- Convenient synthesis of 3,7-diazabicyclo[3.3.1]nonane (bispidine)
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Bispidine 1a is conveniently synthesized via a route involving double Mannich reaction of 1-allylpiperidin-4-one to N,N′-diallylbispidinone, Wolff-Kishner reduction of the bispidinone, and deallylation of the resulting N,N′-diallylbispidine by treatment with ethyl chloroformate in the presence of NaI, followed by alkaline hydrolysis.
- Miyahara,Goto,Inazu
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- C11-CYCLIC SUBSTITUTED 13-MEMBERED MACROLIDES AND USES THEREOF
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Provided are 13-membered macrolides for the treatment of infectious diseases. The 13- membered macrolides described herein are azaketolides. Also provided are methods for preparing the 13-membered macrolides, pharmaceutical compositions comprising the 13-
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Paragraph 00343
(2020/06/10)
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- Highly chemoselective aerobic oxidation of amino alcohols into amino carbonyl compounds
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The direct oxidation of unprotected amino alcohols to their corresponding amino carbonyl compounds has often posed serious challenges in organic synthesis and has constrained chemists to adopting an indirect route, such as a protection/deprotection strategy, to attain their goal. Described herein is a highly chemoselective aerobic oxidation of unprotected amino alcohols to their amino carbonyl compounds in which 2-azaadamantane N-oxyl (AZADO)/copper catalysis is used. The catalytic system developed leads to the alcohol-selective oxidation of various unprotected amino alcohols, carrying a primary, secondary, or tertiary amino group, in good to high yield at ambient temperature with exposure to air, thus offering flexibility in the synthesis of nitrogen-containing compounds. Strong as an ox: The highly chemoselective aerobic oxidation of unprotected amino alcohols to their corresponding amino carbonyl compounds has been achieved by using 2-azaadamantane N-oxyl (AZADO)/copper catalysis. This catalytic system oxidizes not only alcohols with tertiary amino groups but also those with secondary and primary amines in good to high yield at ambient temperature in air. bpy=2,2-bipyridyl, DMAP=4-(N,N-dimethylamino)pyridine.
- Sasano, Yusuke,Nagasawa, Shota,Yamazaki, Mai,Shibuya, Masatoshi,Park, Jaiwook,Iwabuchi, Yoshiharu
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p. 3236 - 3240
(2014/04/03)
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- 10-Substituted benzo[b][1,6]naphthyridines as inhibitors of interleukin 1
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There is disclosed a method for the treatment of inflammatory conditions and of collagenase-induced tissue destruction which comprises the administration of a therapeutically effective amount of a compound of the formula STR1 wherein R 1 is lower alkyl or lower alkenyl or any of the foregoing optionally substituted with fluoro, carboxy, lower alkoxycarbonyl, OR 2, N(R 2) 2, SR 2 CON(R 2) 2, SO 2 R 2, cyano, nitro or trifluoromethyl;R 2 is hydrogen, lower alkyl or phenyl;R 3 is halo, morpholino, 4-methylpiperazino, R 4 NNHR 5, NR 4 R 5, OR 5, SR 5, STR2 R 4 is hydrogen or lower alkyl; R 5 is hydrogen, lower alkyl, lower alkanoyl, lower cycloalkyl or phenyl; andR 6 and R 7 are each independently, hydrogen, halo, nitro, lower alkoxy, lower alkyl or trifluoromethyl;which compounds, by virtue of their ability to inhibit interleukin 1, are useful as antiinflammatory agents and in treatment of disease states involving enzymatic tissue destruction, and are also intermediates in the preparation of other compounds which possess identical activities.
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