98215-75-9Relevant academic research and scientific papers
Synthesis and spectral properties of 6,7-dimethoxy-1-[(ortho; and para-R)-phenyl]-3,4-dihydroisoquinoline
Cortes Cortes,Cortes Romero,Gutierrez Ramirez
, p. 1425 - 1427 (1994)
The preparation of eleven novel 6,7-dimethoxy-1-[(ortho, and para-R)-phenyl]-3,4-dihydroisoquinolines with possible pharmacological activity is described. The structure of all products was corroborated by ir, 1H nmr, 13C-nmr, and ms.
Enantioselective Synthesis of 1-Aryl-Substituted Tetrahydroisoquinolines Through Ru-Catalyzed Asymmetric Transfer Hydrogenation
Perez, Marc,Wu, Zi,Scalone, Michelangelo,Ayad, Tahar,Ratovelomanana-Vidal, Virginie
, p. 6503 - 6514 (2015/10/19)
A convenient and general asymmetric transfer hydrogenation of a wide array of 1-aryl-3,4-dihydroisoquinoline derivatives using a [RuIICl(η6-benzene)TsDPEN] complex in combination with a 5:2 HCOOH-Et3N azeotropic mixture as a hydrogen source was developed. Under mild reaction conditions, the described catalytic transformation secured a practical synthetic access to the corresponding valuable chiral 1-aryltetrahydroisoquinoline units with high atom economy, a broad substrate scope, high isolated yields (up to 97%) and good to excellent enantioselectivities (up to 99% ee). It was found that the stereochemical outcome of the reaction was strongly influenced by both the structure of the catalyst and the substituents present on the substrate. The synthetic utility of the present protocol has been demonstrated through the asymmetric synthesis of several biologically important alkaloids including the antiepileptic drug agent 1c, as well as (-)-nor-cryptostyline alkaloids I and II.
Synthesis and antiplasmodial activity of some 1-azabenzanthrone derivatives
Castro-Castillo, Vicente,Suárez-Rozas, Cristian,Pabón, Adriana,Pérez, Edwin G.,Cassels, Bruce K.,Blair, Silvia
supporting information, p. 327 - 329 (2013/02/23)
Some synthetic 1-azabenzanthrones (7H-dibenzo[de,h]quinolin-7-ones) are weakly to moderately cytotoxic, suggesting that they might also show antiparasitic activity. We have now tested a small collection of these compounds in vitro against a chloroquine-re
Palladium-catalyzed intramolecular C-H amidation: Synthesis and biological activities of indolobenzazocin-8-ones
Boonya-Udtayan, Sasiwadee,Ruchirawat, Somsak,Mahidol, Chulabhorn,Thasana, Nopporn,Eno, Meredith
, p. 10293 - 10301,9 (2012/12/12)
The synthesis of multi ring-fused indolobenzazocinone derivatives, an antimitotic agent, has been carried out using palladium-catalyzed C-H activation/intramolecular amidation of benzo[d]azocinones, which were synthesized by the ring annulations of dihydroisoquinolines and azlactone in refluxing acetonitrile. The target compounds, indolobenzazocin-8-one derivatives, were evaluated for their cytotoxicity against the cancer cell lines HUCCA-1, A549, HepG2, and MOLT-3. The results showed that an unsubstituted indolobenzazocin-8-one 1e exhibited very good activities in the nanomolar IC50 value range (HepG2 and MOLT-3).
Palladium-catalyzed intramolecular C-H amidation: Synthesis and biological activities of indolobenzazocin-8-ones
Boonya-Udtayan, Sasiwadee,Eno, Meredith,Ruchirawat, Somsak,Mahidol, Chulabhorn,Thasana, Nopporn
, p. 10293 - 10301 (2013/01/15)
The synthesis of multi ring-fused indolobenzazocinone derivatives, an antimitotic agent, has been carried out using palladium-catalyzed C-H activation/intramolecular amidation of benzo[d]azocinones, which were synthesized by the ring annulations of dihydroisoquinolines and azlactone in refluxing acetonitrile. The target compounds, indolobenzazocin-8-one derivatives, were evaluated for their cytotoxicity against the cancer cell lines HUCCA-1, A549, HepG2, and MOLT-3. The results showed that an unsubstituted indolobenzazocin-8-one 1e exhibited very good activities in the nanomolar IC50 value range (HepG2 and MOLT-3).
