1100575-44-7Relevant academic research and scientific papers
Native Amine-Directed ortho -C-H Halogenation and Acetoxylation /Condensation of Benzylamines
Chand-Thakuri, Pratibha,Alahakoon, Indunil,Liu, Daniel,Kapoor, Mohit,Kennedy, John F.,Jenkins, Kenneth W.,Rabon, Allison M.,Young, Michael C.
, p. 341 - 354 (2021/10/07)
Free or unfunctionalized benzylamines are well known to participate in C-H activation in the presence of palladium salts. Despite the ease with which these complexes can be activated, subsequent functionalization of the dimeric cyclometalates can be chall
Transaminases applied to the synthesis of high added-value enantiopure amines
Paul, Caroline E.,Rodriguez-Mata, Maria,Busto, Eduardo,Lavandera, Ivan,Gotor-Fernandez, Vicente,Gotor, Vicente,Garcia-Cerrada, Susana,Mendiola, Javier,De Frutos, Oscar,Collado, Ivan
supporting information, p. 788 - 792 (2014/07/08)
Critical parameters affecting the stereoselective amination of (hetero)aromatic ketones using transaminases have been studied, such as temperature, pH, substrate concentration, cosolvent, and source and percentage of amino donor, to further optimize the production of enantiopure amines using both (S)- and (R)-selective biocatalysts from commercial suppliers. Interesting enantiopure amino building blocks have been obtained, overcoming some limitations of traditional chemical synthetic methods. Representative processes were scaled up, affording halogenated and heteroaromatic amines in enantiomerically pure form and good isolated yields.
Structure-activity relationship study of [1,2,3]thiadiazole necroptosis inhibitors
Teng, Xin,Keys, Heather,Jeevanandam, Arumugasamy,Porco Jr., John A.,Degterev, Alexei,Yuan, Junying,Cuny, Gregory D.
, p. 6836 - 6840 (2008/03/14)
Necroptosis is a regulated caspase-independent cell death mechanism that results in morphological features resembling non-regulated necrosis. This form of cell death can be induced in an array of cell types in apoptotic deficient conditions with death receptor family ligands. A series of [1,2,3]thiadiazole benzylamides was found to be potent necroptosis inhibitors (called necrostatins). A structure-activity relationship study revealed that small cyclic alkyl groups (i.e. cyclopropyl) and 2,6-dihalobenzylamides at the 4- and 5-positions of the [1,2,3]thiadiazole, respectively, were optimal. In addition, when a small alkyl group (i.e. methyl) was present on the benzylic position all the necroptosis inhibitory activity resided with the (S)-enantiomer. Finally, replacement of the [1,2,3]thiadiazole with a variety of thiophene derivatives was tolerated, although some erosion of potency was observed.
