- 3-amino-fluorene-2,4-dicarbonitriles (AFDCs) as photocatalysts for the decarboxylative arylation of α-amino acids and α-oxy acids with arylnitriles
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1-(4-(9H-Carbazol-9-yl)phenyl)-3-amino-9H-fluorene-2,4-dicarbonitrile as a new photocatalyst for the decarboxylative cross-coupling reaction of α-amino acids or α-oxy carboxylic acids with arylnitriles is described. This light-driven reaction enables a va
- Chen, Yiyang,Lu, Ping,Wang, Yanguang
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supporting information
p. 2130 - 2133
(2019/03/26)
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- Electrophile, Substrate Functionality, and Catalyst Effects in the Synthesis of α-Mono and Di-Substituted Benzylamines via Visible-Light Photoredox Catalysis in Flow
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We report herein the facile and one-pot synthesis of α-mono- and di-substituted benzylamines from cheap and readily available α-amino acids, via photocatalytic decarboxylative arylation in flow. This enables to access intermediates and building blocks that are difficult to obtain via other synthetic routes, but are key for the manufacture of pharmaceuticals, agrochemicals, and fine chemicals. The optimal decarboxylative conditions were identified through a high-throughput evaluation of catalysts, organic or inorganic bases, ligands, and reaction parameters (i. e., contact time, temperatures, and photoelectron power). The reaction turned out to be electronically controlled as the yields increased with increasing electron-density on the aryl moiety. The results were correlated with the redox properties of the photocatalysts, deriving catalyst structure-performance relationships which can facilitate the future identification of even better materials. In addition, compared to traditional batch chemistry, the use of a flow protocol led to quicker reactions (30 min instead of 12–72 h) and ensured more predictable reaction scale-ups.
- Vilé, Gianvito,Richard-Bildstein, Sylvia,Lhuillery, Arnaud,Rueedi, Georg
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p. 3786 - 3794
(2018/08/03)
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- BENZOLACTAM COMPOUNDS AS PROTEIN KINASE INHIBITORS
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The invention provides a compound of formula (0): or a pharmaceutically acceptable salt, N-oxide or tautomer thereof. The compounds are inhibitors of ERK 1/2 kinases and will be useful in the treatment of ERKl/2-mediated conditions. The compounds are therefore useful in therapy, in particular in the treatment of cancer.
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- Decarboxylative arylation of α-Amino acids via photoredox catalysis: A one-step conversion of biomass to drug pharmacophore
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The direct decarboxylative arylation of α-amino acids has been achieved via visible light-mediated photoredox catalysis. This method offers rapid entry to prevalent benzylic amine architectures from an abundant biomass, specifically α-amino acid precursors. Significant substrate scope is observed with respect to both the amino acid and arene components.
- Zuo, Zhiwei,Macmillan, David W. C.
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supporting information
p. 5257 - 5260
(2014/05/06)
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