95656-97-6Relevant academic research and scientific papers
QUINOLINE AND QUINOXALINE DERIVATIVES AS INHIBITORS OF KINASE ENZYMATIC ACTIVITY
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, (2008/06/13)
Compounds of formula (IA) or (IB), are inhibitors of aurora kinase activity: Formula (IA), (IB) wherein -L1Y1-[CH2]z- is a linker radical wherein Y1, L1 and z are as defined in the claims; R6 is C1-C4alkoxy, hydrogen or halo; W represents a bond, -CH2-, -O-, -S-, -S(=O)2-, or -NR5- where R5 is hydrogen or C1-C4 alkyl; Q is =N-, =CH- or =C(X1)- wherein X1 is cyano, cyclopropyl or halo; linker radicals L2 are as defined in the claims; R is a radical of formula (X) or (Y): wherein R1 is a carboxylic acid group (-COOH), or an ester group which is hydrolysable by one or more intracellular carboxylesterase enzymes to a carboxylic acid group; R4 is hydrogen; or optionally substituted C1-C6 alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, heteroaryl(C1-C6 alkyl)-, -(C=O)R3, -(C=O)OR3, or -(C=O)NR3 wherein R3 is hydrogen or optionally substituted (C1-C6)alkyl, C3-C7 cycloalkyl, aryl, aryl(C1-C6 alkyl)-, heteroaryl, or heteroaryl(C1-C6 alkyl)-; R41 is hydrogen or optionally substituted C1-C6 alkyl; and D is a monocyclic heterocyclic ring of 5 or 6 ring atoms.
Synthesis of a cyclen-functionalized α-amino acid and its incorporation into peptide sequence
Chen, Shan-Yong,Huang, Yu,Zhang, Guo-Lin,Cheng, Hua,Xia, Chuan-Qin,Ma, Li-Jian,Yu, Hong,Yu, Xiao-Qi
, p. 888 - 892 (2007/10/03)
A cyclen-functionlized α-amino acid was obtained through embedding cyclen into the side chain of homoserine. The α-amino acid can be conveniently incorporated into peptide sequence to form new ligands, which have strong coordination ability for transition metal ions. Georg Thieme Verlag Stuttgart.
Side chain homologation of alanyl peptide nucleic acids: Pairing selectivity and stacking
Diederichsen, Ulf,Weicherding, Daniel,Diezemann, Nicola
, p. 1058 - 1066 (2007/10/03)
Alanyl peptide nucleic acids (alanyl-PNAs) are oligomers based on a regular peptide backbone with alternating configuration of the amino acids. All side chains are modified by covalently linked nucleobases. Alanyl-PNAs form very rigid, well defined, and l
Synthesis of orthogonally protected L-homocysteine and L-2-amino-4-phophonobutanoic acid from L-homoserine
Nair,Lee,Hangauer
, p. 810 - 814 (2007/10/02)
Convenient syntheses of N-tert-butoxycarbonyl-S-p-methoxybenzyl-L-homocysteine benzyl ester and benzyl L-4-dimethylphosphono-2-N-phthalimidobutanoate from commercially available L-homoserine are described along with their incorporation into dipeptides.
Synthesis of N-Boc-α-Amino Acids with Nucleobase Residues as Building Blocks for the Preparation of Chiral PNA (Peptidic Nucleic Acids).
Lenzi, Alessandro,Reginato, Gianna,Taddei, Maurizio
, p. 1713 - 1716 (2007/10/02)
N-Boc-Glutamic acid α-benzyl ester was transformed into 4-bromo-2-(tert-butoxycarbonylamino)-butyric acid benzyl ester using the Barton-Crich protocol.This bromo derivative undergoes nucleophilic substitution with nucleobases to give optically active N-Bo
A New Synthesis of Coprine and O-Ethylcoprine
Kienzler, Thomas,Strazewski, Peter,Tamm, Christoph
, p. 1078 - 1084 (2007/10/02)
Coprine (1), a toxine of the mushroom Coprinus atramentarius, was synthesized starting from the 2-amino- and 1-carboxy-protected L-glutamic acids 4 and 12.Compound 4 was first decarboxylated by radical chain reaction to bromide 5 which underwent ring closure to cyclopropanecarboxylate 6 on treatment with NaH (Scheme 1).Subsequent oxidative electrolysis of 7 to form tert-butyl N-(1-ethoxycyclopropyl)carbamate (8) and acidic hydrolysis yielded the 1-aminocyclopropanol hydrochloride (9).Selective cleavage of the amino-protecting group of 8(-> 10 or 11), coupling of the corresponding amine 13 with L-glutamic acid 12, and acidic hydrolysis of the resulting L-glutamine derivative 17 yielded O-ethylcoprine (3) and coprine (1).
MANIPULATION OF THE CARBOXYL GROUPS OF α-AMINO-ACIDS AND PEPTIDES USING RADICAL CHEMISTRY BASED ON ESTERS OF N-HYDROXY-2-THIOPYRIDONE
Barton, Derek H. R.,Herve, Yolande,Potier, Pierre,Thierry, Josiane
, p. 5479 - 5486 (2007/10/02)
Photolysis of α-amino-acid or peptide esters derived from N-hydroxy-2-thiopyridone in the presence of t-butylthiol affords the expected decarboxylation products in good yield.The reaction can be applied to the α-carboxyl or to the side chain carboxyl of g
CONCISE SYNTHESES OF L-SELENOMETHIONINE AND OF L-SELENOCYSTINE USING RADICAL CHAIN REACTIONS
Barton, Derek H. R.,Bridon, Dominique,Herve, Yolande,Potier, Pierre,Thierry, Josiane,Zard, Samir Z.
, p. 4983 - 4990 (2007/10/02)
L-Selenomethionine and L-selenocystine were prepared in high overall yields from protected L-glutamic and L-aspartic acid derivatives respectively.Irradiation of the mixed anhydrides (esters) derived from 4 (e.g. 15) in the presence of dimethyldiselenide provided the protected L-selenomethionine 16 directly.We have shown that triselenocyanide Se3(CN)2 can serve as an efficient selenocyanating agent for radicals; the selenocyanide group is a good precursor for the diselenide moiety of L-selenocystine.
THE FREE RADICAL CHEMISTRY OF CARBOXYLIC ESTERS OF 2-SELENOPYRIDINE-N-OXIDE: A CONVENIENT SYNTHESIS OF (L)-VINYLGLYCINE
Barton, Derek H. R.,Crich, David,Herve, Yolande,Potier, Pierre,Thierry, Josiane
, p. 4347 - 4358 (2007/10/02)
Optically pure (L)-vinylglycine has been synthesised by two different methods.The first of these involves protected (L)-glutamate esters of N-hydroxy-2-seleno-pyridine.Such esters are shown to undergo the same decarboxylative rearrangement as their thio-a
