- Transition-Metal-Free Silylation of Unactivated C(sp2)-H Bonds withtert-Butyl-Substituted Silyldiazenes
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Aromatic organosilanes bearing C(sp2)-Si bonds have found increasing applications across the chemical science, yet are mostly produced by atom-uneconomical stoichiometric procedures. Catalytic alternatives using hydrosilanes as silicon sources
- Neil, Baptiste,Lucien, Franck,Fensterbank, Louis,Chauvier, Clément
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p. 13085 - 13090
(2021/11/01)
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- Synthesis method of 2-bromo-3-fluobenzoic acid
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The invention discloses a synthesis method of 2-bromo-3-fluobenzoic acid. The method comprises the following steps of (1) using o-bromo fluorobenzene as starting raw materials; performing proton abstraction through lithium diisopropylamide; performing rea
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Paragraph 0021; 0024; 0027
(2018/06/16)
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- Pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is optionally substituted phenyl, furanyl, thienyl, pyridyl, pyridyl N-oxide, oxazolyl or pyrrolyl, or cycloalkenyl R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; and Z is optionally substituted aryl or heteroaryl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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Page/Page column 35
(2008/06/13)
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- NEW DISUBSTITUTED PHENYLPIPERIDINES/PIPERAZINES AS MODULATORS OF DOPAMINE NEUROTRANSMISSION
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The present invention relates to compounds which have therapeutic effects against disorders in the central nervous system, and in particular new 4-(ortho, meta-disubstituted phenyl)-1-alkypiperidines and piperazines. (I) wherein R1, R2, R3 and Y are as de
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Page/Page column 65
(2008/06/13)
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- 2-Alkynyl-and 2-alkenyl-pyrazolo-[4,3-e]-1,2,4-triazolo-[1,5-c]-pyrimidine adenosine A2a receptor antagonists
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Compounds having the structural formula I or a pharmaceutically acceptable salt thereof, wherein R is R1, R2, R3, R4 and R5 are H, alkyl or alkoxyalkyl; R6 is H, alkyl, hydroxyalkyl or —CH2F; R7, R8 and R9 are H, alkyl, alkoxy, alkylthio, alkoxyalkyl, halo or —CF3; and Z is optionally substituted aryl, heteroaryl or heteroaryl-alkyl are disclosed. Also disclosed is the use of compounds of formula I in the treatment of central nervous system diseases, in particular Parkinson's disease, alone or in combination with other agents for treating Parkinson's disease, and pharmaceutical compositions comprising them.
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- Bromine as the Ortho-Directing Group in the Aromatic Metalation/Silylation of Substituted Bromobenzenes
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The one-pot metalation/disilylation of selected bromobenzenes bearing electron-withdrawing substituents p-, m-, o-XC6H4Br (X = F, Cl, I, CN, CF3) using 2 equiv of lithium diisopropylamide (LDA) and 2 equiv of chlorotrimethylsilane (TMSCl) was investigated. The best results of disilylation were obtained for para-substituted bromobenzenes, but the regioselectivity of the reaction is strongly influenced by the ortho-directing power of the substituent. On the contrary, the disilylation of metasubstituted bromobenzenes was not efficient or even failed in some cases and hence monosilylated derivatives were isolated as major or sole products. Diverse reactivity was observed for orthosubstituted bromobenzenes, e.g., 2-bromobenzonitrile and 2-bromochlorobenzene, were converted into corresponding disilylated derivatives in a high and moderate yield, respectively, whereas 1-bromo-2-(trifluoromethyl)benzene underwent only monosilylation.
- Lulinski, Sergiusz,Serwatowski, Janusz
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p. 9384 - 9388
(2007/10/03)
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- Lithiations directed by carboxylic acid, fluorine and chlorine: The regioselective synthesis of polysubstituted benzoic acids and acetophenones
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Lithiation/electrophilic quenching of ortho-lithiated benzoates allows the totally regiocontrolled synthesis of a wide range of 2,3-, 2,3,4-, and 2,3,4,5-polysubstituted benzoic acids and related acetophenones. Elsevier,.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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p. 133 - 141
(2007/10/03)
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- Regiospecific Synthesis of Mixed 2,3-Dihalobenzoic Acids and Related Acetophenones via Ortho-Metalation Reactions
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Concise general routes to mixed 2,3-dihalobenzoic acids and related acetophenones-based on directed ortho-metalation and ipso-desilylation reactions are described.
- Moyroud, Joel,Guesnet, Jean-Luc,Bennetau, Bernard,Mortier, Jacques
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p. 881 - 884
(2007/10/02)
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