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FUNGAL CELL WALL SYNTHESIS GENE

A reporter system reflecting the transport process that transports GPI-anchored proteins to the cell wall was constructed and compounds inhibiting this process were discovered. Further, genes conferring resistance to the above compounds were identified and methods of screening for compounds that inhibit the activity of the proteins encoded by these genes were developed.Therefore, through the novel compounds, the present invention showed that antifungal agents having a novel mechanism, i.e. inhibiting the process that transports GPI-anchored proteins to the cell wall, could be achieved.

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The first Bischler-Napieralski cyclization in a room temperature ionic liquid

We have demonstrated the use of the room temperature ionic liquid, 1-butyl-3-methylimidazoliumhexafluorophosphate ([bmim]PF6), as an environmentally benign solvent for the preparation of isoquinoline derivatives through Bischler-Napieralski cyclization under mild conditions with excellent purity and yields. The role of HF as a catalyst in the reaction was also investigated.

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An organocatalyst bound alpha-aminoalkyl radical intermediate for controlled aerobic oxidation of iminium ions

A catalyst bound alpha-aminoalkyl radical intermediate from iminium is developed to control its formation and reactivity with aerobic oxygen. The influence of the catalyst was demonstrated via the ease of radical intermediate formation and its subsequent reactivity, including the first catalyst-controlled enantioselective aerobic oxidation with a chiral phosphite catalyst.

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Transfer hydrogenation process

A catalytic transfer hydrogenation process is provided. The catalyst employed in the process is a metal neutral hydrocarbyl complex which is coordinated to defined bidentate ligands. Preferred metals include rhodium, ruthenium and iridium. Preferred bidentate ligands are diamines and aminoalcohols, particularly those comprising chiral centers. The hydrogen donor is advantageously a mixture of triethylamine and formic acid. The process can be employed to transfer hydrogenate iminium salts, which are preferably prochiral.

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A facile, microwave-assisted, palladium-catalyzed arylation of acetone

We report an expedient method for the heteroarylation of acetone under tin-free conditions. The coupling is performed using the commercially available enol silane of acetone (2-trimethylsilyloxypropene) and a corresponding aryl bromide, chloride or triflate under microwave-assisted conditions, with tris(dibenzylideneacetone)dipalladium (Pd2(dba)3) or palladium acetate (Pd(OAc)2) and 2-(2?,6?-dimethoxybiphenyl)dicyclohexylphosphine (S-Phos) as the catalyst system.

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Isoquinoline – Wikipedia,
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SUBSTITUTED PYRIDINE DERIVATIVES AS FABI INHIBITORS

The present invention provides substituted pyridine derivatives of formula (I), which may be therapeutically useful as as anti-bacterial agents, more particulalrly FabI inhibitors. Formula (I) in which R1 to R5 and L have the meanings given in the specification, and pharmaceutically acceptable salts thereof that are useful in the treatment and prevention in diseases or disorder, in particular their use in diseases or disorder where there is an advantage anti-bacterial agents, more particularly FabI inhibitors. The present invention also provides methods for synthesizing and administering the FabI inhibitor compounds. The present invention also provides pharmaceutical formulations comprising at least one of the FabI inhibitor compounds to gether with a pharmaceutically acceptable carrier, diluent or excipient therefor

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Extracurricular laboratory:new discovery of 891782-60-8

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Asymmetric Cycloisomerization of o-Alkenyl-N-Methylanilines to Indolines by Iridium-Catalyzed C(sp3)?H Addition to Carbon?Carbon Double Bonds

Highly enantioselective cycloisomerization of N-methylanilines, bearing o-alkenyl groups, into indolines is established. An iridium catalyst bearing a bidentate chiral diphosphine effectively promotes the intramolecular addition of the C(sp3)?H bond across a carbon?carbon double bond in a highly enantioselective fashion. The reaction gives indolines bearing a quaternary stereogenic carbon center at the 3-position. The reaction mechanism involves rate-determining oxidative addition of the N-methyl C?H bond, followed by intramolecular carboiridation and subsequent reductive elimination.

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MODULATORS OF THE HISTAMINE H3 RECEPTOR AND THE TREATMENT OF DISORDERS RELATED THERETO

The present invention relates to compounds of Formula (la) and pharmaceutically acceptable salts, solvates, and hydrates thereof, that modulate the activity of the histam­ine H3 receptor. Compounds of the present invention and pharmaceutical compositions thereof are directed to methods useful in the treatment of histamine H3-associated disorders

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PYRAZOLE, ISOTHIAZOLE AND ISOXAZOLE DERIVATIVES USEFUL AS AGRICULTURAL FUNGICIDES

The present invention relates to substituted pyrazole, isoxazole andisothiazole compounds which are of use in the field of agriculture as fungicides.

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FACTOR XIIA INHIBITORS

This invention relates to compoundsof formula (I)and methods of treatment using the compounds. The invention also relates to processes and methods for producing the compounds of the invention. The compounds of the invention are modulators of Factor XII (e.g. Factor XIIa). In particular, the compounds are inhibitors of Factor XIIa and may be useful as anticoagulants.

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