106718-56-3Relevant academic research and scientific papers
Expeditious synthesis of ivacaftor
He, Yang,Xu, Qien,Ma, Wenpeng,Zhang, Jian,Sun, Hongbing,Shen, Jingshan
, p. 1035 - 1040 (2014)
An expeditious synthesis for Ivacaftor featuring modified Leimgruber-Batcho procedure was described. The overall yield is 39% over six steps from commercially available 2-nitrobenzoyl chloride.
Synthesis and cytotoxic activity of 2,5-disubstituted pyrimido[5,4-c] quinoline derivatives
Zhang, Fan,Zhai, Xin,Chen, Li Juan,Qi, Jian Guo,Cui, Bo,Gu, Yu Cheng,Gong, Ping
scheme or table, p. 1277 - 1280 (2012/01/06)
A series of 2,5-disubstituted pyrimido[5,4-c]quinoline derivatives were synthesized and their cytotoxic activity against H460, HT-29 and MDA-MB-231 cell lines was evaluated in vitro. It was found that most of the tested compounds especially compound 17, s
2-arylquinolines and process for producing the same
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, (2008/06/13)
2-Arylquinolines represented by formula (1): STR1 wherein R 1, R 3 to R 9 each represents hydrogen, halogen, lower alkyl, cyclic lower alkyl, aryl, aralkyl, alkoxy or --C m F 2m+1 ; R 2 represents hydrogen, halogen, lower alkyl, cyclic lower alkyl, aryl,
Tricyclic dicarbonyl derivatives
-
, (2008/06/13)
Compounds of general formula (Ia), (Ib) and (II), wherein R1 and R2 each independently signify hydrogen, lower alkyl, lower alkoxy, nitro, trifluoromethyl, amino, halogen, cyano or R3 R4 NS(O)2 -- and R3 and R4 signify lower alkyl, and R2 can additionally signify morpholino or thiomorpholino, a 5- or 6-membered heterocycle with 1-3N atoms optionally substituted by lower alkyl, hydroxy, amino or the group --CH2 NHCH3, a bicyclic heterocycle with 1-3N atoms or a group --NR5 R6 or --OR5 in which R5 and R6 can be the same or different and signify hydrogen, lower alkyl, hydroxy-lower alkyl, lower alkoxy-lower alkyl, amino-lower alkyl or lower alkylamino-lower alkyl, and X in formula (II) signifies --CH=CH--, --CH=N--, --NH--, --CO-- or --O--, as well as pharmaceutically usable salts of compounds of general formula (Ia), (Ib) and (II). They can be used for the treatment or prevention of illnesses, especially for the treatment or prevention of ischemia, hypoglycaemia, hypoxia, cerebral vascular spasms, spasticity, trauma, hemorrhagia, infection (viral, bacterial, amoebic, prional), epileptic seizures, autoimmune diseases, withdrawal symptoms, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's disease, intoxications, olivoponto-cerebellar atrophy, spinal cord injuries, schizophrenia, depressions, anxiety states, dependence, pains,autism and mental retardation.
2,2-Disubstituted-1,2-dihydro-3H-indol-3-ones by Base- and Thermal-induced Cyclisations of o-Azidophenyl s-Alkyl Ketones and o-Azidobenzoyl Esters
Azadi-Ardakani, Manouchehr,Alkhader, Mohamed A.,Lippiatt, John H.,Patel, Dalpat I.,Smalley, Robert K.,Higson, Susan
, p. 1107 - 1112 (2007/10/02)
o-Azidophenyl s-alkyl ketones in ethanolic potassium hydroxide at room temperature undergo loss of nitrogen and cyclisation to 2,2-dialkyl-1,2-dihydro-3H-indol-3-ones in high yield.Kinetic data (E(act.) 62.4 and 71.6 kJ mol-1, respectively) obtained for the o-azidophenylisopropyl and o-azidophenylcyclohexyl ketones support an assisted nitrogen loss from the azide via the enolate ion, rather than a nitrene reaction. 1,2-Dihydro-3H-indol-3-ones, along with in some cases 2,1-benzisoxazoles, have been obtained by the thermolysis and spray vacuum pyrolysis of other o-azidophenyl alkyl ketones, diethyl o-azidobenzoyl malonate, and ethyl o- azidobenzoyl(phenyl)acetate.
