- SUBSTITUTED IMIDAZOLE CARBOXAMIDES AND THEIR USE IN THE TREATMENT OF MEDICAL DISORDERS
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The invention provides substituted imidazole carboxamides and related compounds, compositions containing such compounds, medical kits, and methods for using such compounds and compositions to treat a medical disorder, e.g., cancer, lysosomal storage disorder, neurodegenerative disorder, inflammatory disorder, in a patient.
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Paragraph 00295
(2021/04/01)
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- Palladium-catalyzed regiodivergent hydroaminocarbonylation of alkenes to primary amides with ammonium chloride
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Palladium-catalyzed hydroaminocarbonylation of alkenes for the synthesis of primary amides has long been an elusive aim. Here, we report an efficient catalytic system which enables inexpensive NH4Cl to be utilized as a practical alternative to gaseous ammonia for the palladium-catalyzed alkene-hydroaminocarbonylation reaction. Through appropriate choice of the palladium precursors and ligands, either branched or linear primary amides can be obtained in good yields with good to excellent regioselectivities. Primary mechanistic studies were conducted and disclosed that electrophilic acylpalladium species were capable of capturing the NH2-moiety from ammonium salts to form amides in the presence of CO with NMP as a base.
- Gao, Bao,Zhang, Guoying,Zhou, Xibing,Huang, Hanmin
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p. 380 - 386
(2018/01/12)
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- Primary fatty acid amide preparation method
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The present invention provides a primary fatty acid amide preparation method. According to the present invention, under the action of a single auxiliary agent phosphine-containing transition metal catalyst or a combined auxiliary agent comprising a phosphine-free transition metal catalyst and a phosphine-containing ligand, terminally substituted olefin or cyclo-olefin, carbon monoxide and an ammonium salt are subjected to a hydrogen carboamidation reaction so as to prepare the primary fatty acid amide compound in one step; the raw material and the catalyst of the reaction are inexpensive and easy to obtain, and the synthesis process is simple, such that the synthesis cost is substantially reduced; the preparation method has characteristics of mild reaction condition and high yield, and issuitable for industrial production; and the raw material and the catalyst of the reaction are clean, non-toxic and low environment pollution.
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Paragraph 0157-0159
(2018/10/19)
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- Asymmetric synthesis of α-alkylated N-sulfinyl imidates as new chiral building blocks
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(Chemical Equation Presented) α-Alkylation of N-sulfinyl imidates, prepared via condensation of tert-butanesulfinamide with ortho esters, led to α-substituted N-sulfinyl imidates in good-to-excellent diastereomeric ratios (dr up to >99:1) and yields. Depr
- Colpaert, Filip,Mangelinckx, Sven,Verniest, Guido,De Kimpe, Norbert
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p. 3792 - 3797
(2009/09/29)
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- Superacidic activation of α,β-unsaturated amides and their electrophilic reactions
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The electrophilic reactivity of α,β-unsaturated amides towards weak nucleophiles such as arenes and cyclohexane, initiated either with triflic acid (CF3SO3H) or with excess AlCl3, has been studied. The amides generally condense readily with aromatics in the presence of AlCl3 to give 3-arylpropionamides and related compounds in excellent yields, while some amides also undergo selective ionic hydrogenation with cyclohexane to give saturated amides. The proposed mechanism of these reactions involves dicationic intermediates (superelectrophiles). The direct observation of a dicationic species (by low-temperature NMR) is reported. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Koltunov, Konstantin Yu.,Walspurger, Stephane,Sommer, Jean
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p. 4039 - 4047
(2007/10/03)
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- N-acyl 'Quat' pyrrolidinone auxiliary as a chiral amide equivalent via direct aminolysis
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A novel route to chiral amides through the efficient, non-racemising, cleavage of N-acyl side chains from a 'Quat' chiral auxiliary using N-centred nucleophiles is described. The synthetic utility of the procedure is then highlighted by the preparation of a range of succinamide and succinimide derivatives and through the synthesis of the natural product (S)-(+)-amphetamine via a stereospecific Hofman type degradation using a hypervalent iodine reagent.
- Davies, Stephen G.,Dixon, Darren J.
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p. 1869 - 1876
(2007/10/03)
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- N-acyl 'Quat' pyrrolidinone auxiliary as a chiral amide equivalent via direct aminolysis
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A novel route into chiral amides is achieved through the efficient, non-racemising, cleavage of N-acyl side chains from a 'Quat' pyrrolidinone chiral auxiliary using a range of N-nucleophiles.
- Davies, Stephen G.,Dixon, Darren J.
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p. 963 - 964
(2007/10/03)
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