57074-96-1Relevant articles and documents
Close the ring to break the cycle: Tandem quinolone-alkyne-cyclisation gives access to tricyclic pyrrolo[1,2-: A] quinolin-5-ones with potent anti-protozoal activity
Szamosvári, Dávid,Sylvester, Kayla,Schmid, Philipp,Lu, Kuan-Yi,Derbyshire, Emily R.,B?ttcher, Thomas
supporting information, p. 7009 - 7012 (2019/06/20)
Expanding the chemical space of quinolones led to a tandem quinolone-alkyne-cyclisation reaction allowing chemoselective control of the synthesis of tricyclic pyrrolo[1,2-a]quinolin-5-ones. Importantly, we discovered anti-protozoal activity against Plasmodium and Toxoplasma with specific potency of one of the compounds against the liver stage of the malaria parasite in the nanomolar range.
The Renaissance of an Old Problem: Highly Regioselective Carboxylation of 2-Alkynyl Bromides with Carbon Dioxide
Miao, Bukeyan,Li, Gen,Ma, Shengming
supporting information, p. 17224 - 17228 (2016/01/25)
A steric effect-controlled, zinc-mediated carboxylation of different 2-alkynyl bromides under an atmospheric pressure of CO2 has been developed by careful tuning of different reaction parameters, including the metal, solvent, temperature, and additive. 2-Substituted 2,3-allenoic acids were afforded from primary 2-alkynyl bromides, whereas the carboxylation of secondary 2-alkynyl bromides yielded 3-alkynoic acids in decent yields. A rationale for the observed regioselectivity has been proposed.
