1021389-54-7Relevant academic research and scientific papers
NOVEL IMIDAZO-PYRAZINE DERIVATIVES
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Page/Page column 45; 178-179, (2021/12/31)
The invention provides novel imidazo-pyrazine derivatives having the general formula (I), and pharmaceutically acceptable salts thereof, wherein X, m, n, and R1to R3 are as described herein: formula (I). Further provided are pharmace
Enantioselective, Catalytic Vicinal Difluorination of Alkenes
Scheidt, Felix,Sch?fer, Michael,Sarie, Jér?me C.,Daniliuc, Constantin G.,Molloy, John J.,Gilmour, Ryan
supporting information, p. 16431 - 16435 (2018/11/23)
The enantioselective, catalytic vicinal difluorination of alkenes is reported by II/IIII catalysis using a novel, C2-symmetric resorcinol derivative. Catalyst turnover via in situ generation of an ArIIIIF2 species is enabled by Selectfluor oxidation and addition of an inexpensive HF–amine complex. The HF:amine ratio employed in this process provides a handle for regioselective orthogonality as a function of Br?nsted acidity. Selectivity reversal from the 1,1-difluorination pathway (geminal) to the desired 1,2-difluorination (vicinal) is disclosed (>20:1 in both directions). Validation with electron deficient styrenes facilitates generation of chiral bioisosteres of the venerable CF3 unit that is pervasive in drug discovery (20 examples, up to 94:06 e.r.). An achiral variant of the reaction is also presented using p-TolI (up to >95 % yield).
Thermal switchability of N-chelating hoveyda-type catalyst containing a secondary amine ligand
Zukowska, Karolina,Szadkowska, Anna,Pazio, Aleksandra E.,Wo?niak, Krzysztof,Grela, Karol
experimental part, p. 462 - 469 (2012/04/23)
An investigation of aza analogues of the popular Hoveyda-Grubbs catalyst containing a secondary amine ligand is presented, proving the crucial impact of steric as well as electronic factors on the catalyst's stability and performance. The issue of latency in the reactivity profile of studied catalysts is examined, followed by structural and application studies.
Benzo-fused heterocycles and carbocycles by intramolecular SNAr and tandem SN2-SNAr reactions
Bunce, Richard A.,Nago, Takahiro,Sonobe, Nathan,Slaughter, LeGrande M.
, p. 551 - 557 (2008/09/18)
(Chemical Equation Presented) Benzo-fused heterocyclic and carbocyclic systems have been synthesized by intramolecular SNAr and tandem SN2-SNAr reactions. Treatment of 3-(2-fluoro-5- nitrophenyl)-1-propanol with sodium hydride in N,N-dimethylformamide gave 6-nitrochroman in 80% yield by an intramolecular SNAr reaction. Treatment of 2-(3-bromopropyl)-1-fluoro-4-nitrobenzene with benzylamine in N,N-dimethylformamide gave 1-benzyl-6-nitrotetrahydroquinoline in 98% yield by a tandem SN2-SNAr reaction. Finally, in a similar process, reaction of this same bromide with dimethyl malonate under basic conditions gave 1,1-bis(methoxycarbonyl)-6-nitro-1,2,3,4-tetrahydronaphthalene in 80% yield. Further studies exploring ring size effects are also presented.
SUBSTITUTED ISOQUINOLINONES
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Page/Page column 61, (2010/02/11)
Isoquinolinone compounds are provided that are useful for the inhibition of ADP-platelet aggregation, particularly in the treatment of thrombosis and thrombosis related conditions or disorders.
Organosilicon polymers, and dyes, exhibiting nonlinear optical response
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, (2008/06/13)
Organosilicon polymers, including crosslinked polymers and crosslinkable prepolymers, of cyclic polysiloxane, organic dyes, and, optionally, polyenes. The dyes include those with delocalized Pi electron systems linking electron donor groups and electron acceptor groups, and with at least two carbon-carbon double bond-containing pendant groups attached to at least two different sites from among the indicated delocalized Pi electron systems, donor groups, and acceptor groups.
