4874-17-3Relevant academic research and scientific papers
Synthesis of Ring-Opened Analogues of Oxysterol-Binding Protein-Inhibiting Piperidinyl-thiazole Fungicides
Sulzer-Mosse, Sarah,Lamberth, Clemens,Kubizna, Peter
supporting information, p. 2277 - 2280 (2017/10/06)
Novel aminoethyl-, aminopropyl-, and aminobutyl-substituted thiazole-4-carboxamides have been prepared which are ring-opened analogues of piperidinyl-thiazole fungicides. Depending of the chain length, completely different synthetic approaches had to be chosen which vary from a Sonogashira coupling with a 2-bromothiazole derivative to a thiazole ring construction from different β- and δ-amino acids.
QUINAZOLINE DERIVATIVES
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Page/Page column 151, (2008/06/13)
A quinazoline derivative of the formula (I) wherein: R1, R2, R3, R3a, R4, R5, R5a R6, R7, a, m and p are as defined in the description. Also claimed are pharmaceutical compositions containing the quinazoline derivative, the use of the quinazoline derivatives as medicaments and processes for the preparation of the quinazoline derivative. The quinazoline derivatives of formula (I), are useful in the treatment of hyperproliferative disorders such as a cancer.
Synthesis of [18F]-labeled EF3 [2-(2-nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide], a marker for PET detection of hypoxia
Josse, Olivier,Labar, Daniel,Georges, Benoit,Grégoire, Vincent,Marchand-Brynaert, Jacqueline
, p. 665 - 675 (2007/10/03)
[18F]-2-(2-Nitroimidazol-1-yl)-N-(3,3,3-trifluoropropyl)-acetamide ([18F]-EF3) has been prepared, in 65% chemical yield and 5% radiochemical yield, by coupling 2,3,5,6-tetrafluorophenyl 2-(2-nitroimidazol-1-yl) acetate 1 with [18F]-3,3,3-trifluoropropylamine 7. This original radiolabelled key-synthon was obtained in 40% overall chemical yield by oxidative [18F]-fluorodesulfurization of ethyl N-phthalimido-3-aminopropane dithioate 4, followed by deprotection with hydrazine of the resulting [18F]-N-phthalimido-3,3,3-trifluoropropylamine 5. All the process was performed within 90min, from the [18F]-HF production in the cyclotron to the purification of the final target. Copyright
2-Substituted Penems with Amino Acid-Related Side Chains: Synthesis and Antibacterial Activity of a New Series of β-Lactam Antibiotics
Altamura, Maria,Perrotta, Enzo,Sbraci, Piero,Pestellini, Vittorio,Arcamone, Federico,et al.
, p. 4244 - 4256 (2007/10/03)
A new series of 6-(hydroxyethyl)penems 2-substituted with amino acid-related side chains was synthesized.The nature of the amino acyl derivative proved to be crucial both from a synthetic point of view, as β-lactam ring opening can compete with C-2 nucleophilic substitution, and for antibacterial activity.Primary amino acid amides emerged as the most suitable side chains for enhancing permeability through a Gram-negative outer membrane.In vitro activity of the new 2-penems 3a-u was influenced by the nature and position of the amide moiety, the ring size for cyclic amides, and the configuration of the amino acid.Compounds bearing amides derived from small N-methyl amino acids (such as 3a) or from cyclic amino acids (such as prolinamide 3p and 4-hydroxyprolinamide 3r) showed broad spectrum in vitro activity against both Gram-positive and Gram-negative microorganisms.
