- Solvent-free mechanochemical oxidation and reduction of biomass-derived 5-hydroxymethyl furfural
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The simultaneous synthesis of 5-hydroxymethyl-2-furoic acid and 2,5-hydroxymethylfuran from biomass-derived 5-hydroxymethyl furan was developed using a solvent-free mechanochemical approach. The results obtained for the Cannizzaro disproportionation reaction show quantitative conversions of the starting materials with reaction times of only 5 min. Employing solvent-free conditions allows for a more sustainable synthetic approach that is reflected in an Efactor 7 times smaller than that in previous reports. Additionally, initial results of the use of a sacrificial reagent, with the same solvent-free mechanochemical approach, for the selective reduction and oxidation of HMF are presented.
- Chacón-Huete,Messina,Chen,Cuccia,Ottenwaelder,Forgione
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p. 5261 - 5265
(2018/12/05)
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- INHIBITORS OF STEAROYL-COA DESATURASE
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Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of diseases such as, for example, obesity.
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- PdII-catalyzed monoselective ortho halogenation of C-H bonds assisted by counter cations: A complementary method to directed ortho lithiation
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(Chemical Equation Presented) When the counterion counts: The yield and selectivity of the title transformation of benzoic acid derivatives were improved greatly by using tetraalkyl ammonium salts as additives (see scheme; monoselectivity: 5:1-18:1). These effects are attributed to the influence of counter cations. The halogenated products are versatile intermediates for the construction of substituted aromatic compounds. DMF=N,N-dimethylformamide.
- Mei, Tian-Sheng,Giri, Ramesh,Maugel, Nathan,Yu, Jin-Quan
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supporting information; experimental part
p. 5215 - 5219
(2009/04/11)
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- FXR AGONISTS
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Compounds of formula wherein variables are as defined herein and their pharmaceutical compositions and methods of use are disclosed as useful for treating dyslipidemia and related diseases.
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Page/Page column 62-63
(2008/06/13)
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- Thioxanthenone antitumor agents
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Compounds having anti-tumour activity are disclosed having the formulawherein: (1) n is 2 or 3;R1 and R2 are independently lower-alkyl;Q is a residue chosen from the group consisting ofCH2NHR3, CH2N(R4)SO2R7, CH2NHCHO, CH=N-Ar,C(O)NR5R6, CH2N(R4)C(O)R7, CH2N(C2H5)CHO,CH2N(R4)P(O)(O-lower-alkyl)2, CH2N=CH-N(R9)(R10),CH2N(R4)C(O)CF3 and CH2N(R4)C(O)OR7;R3 is hydrogen or lower-alkyl;R4 is hydrogen, lower-alkyl or Ar;R5 is hydrogen, lower-alkyl or Ar;R6 is hydrogen or lower-alkyl;R7 is lower-alkyl, or Ar;R8 is hydroxy;Ar is phenyl or phenyl substituted with methyl, methoxy, hydroxy, halogen or nitro; andR9 and R10 are independently lower-alkyl; or(2) Q is a residue chosen from the group consisting of CH2N(R4)SO2R7, CH=N-Ar, C(O)NR5R6, CH2N(R4)C(O)R7, CH2N(R4)P(O)(O-lower-alkyl)2, CH2N(R4)C(O)CF3 and CH2N(R4)C(O)OR7; R8 is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; Ar is phenyl substituted by hydroxy; and n, R1, R2, R4, R5, R6, and R7 are as defined hereinabove in part (1) with the proviso that one or more of R4, R5, or R7 is Ar; or(3) Q is a residue chosen from the group consisting of CH2N=CH-N(R9)(R10) and CH2N(R4)C(O)CF3 ; R8 is hydrogen, lower-alkyl, lower-alkoxy, or hydroxy; and n, R1, R2, R4, R7, Ar, R9 and R10 are as defined hereinabove in part (1), or a pharmaceutically acceptable acid-addition salt or solvate thereof . Compositions containing the thioxanthenones and methods of treating tumors and cancer in mammals with the thioxanthenones are also disclosed.
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- SYNTHESIS AND POLYMERIZATION OF 2,5-DISUBSTITUTED PHENYLACETYLENES CONTAINING TRIFLUOROMETHYL GROUPS
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Four phenylacetylenes (2-R2-5-R5-C6H3CCH : 1a R2=R5=CF3; 1b R2=CF3, R5=CH3; 1c R2=CH3, R5=CF3; 1d R2=R5=CH3) were synthesized via lithio compounds or Grignard reagent.Bromo(methyl)benzotrifluorides, the precursors for the lithio compounds, were prepared by the fluorination of the corresponding benzoic acids with sulfur tetrafluoride.Polymerization using transition metal catalysts provided polyacetylenes in high yields for all the monomers, while the yields of γ-ray induced polymerization depended on the monomers.The molecular weights of polyacetylenes have a positive correlation with the yields for all the polymerizations.The substituent effects on the molecular weights and tehrmal stabilities of polymers obtained were discussed.
- Nishida, Masakazu,Hosokawa, Kenzo,Ueda, Teruo,Aoki, Toshiki,Muramatsu, Hiroshige
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- ACCES AUX DINITRO-2,4 DIARYLAMINES PAR SUBSTITUTION NUCLEOPHILE SNAr-LIMITES DE LA REACTION ET APPLICATION A LA SYNTHESE DE CYANOCARBAZOLES
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3-Cyanocarbazoles, key-intermediates in the total synthesis of pyrido carbazoles, have been obtained starting from easily available materials and involving the cyclization of diarylamines.The first step of the preparation consists in a SNAr reaction between a para substituted aniline and a chloro- (or bromo)-dinitrobenzene.This nucleophilic substitution has been found to be hindered by the steric effect of a methyl group, explained in terms of inhibition of resonance and confirmed by X-ray determination.
- Henichart, J. P.,Bernier J. L.,Vaccher, C.,Houssin, R.,Warin, V.,Baert, F.
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p. 3535 - 3542
(2007/10/02)
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