74998-19-9Relevant academic research and scientific papers
An Efficient Palladium-Catalyzed α-Arylation of Acetone below its Boiling Point
Ledgard, Andrew J.,Martin, Fionna M.,Mutton, Simon P.,Richardson, Jeffery,Walton, Lesley
, (2020/07/24)
The monoarylation of acetone is a powerful transformation, but is typically performed at temperatures significantly in excess of its boiling point. Conditions described for performing the reaction at ambient temperatures led to significant dehalogenation when applied to a complex aryl halide. We describe our attempts to overcome both issues in the context of our drug-discovery program.
Preparation of a highly congested carbazoyl-derived p,n-type phosphine ligand for acetone monoarylations
Fu, Wai Chung,Zhou, Zhongyuan,Kwong, Fuk Yee
, p. 1553 - 1558 (2016/06/09)
We report a newly developed carbazoyl-derived P,N-type phosphine ligand (L1) for the monoarylation of acetone with aryl chlorides. The proposed Pd(dba)2/L1 catalyst exhibited remarkable catalytic reactivity toward highly electron rich and sterically congested aryl chlorides, with catalyst loading as low as 0.1 mol % of Pd along with excellent chemoselectivity. A reaction rate study of the system using electronically diverse aryl chlorides determined the mechanisms regarding the rate-limiting steps in this reaction. The oxidative addition adduct of Pd-PhenCar-Phos with p-chlorotoluene showed the participation of N-Pd coordination in the metal complex. The isolated palladium complex C1 could be utilized as a precatalyst in the transformation and achieved performance comparable to that of the in situ generated palladium species.
THIAZOLE AND THIADIAZOLE COMPOUNDS FOR INFLAMMATION AND IMMUNE-RELATED USES
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Page/Page column 99, (2010/11/28)
The invention relates to compounds of structural formula (I) or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof, wherein R'i, X, X', L and Y are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions, allergic disorders, and immune disorders.
Phenylethanolamine derivatives as beta-2 agonists
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Page/Page column 83, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
FORMAMIDE DERIVATIVES USEFUL AS ADRENOCEPTOR
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Page/Page column 102, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Compounds for the treatment of diseases
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Page/Page column 40, (2008/06/13)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
2-(6-AMINO-PYRIDIN-3-YL)-2-HYDROXYETHYLAMINE DERIVATIVES AS BETA 2-ADRENOCEPTORS AGONISTS
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Page 159-160, (2010/02/09)
The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in
Secondary amines, their preparation and use in pharmaceutical compositions
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, (2008/06/13)
The compounds of the formula (II): STR1 and their pharmaceutically acceptable salts wherein R1 is a hydrogen, fluorine or chlorine atom or a hydroxyl, hydroxymethyl, methyl, methoxyl, amino, formamido, acetamido, methylsulphonylamido, nitro, benzyloxy, methylsulphonylmethyl, ureido, trifluoromethyl or p-methoxybenzylamino group; R2 is a hydrogen, fluorine or chlorine atom or a hydroxyl group; R3 is a hydrogen or chlorine atom or a hydroxyl group; R4 is a carboxylic acid group or a salt, ester or amide thereof; R5 is a hydrogen, chlorine or fluorine atom or a methyl, methoxyl or hydroxyl group or a carboxylic acid group or a salt, ester or amide thereof; R6 is a hydrogen atom or a methyl, or propyl group; X is an oxygen atom or a bond; and Y is an alkylene group of up to 6 carbon atoms or a bond have been found to possess anti-obesity and/or antihyperglycaemic activity.
