- Synthesis and biological evaluation of 3-(2-aminoethyl) uracil derivatives as gonadotropin-releasing hormone (GnRH) receptor antagonists
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We investigated a series of uracil analogues by introducing various substituents on the phenyl ring of the N-3 aminoethyl side chain and evaluated their antagonistic activity against human gonadotropin-releasing hormone (GnRH) receptors. Analogues with su
- Kim, Seon-Mi,Lee, Minhee,Lee, So Young,Lee, Soo-Min,Kim, Eun Jeong,Kim, Jae Sun,Ann, Jihyae,Lee, Jiyoun,Lee, Jeewoo
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p. 413 - 424
(2018/01/17)
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- Highly enantioselective synthesis of cyclic sulfamidates and sulfamides via rhodium-catalyzed transfer hydrogenation
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We achieved highly enantioselective synthesis of cyclic 1,2-sulfamidates and -sulfamides via rhodium-catalyzed transfer hydrogenation, and also revealed one-pot preparation of cyclic N-sulfonylimines from α-hydroxy ketones.
- Lee, Sun Ah,Kwak, Se Hun,Lee, Kee-In
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p. 2372 - 2374
(2011/03/22)
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- Approach to a better understanding and modeling of (S)-dihydrofuran-2-yl, (S)-tetrahydrofuran-2-yl-, and furan-2-yl-β-dialkylaminoethanol ligands for enantioselective alkylation
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This paper outlines our efforts to study the influence of an oxygen atom adjacent to the stereogenic center of β-aminoalcohol derivatives used as ligands for catalysts in the asymmetric alkylation of aldehydes. Thirty-four enantiomerically pure (S)-dihydrofuran-2-yl, (S)-tetrahydrofuran-2-yl-, and furan-2-yl-β-dialkylamino alcohols have been prepared from 1,4:3,6-dianhydromannitol, 1,4:3,6-dianhydrosorbitol, and aminoacids, and then have been evaluated as ligands for the enantioselective addition of diethylzinc to benzaldehyde. Attention has been focused on the structural features governing the extent of chiral induction, the reaction rate, and the chemical yield of 1-phenyl-1-propanol which has been promoted by this wide collection of β-dialkylamino alcohols.
- Paolucci, Claudio,Rosini, Goffredo
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p. 2923 - 2946
(2008/09/17)
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- Preparation of enantiomerically pure 2-(1′-aminomethyl)furan derivatives and synthesis of an unnatural polyhydroxylated piperidine
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Zinc-mediated propargylation of α-acylaminoaldehydes, and subsequent oxidative isomerization followed by Ag(I)-catalyzed cycloisomerization conveniently provides a new enantioselective route to the corresponding 2-aminoalkylfurans. One of these furans was
- Cong, Xin,Liu, Ke-Gang,Liao, Qing-Jiang,Yao, Zhu-Jun
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p. 8567 - 8571
(2007/10/03)
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- Enantioselective synthesis of both enantiomers of 2-amino-2-(2-furyl)ethan-1-ol as a flexible building block for the preparation of serine and azasugars
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The selective conversion of 1-(2-furyl)-2-hydroxyethan-1-one and ethyl 2-(2-furyl)-2-oxo acetate into (E)- and (Z)-oximes and oxime ethers followed by oxazaborolidine-catalyzed enantioselective reduction using different amino alcohols furnished both enantiomers of the important chiral building block 2-amino-2-(2-furyl)ethan-1-ol with an ee of up to 96%.
- Demir, Ayhan S.,Sesenoglu, Oezge,Aksoy-Cam, Hilal,Kaya, Handan,Aydogan, Kenan
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p. 1335 - 1340
(2007/10/03)
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