- A CONVENIENT SYNTHESIS OF ACETYLENIC KETONES FROM β-DIKETONES USING α,α-DIFLUOROALKYLAMINES AND FREEZE-DRIED POTASSIUM FLUORIDE
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α,α-Difluoroalkylamines, such as 1-diethylamino-2-chloro-1,1,2-trifluoroethane (1) and 1-diethylamino-1,1,2,3,3,3-hexafluoropropane (2), were found to be useful dehydrating agents for the sysnthesis of acetylenic ketones from β-diketones in the presence o
- Kitazume, Tomoya,Ishikawa, Nobuo
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- Highly efficient oxidation of alcohols catalyzed by a porphyrin-inspired manganese complex
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A novel strategy for catalytic oxidation of a variety of benzylic, allylic, propargylic, and aliphatic alcohols to the corresponding aldehydes or ketones by an in situ formed porphyrin-inspired manganese complex in excellent yields (up to 99%) has been successfully developed.
- Dai, Wen,Lv, Ying,Wang, Lianyue,Shang, Sensen,Chen, Bo,Li, Guosong,Gao, Shuang
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supporting information
p. 11268 - 11271
(2015/07/07)
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- Selective oxidation of unsaturated alcohols catalyzed by sodium nitrite and 2,3-dichloro-5,6-dicyano-1,4-benzoquinone with molecular oxygen under mild conditions
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We have developed a simple and practical process for the oxidation of alcohols to the corresponding carbonyl compounds by using a low catalytic amount of DDQ, NaNO2 as a cocatalyst, and molecular oxygen as terminal oxidant. Nitric oxide generated in situ by NaNO2 in the presence of AcOH is essential for the realization of the catalytic cycle at room temperature. The practical utility of this catalytic process has been demonstrated in the gram-scale oxidation of cinnamyl alcohol.
- Wang, Lianyue,Li, Jun,Yang, Hua,Lv, Ying,Gao, Shuang
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experimental part
p. 790 - 794
(2012/02/16)
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- Pd(II)-catalyzed cascade Wacker-Heck reaction: Chemoselective coupling of two electron-deficient reactants
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A novel palladium(II)-catalyzed oxy-carbopalladation process was developed allowing for the orchestrated union of hydroxyynones with ethyl acrylate, two electron-deficient reactants. With β-hydroxy ynones, this cascade Wacker-Heck process gave access to highly functionalized tri- or tetrasubstituted dihydropyranones featuring an unusual dienic system. For diastereomerically pure and for enantioenriched β-hydroxyynones, these reactions proceed without affecting the stereochemical integrity of the existing stereocenters. In addition, tetrasubstituted furanones can be prepared when α-hydroxyynones and ethyl acrylate are used as starting materials. The dihydropyranones and furanones obtained upon cyclization are novel compounds, but structurally related carbohydrate derivatives featuring a similar dienic system have been used as starting materials for the construction of polyannulated products, suggesting that these cascade Pd(II)-mediated oxidative heterocyclizations are of value for various synthetic applications.
- Silva, Franck,Reiter, Maud,Mills-Webb, Rebecca,Sawicki, Marcin,Klaer, Daniel,Bensel, Nicolas,Wagner, Alain,Gouverneur, Veronique
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p. 8390 - 8394
(2007/10/03)
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- N-(3-(4-substituted-1-piperidinyl)-1-phenylpropyl) substituted sulfonamides as NK-3 receptor antagonists
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The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.
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Page/Page column 29-30
(2010/11/30)
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- Modulators of CCR5 chemokine receptor activity
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Compounds of Formula I: (wherein R1, R2, R3, R4, Q, and X are defined herein) are described. The compounds are modulators of CCR5 chemokine receptor activity. The compounds are useful, for example, in the prevention or treatment of infection by HIV and the treatment of AIDS, as compounds or pharmaceutically acceptable salts, or as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines. Methods of treating AIDS and methods of preventing or treating infection by HIV are also described.
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- Chromium(II) Reagents; 1. Reduction of α-Acetylenic Ketones to trans-Enones
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The preparation and chromium(II)-induced reduction of twelve α-acetylenic ketones are reported.In general only trans-olefinic products were observed; the yields ranged from 40-84percent.A particular advantage of this protocol is its selectivity, thereby permitting use with a wide variety of functionalities.
- Smith, Amos B.,Levenberg, Patricia A.,Suits, Joan Z.
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p. 184 - 189
(2007/10/02)
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- REACTION OF HYDROXY AND CARBONYL COMPOUNDS WITH SULFUR TETRAFLUORIDE. IX. REACTIONS OF ALIPHATIC β-DIKETONES WITH SF4
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Aliphatic β-diketones react with sulfur tetrafluoride to form the corresponding di- and tetrafluoro derivatives and also compounds containing double and triple carbon-carbon bonds.In the reactions of 1,1,1-trifluoro derivatives of β-diketones with sulfur tetrafluoride the acyl fluoride is eliminated, and 1,1,1,2-tetrafluoropropene is obtained.Hexafluoroacetylacetone only forms 3-hydroperfluoro-2-pentene under the influence of sulfur tetrafluoride.
- Stepanov, I. V.,Burmakov, A. I.,Kunshenko, B. V.,Alekseeva, L. A.,Yagupol'skii, L. M.
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p. 244 - 248
(2007/10/02)
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