102987-40-6Relevant academic research and scientific papers
Compound of dipyrrolopyridine structure Preparation method and medical application
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Paragraph 0147-0150, (2021/08/25)
The invention discloses a compound with a dipyrrolo-pyridine structure as well as a preparation method and medical application thereof. The compound provided by the invention has obvious inhibitory activity on JAK family proteins, is an effective JAK inhibitor, and has the prospect of being developed into drugs for inhibiting JAK and further treating diseases.
Palladium-Catalyzed Decarboxylative Benzylation of Acetylides and Enolates
Torregrosa, Robert R. P.,Mendis, Shehani N.,Davies, Alex,Tunge, Jon A.
, p. 3205 - 3216 (2018/08/17)
Benzylic alkylation of enolates and acetylides has been achieved through the use of a decarboxylative benzylation strategy. Previous research in this area is often limited by the need for extended conjugation in the electrophiles that are coupled. Herein, we report that the use of 1,1'-bis(diphenylphosphino)ferrocene (dppf) ligand allows the coupling of simple benzyl electrophiles with enolates, while the use of XPhos ligand promotes the decarboxylative couplings of propiolates.
Enantioselective Synthesis of the Tricyclic Core of FR901483 Featuring a Rhodium-Catalyzed [2+2+2] Cycloaddition
Perreault, Stéphane,Rovis, Tomislav
, p. 719 - 728 (2013/04/23)
An efficient approach to the tricyclic framework of FR901483 is described. The sequence features a [3,3]-sigmatropic rearrangement of a cyanate to an isocyanate, followed by its subsequent asymmetric rhodium-catalyzed [2+2+2] cycloaddition with a terminal
Synthesis of substituted anthracenes, pentaphenes and trinaphthylenes via alkyne-cyclotrimerization reaction
Saino, Naoko,Kawaji, Tsuyoshi,Ito, Taichi,Matsushita, Yuko,Okamoto, Sentaro
scheme or table, p. 1313 - 1316 (2010/04/29)
The [2+2+2] cycloaddition reaction of 1,6-diynes 3 with 4-aryl-2-butyn-1-ols 4 and the following oxidation of the resulting benzylic alcohols to the aldehydes 1 and then treatment with an acid catalyst provided annulated anthracenes 2 in good yields.
Ruthenium-catalyzed propargylic reduction of propargylic alcohols with silanes
Nishibayashi, Yoshiaki,Shinoda, Akira,Miyake, Yoshihiro,Matsuzawa, Hiroshi,Sato, Mitsunobu
, p. 4835 - 4839 (2007/10/03)
Ru2 can do it! Substitution of the OH moiety in propargylic alcohols by hydride proceeds smoothly with triethylsilane by catalysis with the thiolate-bridged diruthenium complex 1 (see scheme; Cp* = η5-C5Me5). Th
Cobalt-catalyzed benzyl-alkynyl coupling
Kuno, Akiko,Saino, Naoko,Kamachi, Taku,Okamoto, Sentaro
, p. 2591 - 2594 (2007/10/03)
Benzylic halides coupled with 1-alkynylmagnesium halides in the presence of a catalytic amount of Co(acac)3 to provide 1-aryl-2-alkynes in moderate to good yield.
Indium tribromide-catalyzed deacetoxylation of propargylic acetate with triethylsilane
Sakai, Norio,Hirasawa, Maki,Konakahara, Takeo
, p. 6407 - 6409 (2007/10/03)
Indium(III) bromide catalyzed the deacetoxylation of propargylic acetates with Et3SiH to produce the corresponding internal alkynes containing a variety of functional groups in good yields.
Ipso Selectivity in the Reductive Iodonio-Claisen Rearrangement of Allenyl(p-methoxyaryl)iodinanes
Ochiai, Masahito,Ito, Takao,Masaki, Yukio
, p. 15 - 16 (2007/10/02)
Allenyl(aryl)iodinanes, generated from p-methoxy(diacetoxyiodo)arenes by the reaction with propyn-2-yl(trimethyl)silanes in the presence of BF3-Et2O in dichloromethane, undergo reductive ipso iodonio-Claisen rearrangement selectively at -20 deg C yielding
A NOVEL AND EFFICIENT METHOD TO PREPARE 3-(HETERO)ARYL-1-PROPYNES AND ITS APPLICATION TO THE STEREOSELECTIVE SYNTHESIS OF (2E,4E)-N-(2-METHYLPROPYL)-6-(2-METHYLPROPYL)-6-(2-THIENYL)-2,4-HEXADIENAMIDE, PIPEROVATINE AND (E)-N-(2-METHYLPROPYL)-6-(4-METHOXYPHENYL)-4-HEXYN-2-ENAMIDE
Rossi, Renzo,Carpita, Adriano,Lippolis, Vito,Benetti, Massimo
, p. 783 - 791 (2007/10/02)
Chemically pure 3-(hetero)aryl-1-propynes, 13, have been prepared in high overall yields by a novel method which involves: (a) a copper(I)-mediated cross-coupling between a halomethyl(hetero)arene, 16, and trimethylsilylethylmagnesium bromide, 17, to give a trimethylsilyl-3-(hetero)aryl-1-propyne, 18; (b) removal of the trimethylsilyl group from 18 by treatment with potassium fluoride dihydrate in DMF.One of these 1-alkynes, i.e. 3-(2-thienyl)-1-propyne, 13a, has been employed in the key step of a highly stereoselective synthesis of naturally-occurring (2E,4E)-N-(2-methylpropyl)-6-(2-thienyl)-2,4-hexadienamide, 6.On the other hand, 3-(4-methoxyphenyl)-1-propyne, 13b, has been used either in two stereoselective syntheses of another natural N-(2-methylpropyl) amide, i.e. piperovatine, 7, or in the preparation of a structural analogue of 7, i.e. (E)-N-(2-methylpropyl)-6-(4-methoxyphenyl)-4-hexyn-2-enamide, 15.
