- 1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes in the pores of zeolite NaY
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Zeolite NaY promotes 1,3-dipolar cycloaddition of ethyl diazoacetate to alkynes having an electron-withdrawing group to afford the corresponding functionalized pyrazoles in high yields. The activation of the dipolarophile inside the pores of NaY is proposed based on the 13CMASNMR analysis. Copyright
- Kobayashi, Keijiro,Igura, Yuta,Imachi, Shouhei,Masui, Yoichi,Onaka, Makoto
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- SUBSTITUTED PYRAZOLE COMPOUNDS, COMPOSITIONS CONTAINING SAME, AND USE THEREOF
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The present invention provides substituted pyrazole compounds, compositions containing same, and use thereof. The substituted pyrazole compounds comprise a compound represented by formula (I) or a tautomer, stereoisomer, prodrug, crystalline form, pharmaceutically acceptable salt, hydrate, or solvate thereof. The compound represented by formula (I) can serve as a tissue selective androgen receptor modulator (SARM), particularly serving as a drug for treating prostate cancer and other AR-dependent conditions and diseases in which AR antagonism is desired.
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Paragraph 0244-0245
(2022/01/12)
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- Compound and process for synthesizing 5-acetyl-1H-pyrazole-3-carboxylic acid by using compound
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The invention belongs to the field of chemical synthesis of substances and discloses a compound, application and a process for synthesizing 5-acetyl-1H-pyrazole-3-carboxylic acid by using the compound. A compound 2, 3-butanedione is used as a starting material to synthesize a compound intermediate III, the compound intermediate III is separated out from the system, the product conversion is promoted, the purification purpose can be achieved through filtration, the conversion rate reaches 95%, and the yield is increased; synthesis of an intermediate IV: by taking the intermediate III and a hydrazine compound as raw materials, the pH of the system is regulated, the yield is increased, and impurity production is reduced; after the reaction is ended, concentrating and filtering are carried out, so that the yield reaches 98%, and the HPLC purity is greater than 98.5%; and through the operation, high-purity V is obtained. The process of the invention is simple and safe, high in yield, suitable for industrialization, beneficial to impurity control and capable of reducing quality risks.
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Paragraph 0016; 0046-0047
(2020/06/02)
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- Metal-free C-C, C-O, C-S and C-N bond formation enabled by SBA-15 supported TFMSA
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The construction of intermolecular C-C, C-O, C-S and C-N bonds between diazo compounds and acyclic and cyclic 1,3-dicarbonyl compounds, thiophenol and alkynes was developed by using TFMSA@SBA-15, thus providing a metal-free and eco-friendly platform for f
- Yi, Xiangyan,Feng, Jiajun,Huang, Fei,Baell, Jonathan Bayldon
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supporting information
p. 1243 - 1246
(2020/02/04)
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- Synthesis of 1,3-dioxo-substituted allenes via copper(I)-catalyzed coupling of α-oxo-alkynes and α-oxo-diazos by controlling the sequence of adding substrates
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A novel direct synthesis of 1,3-dioxo-substituted allenes was developed by copper(I)-catalyzed coupling of α-oxo-alkynes and α-oxo-diazos. It was a sequence of adding substrates-controlled method and the desired products were synthesized chemoselectively by adding α-oxo-alkyne terminally.
- Liu, Chulong,Weng, Yunxiang,Zeng, Xiaobao,Zheng, Weiping,Wang, Xinyan,Hu, Yuefei
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p. 493 - 496
(2019/01/15)
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- Synthetic method for one-step C-N construction C-S of C-C(I), (C) and (C)-(C) bonds (by machine translation)
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An acid load type catalyst is used under the heating C - C condition C - N, C - S and under the heating condition, the α - protonation of the heavy nitrogen ester is carried out, and the construction of the keys is realized in one step, and the method α -
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Paragraph 0036-0038; 0054-0065
(2019/11/28)
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- Synthesis of functionalized pyrazole derivatives by regioselective [3+2] cycloadditions of N-Boc-α-amino acid-derived ynones
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[3+2] cycloadditions of ynones derived from glycine and (S)-alanine and some other dipolarophiles with azomethine imines, nitrile oxides, diazoacetate, and azidoacetate were studied. The dipolarophiles were obtained from α-amino acids, either by the reduc
- Kirar, Eva Pu?avec,Gro?elj, Uro?,Golobi?, Amalija,Poagan, Franc,Ri?ko, Sebastijan,?tefane, Bogdan,Svete, Jurij
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p. 467 - 480
(2018/06/18)
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- PYRAZOLYL SUBSTITUTED TETRAHYDROPYRANYLSULFONES
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The invention relates to pyrazolyl substituted tetrahydropyranylsulfones as voltage gated calcium channel blockers, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
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Paragraph 0294; 0295
(2017/05/14)
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- NOVEL COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS THEREOF FOR THE TREATMENT OF CYSTIC FIBROSIS
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The present invention discloses compounds according to Formula I: wherein R1 is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
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Paragraph 0707
(2015/02/25)
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- THIENO[2,3-C]PYRANS AS CFTR MODULATORS
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The present invention discloses compounds according to Formula I: Wherein R is as defined herein. The present invention relates to compounds and their use in the treatment of cystic fibrosis, methods for their production, pharmaceutical compositions comprising the same, and methods of treatment cystic fibrosis by administering a compound of the invention.
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Paragraph 00211
(2015/02/25)
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- PYRAZOLYL-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
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The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
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Paragraph 0328-0332
(2014/03/24)
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- PYRAZOLYL-PYRIMIDINE DERIVATIVES AS KINASE INHIBITORS
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The present invention relates to pyrazolyl-pyrimidine derivatives which modulate the activity of protein kinases and are therefore useful in treating diseases caused by dysregulated protein kinase activity. The present invention also provides methods for preparing these compounds, pharmaceutical compositions comprising these compounds, and methods of treating diseases utilizing such compounds or the pharmaceutical compositions containing them.
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Page/Page column 36
(2012/11/06)
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- 5-SUBSTITUTED 2H-PYRAZONE-3-CARBOXYLIC ACID DERIVATIVES AS ANTILIPOLYTIC AGENTS FOR THE TREATMENT OF METABOLIC-RELATED DISORDERS SUCH AS DYSLIPIDEMIA
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The present invention relates to certain pyrazole carboxylic acid derivatives of Formula (Ia), and pharmaceutically acceptable salts thereof, as antilipolytic agents and against for the receptor RUP25, wherein: R2 is H, halogen, C1-12/sub
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Page/Page column 64-65
(2008/06/13)
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- Novel 1,3-dipolar cycloaddition of diazocarbonyl compounds to alkynes catalyzed by InCl3 in water
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The first intermolecular 1,3-dipolar cycloaddition of diazocarbonyl compounds with alkynes was developed by using an InCl3 catalyzed cycloaddition in water. The reaction was found to proceed by a domino 1,3-dipolar cycloaddition-hydrogen (alkyl or aryl) migration.
- Jiang, Nan,Li, Chao-Jun
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p. 394 - 395
(2007/10/03)
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- Substituted pyrazolyl compounds and methods employing such compounds
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This invention pertains to novel substituted pyrazolyl compounds useful as intravenous anesthetics represented by the Formula: STR1 including geometric and optically active isomeric forms, and the pharmaceutically acceptable acid addition salts thereof, wherein: one of Y and Z is nitrogen, and the other is CH; R1 is hydrogen or lower-alkyl; R2 and R3 are selected from the group consisting of hydrogen, --CHO, lower-alkylcarbonyl, lower-alkoxy carbonyl, lower-alkylaminocarbonyl, lower-alkyl, lower-alkenyl, lower-alkoxy-lower-alkenyl, lower-alkylcarbonyloxymethyl, substituted and unsubstituted heterocyclic rings, and substituted or unsubstituted aryl groups, wherein the symbol * represents a carbon atom which may be asymmetric and at least one of R2 and R3 is other than hydrogen.
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