29753-99-9Relevant academic research and scientific papers
Cyanide ion promoted addition of acyl phosphonates to ethyl cyanoformate: Synthesis of tertiary carbinols via tandem carbon-carbon bond formations
Demir, Ayhan S.,Reis, Barbaros,Reis, Oemer,Eymuer, Serkan,Goellue, Mehmet,Tural, Servet,Saglam, Gueluezar
, p. 7439 - 7442 (2008/02/11)
(Chemical Equation Presented) New cyanation/phosphonate-phosphate rearrangement/C-acylation reactions of cyanophosphate anion with cyanoformate esters are described. Phase-transfer cocatalysts facilitate cyanide-catalyzed reactions between acyl phosphonates and cyanoformates to afford protected tertiary carbinol products in good to excellent yields (74-95%). Ethyl cyanoformate is used as a cyanide source and electrophile. The scope of the reaction was investigated by using a number of benzoyl and acyl phosphonates along with ethyl cyanoformate. Representative chemoselective reduction of the product 5a afforded ethyl 3-amino-2-hydroxy-2-phenylpropanoate (13) in good yield.
PYRIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Page/Page column 37, (2010/02/10)
Pyridylpyrrole derivatives of formula (I) and pharmaceutically acceptable salts thereof, as defined in the specification, and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treat
PYRIMIDYLPYRROLE DERIVATIVES ACTIVE AS KINASE INHIBITORS
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Page/Page column 28, (2010/02/10)
Pyrimidylpyrrole derivatives of formula (1) and pharmaceutically acceptable salts thereof, as defined in the specification, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be
Rationally designed 'dipeptoid' analogues of cholecystokinin (CCK): C-terminal structure-activity relationships of α-methyl tryptophan derivatives
Boden, P. R.,Eden, J. M.,Higginbottom, M.,Hill, D. R.,Horwell, D. C.,et al.
, p. 47 - 61 (2007/10/02)
This paper outlines the synthesis and C-terminal structure-activity relationships (SAR) of a series of α-methyl tryptophanylphenethylamide analogues of the neuropeptide cholecystokinin (CCK).CCK-B and CCK-A receptor binding affinities of these analogues are described and the contributions of the various side chains on the phenethylamide moiety to binding affinity are discussed.Several of the compounds prepared have CCK-B receptor binding affinities similar to that found with the endogenous neuropeptide CCK-26-33 (sulphated) (CCK-B, IC50 = 0.3 nM) and are highly selective over the CCK-A receptor.Amongst the most potent of the compounds synthesized are *,S*)>-β-3,7>dec-2-yloxy)carbonyl>amino>propyl>amino>benzenebutanoic acid 22, *,S*)>-3,7>dec-2-yloxy)carbonyl>amino>propyl>amino>-3-phenylpropyl>thio>acetic acid 28a and *,S*)>-3,7>dec-2-yloxy)carbonyl>amino>propyl>amino>-3-phenylpropyl>sulfonyl>acetic acid 32 which have CCK-B receptor binding affinities of IC50 = 0.3, 0.3 and 0.2 nM with CCK-A/B ratios of 220, 700 and 1000, respectively.CCK-B receptor selective ligands, 22, 28a and 32 were also shown to be potent anatagonists in blocking pentagastrin-evoked excitation in neurons of the rat hypothalamic ventro-medial nucleus (VMN) with the Ke values of 2.8, 23 and 5.9 nM, respectively. Keywords: cholecystokinin / dipeptoid analogues / structure-affinity relationships / α-methyl-tryptophan derivatives / C-terminal
