- CHIRAL INDOLE COMPOUNDS AND THEIR USE
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The present disclosure relates to indole compounds of Structural Formula 2 and pharmaceutical compositions thereof, and their use in stimulating the immune system of patients in need thereof and in treating cancer. Formula (II)
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Paragraph 00238; 00239
(2020/10/28)
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- Cyanocuprates convert carboxylic acids directly into ketones
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Carboxylic acids were converted directly in 56-99% yields into methyl, n-butyl, and isopropyl ketones using excess cyanocuprates R2CuLi 3 LiCN. A substrate with a stereocenter α to the carboxylic acid was converted into ketones with very little loss of enantiomeric purity. A variety of functional groups were tolerated including aryl bromides. This direct transformation of a carboxylic acid into ketone with minimal tertiary alcohol formation is proposed to involve a relatively stable copper ketal tetrahedral intermediate.
- Genna, Douglas T.,Posner, Gary H.
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supporting information; experimental part
p. 5358 - 5361
(2011/12/15)
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- SELECTIVE AZOLE PDE10A INHIBITOR COMPOUNDS
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The invention pertains to heteroaromatic compounds of the formula I, as defined herein, that serve as effective phosphodiesterase (PDE) inhibitors. In particular, the invention relates to said compounds which are selective inhibitors of PDE10. The invention also relates to pharmaceutical compositions comprising said compounds; and the use of said compounds in a method for treating certain central nervous system (CNS) or other disorders.
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Page/Page column 161-162
(2010/11/29)
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- Kinetics of the Enolisation Reactions of 2-Acetylpyrrole and of 2-, 4- and 5-Acetylthiazoles
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Kinetic results are reported on the rates of enolisation of title compounds in water, in acetate buffers, in dilute hydrochloric acid, in dilute sodium hydroxide solutions and in the presence of several metal-ion salts, as measured by their rates of halogenation at 25 deg C.The results have been compared with those previously obtained from the corresponding reactions of acetophenone and a number of acetylheterocycles.It is shown that a suitable metal cation (e.g., Cu2+) can be hundreds of times more effective than the proton in catalysing the enolisation process of an acetylheterocyclic compound.This can be due either to the 'soft' character of the acetyl group, as, for example, that of 2-acetylpyrrole, or to coordination of both the carbonyl oxygen and the heteroatom by the metal cation in the transition state of the reaction, as for 2- and 4-acetylthiazoles.
- Maria, Paolo De,Fontana, Antonella,Arlotta, Marialuisa,Chimichi, Stefano,Spinelli, Domenico
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p. 415 - 420
(2007/10/02)
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