- NEW METHOD FOR PREPARATION OF 1-AZABICYCLOOCTANE-4-CARBONITRILE AND 1-AZABICYCLONONANE-5-CARBONITRILE
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The title compounds were prepared from pyridine-4-carboxamide.Its alkylation with 2-chloroethanol or 3-chloropropanol, followed by hydrogenation gave 1-substituted piperidine-4-carboxamides IIIa and IIIb, respectively, which on treatment with thionyl chloride were converted into the respective 1-substituted halogenoalkylpiperidine-4-carbonitriles IVa and IVb.On cyclization, compounds IVa and IVb afforded 1-azabicyclooctane-4-carbonitrile and 1-azabicyclononane-5-carbonitrile, respectively.
- Svoboda, Jiri,Palecek, Jaroslav
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- Anti-Hiv Quinuclidine Compounds
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The invention provides a therapeutic method for preventing or treating a pathological condition or symptom in a mammal, such as a human, wherein the infectivity of a pathogen such as a retrovirus toward mammalian cells is implicated and inhibition of its
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Page/Page column 2-3; 5
(2008/12/07)
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- Pleuromutilin derivatives as antimicrobials
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The present invention relates to pleuromutilin derivatives, to processes for their preparation, to pharmaceutical compositions containing them and to their use in medical therapy, particularly antibacterial therapy.
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- NEW AND EFFICIENT SYNTHESES OF 4-CARBAMOYLQUINUCLIDINE
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Two efficent routes starting from 4-carbamoylpiperidine or 2,2',2''-trichlorotriethylamine were developed for preparing 4-cyanoquinuclidine which was hydrolyzed to give 4-carbamoylquinuclidine, a chemical modifier of cephalosporin antibiotics.
- Kanai, Takeo,Nomoto, Seiichiro,Komatsu, Yuhki,Ogura,Katsuyuki
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p. 2137 - 2142
(2007/10/02)
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- 4-cyanopiperidine derivatives
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A novel 4-cyanopiperidine derivative, which is represented by the following general formula (I): STR1 wherein X means a halogen atom, or an acid addition salt thereof, is prepared by reacting N-(2-hydroxyethyl)-4-carbamoylpiperidine or an acid addition salt thereof with a dehydrating and halogenating agent; or by reacting 4-cyanopiperidine or a salt thereof with a compound represented by the following general formula (IV): wherein X has the same meaning as defined above and Y denotes the same halogen atom as X or another halogen atom. The derivative is useful as intermediate for synthesis of quinuclidine derivative which is in turn useful as intermediate for the production of medicines, chemicals, etc.
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- Process for the synthesis of 4-cyanoquinuclidine or a salt thereof
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4-Cyanoquinuclidine or a salt thereof is synthetically prepared by reacting a compound represented by the following formula (I): wherein X means a halogen atom, or a salt thereof with acetonitrile in the presence of a base.
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