- Palladium-catalyzed coupling reaction of amino acids (esters) with aryl bromides and chlorides
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The bulky and electron-rich MOP type ligands and Pd(dba)2 combinations showed high efficiency for the coupling reactions of amino acids and inactive aryl halides to give N-aryl amino acids. Under the catalytic conditions, not only α-amino acids, but also β-, γ-, and δ-amino acids have been coupled with aryl chlorides in moderate to high yields; in the case of optically pure β-amino acids as substrates, the optical purities of the coupling products retained.
- Ma, Fangfang,Xie, Xiaomin,Ding, Lina,Gao, Jinsheng,Zhang, Zhaoguo
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experimental part
p. 9405 - 9410
(2011/12/14)
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- Tetrahydroquinoline derivatives as CRTH2 antagonists
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A series of tetrahydroquinoline-derived inhibitors of the CRTH2 receptor was discovered by a high throughput screen. Optimization of these compounds for potency and pharmacokinetic properties led to the discovery of potent and orally bioavailable CRTH2 an
- Liu, Jiwen,Wang, Yingcai,Sun, Ying,Marshall, Derek,Miao, Shichang,Tonn, George,Anders, Penny,Tocker, Joel,Tang, H. Lucy,Medina, Julio
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scheme or table
p. 6840 - 6844
(2010/05/19)
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- Method of hydroaminating N-alkenoylcarbamates with primary aromatic amines
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The invention provides methods for hydroaminating N-alkenoyl carbamates with aromatic amines.
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Page/Page column 4
(2008/06/13)
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- Palladium-catalysed enantioselective conjugate addition of aromatic amines to α,β-unsaturated N-imides. Effect of the chelating moiety
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Palladium-catalysed enantioselective additions of aromatic amines to α,β-unsaturated N-imides 4-6 are reported. The N-substituent of the Michael acceptor appears to have an unusual modulating effect on the amine activity. The effects of introducing differ
- Pim, Huat Phua,De Vries, Johannes G.,King, Kuok Hii
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p. 1775 - 1780
(2007/10/03)
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- Amine-salt-controlled, catalytic asymmetric conjugate addition of various amines and asymmetric protonation
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Matrix presented. The combined use of chiral Pd complex 2 and amine salt enabled completely regulated release of free nucleophilic amine. Under these conditions, an efficient catalytic asymmetric conjugate addition of various amines was achieved to afford
- Hamashima, Yoshitaka,Somei, Hidenori,Shimura, Yuta,Tamura, Toshihiro,Sodeoka, Mikiko
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p. 1861 - 1864
(2007/10/03)
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- Asymmetric synthesis of β-amino acid and amide derivatives by catalytic conjugate addition of aromatic amines to N-alkenoylcarbamates
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We report a highly active palladium catalyst for the enantioselective conjugate addition of primary aromatic amines to N-alkenoylcarbamates, furnishing β-amino N-Boc-amides in extremely high yields (>99%) and unprecedented optical purity (>99% ee) with just 2 mol % catalyst loading. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2004.
- Li, Kelin,Cheng, Xiaohui,Hii, King Kuok
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p. 959 - 964
(2007/10/03)
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- Pd/Cu-catalyzed couplings of β-amino esters with aryl bromides. Synthesis of chiral 1,2,3,4-tetrahydro-4-oxo-2-alkyl-1-quinolines
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A new protocol to prepare chiral 1,2,3,4-tetrahydro-4-oxo-2-alkyl-l- quinolines has been developed. The key steps are Pd/Cu-catalyzed couplings of chiral β-amino esters and aryl bromides, and intramolecular acylation.
- Ma, Dawei,Jiang, Jiqing
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p. 1137 - 1142
(2007/10/03)
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