- HETEROCYCLIC AMIDES AS KINASE INHIBITORS
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Disclosed are compounds having the formula (I) wherein X, Y, Z1, Z2, Z3, Z4, R5, RA, m, A. L, and B are as defined herein, and methods of making and using the same.
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Page/Page column 68
(2014/09/03)
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- Practical synthesis of (-)-α-aminobenzolactam via nitration-cyclization of L-homophenylalanine ethyl ester
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A practical synthesis of chiral (-)-α-aminobenzolactam (2) is described. The target compound (2) was prepared from commercially available L-homophenylalanine ethyl ester hydrochloride (LHPE-HCl 1) with a highly enantiomeric purity (>98% e.e.) by employing
- Y.U., Luoting,Huang, Jiling,Chang, Ching-Yao,Yang, Teng-Kuei
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p. 323 - 330
(2008/02/09)
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- Synthesis of optically active α-aminobenzolactam via an oxidative-cyclization reaction
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A convergent pathway for the asymmetric synthesis of (-)-α-aminobenzolactam 1 is described. For the first time, the key intermediate N-methoxybenzolactam 8 was prepared from L-homophenylalanine ethyl ester hydrochloride (LHPE·HCl) 5 by employing an oxidat
- Chang, Ching-Yao,Yang, Teng-Kuei
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p. 2081 - 2085
(2007/10/03)
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- Concise Synthesis of Enantiomerically Pure Phenylalanine, Homophenylalanine, and Bishomophenylalanine Derivatives Using Organozinc Chemistry: NMR Studies of Amino Acid-Derived Organozinc Reagents
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Protected phenylalanines 23 (seven examples), homophenylalanines 7 (eight examples), and bishomophenylalanines 8 (seven examples) have been prepared by palladium-catalyzed coupling of the amino acid-derived organozinc reagents 13, 5, and 6, respectively, with aryl iodides. While the reactions of the zinc reagent 13 may be conducted in both THF and DMF as solvent, the results obtained in DMF are generally superior. In the case of the reagents 5 and 6 the results are far superior in DMF. NMR investigations on the structure of the zinc reagents 13 in THF suggest that there is strong intramolecular coordination of the urethane carbonyl group, whereas in DMF this interaction is completely suppressed.
- Jackson, Richard F. W.,Moore, Rebecca J.,Dexter, Charles S.,Elliott, Jason,Mowbray, Charles E.
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p. 7875 - 7884
(2007/10/03)
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- A novel 3-substituted benzazepinone growth hormone secretagogue (L- 692,429)
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The 3-substituted benzazepinone, L-692,429 (compound 1), is the prototype compound of a novel class of compounds that stimulate release of growth hormone (GH). The molecule evolved from efforts to identify a non-peptide mimic of the growth hormone-releasing hexapeptide, GHRP-6. Compound 1 is prepared by sequential attachment of dimethyl-β-alanine and 2'- biphenylyltetrazole side chains to a chiral 3-aminobenzolactam nucleus. Comparison of the biological activity of 1 with the corresponding six- and eight-membered lactam analogs shows the seven-membered benzazepinone skeleton to be preferred. Molecular modeling of the structurally diverse GH secretagogues, L-692,429 and GHRP-6, was performed.
- Schoen,Pisano,Prendergast,Wyvratt Jr.,Fisher,Cheng,Chan,Butler,Smith,Ball
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p. 897 - 906
(2007/10/02)
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- An Efficient Asymmetric Synthesis of (R)-3-Amino-2,3,4,5-tetrahydro-1H-benzazepin-2-one
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Two approaches for the asymmetric preparation of (-)- or (+)-α-aminobenzlactam 1 are described.One route is based on the asymmetric hydrogenation of enamide 5 and the other on the racemization/resolution of (+/-)-1.
- Armstrong, Joseph D. III,Eng, Kan K.,Keller, Jennifer L.,Purick, Robert M.,Hartner, Frederick W. Jr.,et al.
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p. 3239 - 3242
(2007/10/02)
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