564441-49-2Relevant academic research and scientific papers
Synthesis of Indole-2-carboxylate Derivatives via Palladium-Catalyzed Aerobic Amination of Aryl C-H Bonds
Clagg, Kyle,Hou, Haiyun,Weinstein, Adam B.,Russell, David,Stahl, Shannon S.,Koenig, Stefan G.
supporting information, p. 3586 - 3589 (2016/08/16)
A direct oxidative C-H amination affording 1-acetyl indolecarboxylates starting from 2-acetamido-3-arylacrylates has been achieved. Indole-2-carboxylates can be targeted with a straightforward deacetylation of the initial reaction products. The C-H amination reaction is carried out using a catalytic Pd(II) source with oxygen as the terminal oxidant. The scope and application of this chemistry is demonstrated with good to high yields for numerous electron-rich and electron-poor substrates. Further reaction of selected products via Suzuki arylation and deacetylation provides access to highly functionalized indole structures.
Synthesis and activity of novel analogs of hemiasterlin as inhibitors of tubulin polymerization: Modification of the a segment
Yamashita, Ayako,Norton, Emily B.,Kaplan, Joshua A.,Niu, Chuan,Loganzo, Frank,Hernandez, Richard,Beyer, Carl F.,Annable, Tami,Musto, Sylvia,Discafani, Carolyn,Zask, Arie,Ayral-Kaloustian, Semiramis
, p. 5317 - 5322 (2007/10/03)
Analogs of HTI-286 (1), containing various aromatic rings in the A segment, were synthesized as potential inhibitors of tubulin polymerization, and the structure-activity relationships related to stereo- and regio-chemical effects of substituents on the a
meta-substituent effects on the photocyclization of aryl-substituted N-acyl-α-dehydroalanine derivatives
Maekawa, Kei,Kajiwara, Hiroo,Iseya, Yoshiyuki,Igarashi, Tetsutaro,Sakurai, Tadamitsu
, p. 637 - 654 (2007/10/03)
On irradiation in methanol, the title compounds having chloro, trifluoromethyl or methyl group at the meta position on the styryl benzene ring gave 6-substituted (2) and 8-substituted (3) 1-methyl-3-(methylaminocarbonyl)isoquinolines along with 1-azetines
Potent, selective tetrahydro-β-carboline antagonists of the serotonin 2B (5HT(2B)) contractile receptor in the rat stomach fundus
Audia, James E.,Evrard, Deborah A.,Murdoch, Gwyn R.,Droste, James J.,Nissen, Jeffrey S.,Schenck, Kathy W.,Fludzinski, Pawel,Lucaites, Virginia L.,Nelson, David L.,Cohen, Marlene L.
, p. 2773 - 2780 (2007/10/03)
A series of potent, selective 5HT(2B) receptor antagonists has been identified based upon yohimbine, with SAR studies resulting in a 1000-fold increase in 5HT(2B) receptor affinity relative to the starting structure (- log K(B)s > 10.0 have been obtained). These high-affinity tetrahydro-β- carboline antagonists are able to discriminate among the 5HT2 family of serotonin receptors, with members of the series showing selectivities of more than 100-fold versus both the 5HT(2A) and 5HT(2C) receptors based upon radioligand binding and functional assays. As the first compounds reported with such selectivity and enhanced receptor affinity, these tetrahydro-β- carboline antagonists are useful tools for elucidating the role of serotonin acting at the 5HT(2B) receptor in normal and disease physiology.
