprises the following steps: selecting concentrated hydrochloric acid as acid, selecting Selectfluor as a fluorination reagent, hydrolyzing 1, 1, 3, 3-tetramethoxypropane (compound II), and closing a pyrazole ring by using the one-pot process to prepare the 4-fluoro-1H-pyrazole (compound I). The method is convenient to operate, stable in yield and suitable for industrial production.
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Paragraph 0036-0045
(2021/10/02)
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- SUBSTITUTED PYRIMIDINES
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Disclosed are substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
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Page/Page column 87; 88
(2013/04/10)
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- SUBSTITUTED PYRIMIDINES
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The present invention relates to substituted pyrimidines useful as HIF prolyl hydroxylase inhibitors to treat anemia and like conditions.
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Page/Page column 87; 88
(2013/04/10)
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- An improved synthesis of a novel α1A partial agonist including a new two-step synthesis of 4-fluoropyrazole
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This Letter outlines a new two-step process for the synthesis of 4-fluoropyrazole and its application in an improved synthesis of 4-fluoro-1-[5-fluoro-1-(1H-imidazol-2-yl)-indan-4-ylmethyl]-1H-pyrazole. The original synthesis of 4-fluoro-1-[5-fluoro-1-(1H-imidazol-2-yl)-indan-4-ylmethyl]-1H-pyrazole is also described.
- England, Katherine,Mason, Helen,Osborne, Rachel,Roberts, Lee
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experimental part
p. 2849 - 2851
(2010/07/06)
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- 2-AMINO PYRIMIDINE COMPOUNDS AS POTENT HSP-90 INHIBITORS
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The present invention is directed to compounds of formula (I), or pharmaceutically acceptable salts thereof, their synthesis, and their use as HSP-90 inhibitors.
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Page/Page column 26-27
(2010/03/04)
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- N-Arylation of 4-fluoro-5-trimethylsilyl-1H-pyrazole
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The 1,3-dipolar cycloaddition reaction of fluoro(trimethylsilyl)acetylene prepared in situ with an excess of diazomethane smoothly proceeded to give the corresponding 4-fluoro-5-trimethylsilyl-1H-pyrazole in 84% yield. The copper iodide-catalyzed N-arylation of the fluorinated pyrazole with a variety of aryl iodides afforded N-aryl-4-fluoropyrazoles as desilylation products in good to excellent yields.
- Hanamoto, Takeshi,Iwamoto, Yuhko,Yamada, Kenji,Anno, Ryoko
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p. 1126 - 1130
(2008/02/10)
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- Palladium catalyzed cross-coupling reaction of 5-tributylstannyl-4- fluoropyrazole
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The palladium catalyzed cross-coupling reactions of aryl iodides and 5-tributylstannyl-4-fluoropyrazole prepared from fluoro(tributylstannyl) acetylene proceeded smoothly giving the corresponding 5-aryl-4-fluoropyrazole in good yields. The Royal Society of Chemistry 2005.
- Hanamoto, Takeshi,Koga, Yukinori,Kido, Eisaku,Kawanami, Toshio,Furuno, Hiroshi,Inanaga, Junji
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p. 2041 - 2043
(2007/10/03)
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- Composition and antiviral activity of substituted azaindoleoxoacetic piperazine derivatives
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This invention provides compounds having drug and bio-affecting properties, their pharmaceutical compositions and method of use. In particular, the invention is concerned with azaindoleoxoacetyl piperazine derivatives. These compounds possess unique antiviral activity, whether used alone or in combination with other antivirals, antiinfectives, immunomodulators or HIV entry inhibitors. More particularly, the present invention relates to the treatment of HIV and AIDS.
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- Reactions of β-Fluorovinamidinium Salt with Bifunctional Hetero Nucleophiles. A New Synthetic Route to Fluorinated Heterocycles
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β-Fluorovinamidium salt (2), readily prepared from N-(2,3,3-trifluoro-1-propenyl) trimethyl-ammonium iodide (1) and diethylamine, reacted with bifunctional hetero nucleophiles such as amidine and guanidine hydrochlorides in the presence of a base to afford regiospecifically monofluoronated pyrimidines 4 in good yields.The one-pot procedure starting from 1 was applicable for synthesizing heterocyclic compounds 4 in almost comparable yields.
- Shi, Xifeng,Ishihara, Takashi,Yamanaka, Hiroki,Gupton, John T.
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p. 1527 - 1530
(2007/10/02)
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- 1-fluoro-1-halo-3,6-dioxabicyclo [4.1.0]heptane preparation, process and use
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A class of compounds, namely 1-fluoro-1-halo-3,6-dioxabicyclo[4.1.0]heptanes and a process using these compounds in the preparation of fluoromalonaldehyde acetals. The 1-fluoro-1-halo-3,6-dioxabicyclo[4.1.0]heptane is brought into contact with an alcohol in an acid medium. The fluoromalonaldehyde acetals obtained are also new products, which are useful for the synthesis of alkyl fluoromalonates or of fluorinated nitrogen-containing heterocycles.
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