- Synthesis of N-Glycosyl-2-oxindoles by Pd-Catalyzed N-Arylation of 1-Amidosugars
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An efficient intramolecular Pd-catalyzed N-arylation of o-iodo-amidosugars for the synthesis of N-glycosylated oxindoles has been reported. The coupling reaction takes place in toluene and involves Pd(OAc)2/RuPhos catalytic systems in the presence of K2CO3. This versatile approach was extended successfully to the synthesis of other N-glycosylated heterocycles.
- Letribot, Boris,Redjdal, Wafa,Redjdal, Wafa,Benmerad, Belkacem,Le Bideau, Franck,Alami, Mouad,Messaoudi, Samir
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supporting information
p. 4201 - 4206
(2020/06/04)
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- Palladium-Catalyzed, Norbornene-Mediated, ortho-Amination ipso-Amidation: Sequential C-N Bond Formation
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A palladium-catalyzed, norbornene-mediated ortho- and ipso-C-N bond-forming Catellani reaction is reported. This reaction proceeds through a sequential intermolecular amination followed by intramolecular cyclization of a tethered amide. The products, ortho-aminated dihydroquinolinones, were generated in moderate to good yields and are present in bioactive molecules. This work highlights the challenge of competing intra- vs intermolecular palladium-catalyzed processes.
- Whyte, Andrew,Olson, Maxwell E.,Lautens, Mark
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p. 345 - 348
(2018/01/27)
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- Methods for the treatment of hypertension
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Acetylene compounds of the formula (I): STR1 wherein Y, R1, R2, R3, and R4 are as described herein, m is 0-3, n is 0-2 and Ar is phenyl or an aromatic heterocycle are disclosed. The compounds possess antihyperte
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- Acetylene amines and their use as vasodilators and antihypertensives
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Acetylenes of the following formula (I): STR1 wherein Y, m, R1, R2, R3, n and R4 are defined herein and R5 is hydrogen, alkyl, cycloalkyl or substituted alkyl are useful vasodilators and antihypertens
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- Aralykyl (arylethynyl)aralkyl amines and their use as vasodilators and antihypertensives
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Acetylenes of the formula (I): STR1 wherein Y, m, R1, R2 q, Alk, R3, n and R4 are as defined herein and Ar1 and Ar2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias. Pharmaceutical compositions, methods of use and synthesis and novel intermediates are also part of the invention.
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- Cis & trans stilbenes and their composition for the treatment of hypertension
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Stilbenes of the formula (I): wherein Y, m, R1, R2, q, Alk, R3, n and R4 are as defined herein and Ar1 and Ar2 are aromatic, including the salts and ammonium derivatives of formula (I), in treating angina, hypertension and cardiac arrhythmias.
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