- ADAMANTANYL-SUBSTITUTED BENZAMIDE COMPOUNDS AND THEIR USE AS P2X7 RECEPTOR ANTAGONISTS
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The present invention relates to adamantanyl-substituted benzamide compounds and their use as antagonists of the P2X7 purinoreceptor. The invention further relates to methods for the treatment of disease and conditions associated with the P2X7 purinoreceptor.
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Page/Page column 20-21; 25
(2020/03/15)
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- Radical cyanocarbonylation using alkyl allyl sulfone precursors
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Acyl cyanides have been prepared by the three-component coupling reactions comprised of alkyl allyl sulfones, carbon monoxide, and p-tolylsulfonyl cyanide under tin-free radical reaction conditions. Georg Thieme Verlag Stuttgart.
- Kim, Sangmo,Cho, Chang Ho,Kim, Sunggak,Uenoyama, Yoshitaka,Ryu, Ilhyong
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p. 3160 - 3162
(2007/10/03)
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- Dual Reaction Channels for Solvolyses of Acyl Chlorides in Alcohol-Water Mixtures
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Rate constants are reported for solvolyses at 0 deg C of trimethylacetyl chloride (3) in 90-30percent v/v acetonitrile-, acetone-, ethanol- and methanol-water mixtures, of adamantane-1-carbonyl chloride (4) in 90-60percent acetone-, ethanol- and methanol-water mixtures, and of cyclopropanecarbonyl chloride (5) in 90-40percent acetone-water.Quantitative product data (acid and ester) are also reported for solvolyses of trimethylacetyl chloride in 98-20percent ethanol- and methanol-water mixtures.Product selectivities (S) show maxima in 90-95percent alcohol-water mixtures, similar to those, reported previously for solvolyses of p-chlorobenzoyl chloride (1a), benzoyl chloride (1b), 2,4,6-trimethylbenzenesulfonyl chloride (2a) and 4-methoxy-2,6-dimethylbenzenesulfonyl chloride (2b).Using rate-rate profiles, logarithms of rate constants are dissected into the competing reaction channels.Given the sharp maxima in S that occur at different alcohol compositions for different substrates, and the link to 'breaks' in rate-rate profiles, the results are consistent with competing mechanisms having different rate-limiting steps.The competing mechanisms involve two broad reaction channels: (1) nucleophilic attack by one molecule of solvent assisted by a second molecule of solvent acting as a general base catalyst-consequently, in aqueous alcohol there are four mechanistic combinations operating simultaneously within this one reaction channel; (2) nucleophilic attack by solvent occurs via a carbocationic reaction within the SN2-SN1 mechanistic spectrum, involving for example, a solvent-separated ion pair intermediate (SN1) or a concerted nucleophilic attack (SN2).
- Bentley, T. William,Shim, Chang Sub
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p. 1659 - 1664
(2007/10/02)
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- Synthesis of 1-adamantyl and 1-adamantylmethyl alkyl ketones
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The reaction of 1-adamantanecarboxylic and 1-adamantylacetic acids with Grignard reagents in the presence of cuprous chloride or iodide gave the corresponding ketones.
- Grava, I. Ya.,Polis, Ya. Yu.,Lidak, M. Yu.,Liepin'sh, E. E.,Shatts, V. D.,et al.
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p. 679 - 686
(2007/10/02)
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