139237-78-8Relevant academic research and scientific papers
Reaction of Thiocarbonyl Fluoride Generated from Difluorocarbene with Amines
Yu, Jiao,Lin, Jin-Hong,Xiao, Ji-Chang
supporting information, p. 16669 - 16673 (2017/12/07)
The reaction of thiocarbonyl fluoride, generated from difluorocarbene, with various amines under mild conditions is described. Secondary amines, primary amines, and o-phenylenediamines are converted to thiocarbamoyl fluorides, isothiocyanates, and difluoromethylthiolated heterocycles, respectively. Thiocarbamoyl fluorides were further transformed into trifluoromethylated amines by using a one-pot process. Thiocarbonyl fluoride is generated in situ and is rapidly fully converted in one pot under mild conditions; therefore, no special safety precautions are needed.
Thiocarbonyl Surrogate via Combination of Sulfur and Chloroform for Thiocarbamide and Oxazolidinethione Construction
Tan, Wei,Wei, Jianpeng,Jiang, Xuefeng
supporting information, p. 2166 - 2169 (2017/04/27)
An efficient and practical thiocarbonyl surrogate via combination of sulfur and chloroform has been developed. A variety of thiocarbamides and oxazolidinethiones have been established, including chiral thiourea catalysts and chiral oxazolidinethione auxiliaries with high selectivity. Meanwhile, pesticides Diafenthiuron (an acaricide), ANTU (a rodenticide), and Chloromethiuron (an insecticide) were practically synthesized through this method in gram scale. Dicholorocarbene, as the key intermediate, was further confirmed via a carbene-trapping control experiment.
Resolution of (4RS,5RS)-4,5-diphenylimidazolidine-2-thione using pentafluorophenyl active esters
Andreou, Anna,Shaye, Najla Al,Brown, Hannah,Eames, Jason
, p. 6935 - 6938 (2011/03/18)
(4RS,5RS)-4,5-Diphenylimidazolidine-2-thione is resolved efficiently by treatment with NaHMDS and an enantiomerically pure pentafluorophenyl active ester. The levels of diastereocontrol were excellent (up to 90% de).
Reversal of enantioselectivity using tethered bisguanidine catalysts in the aza-Henry reaction
Lovick, Helena M.,Michael, Forrest E.
supporting information; scheme or table, p. 1016 - 1019 (2009/05/27)
A series of chiral guanidines were synthesized and shown to efficiently catalyze the aza-Henry reaction. Modifications of the catalyst structure revealed important selectivity trends as well as an intriguing reversal in stereoselectivity with bisguanidine
Heterocyclic compounds as P2X7 ion channel blockers
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Page/Page column 28, (2010/02/10)
The present invention relates to a novel series of 4,5-diphenyl-2-amino-4,5-dihydro-imidazole derivatives of the formula II: 1 wherein R, R1, R2, R3, R4, R5, X and Y are as defined herein. This invention also relates to methods of making these compounds. The compounds of this invention are P2X7 ion channel blockers and are therefore useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases having an inflammatory component, including inflammatory bowel disease, rheumatoid arthritis and disease conditions associated with the central nervous system, such as stroke, Alzheimer''s disease, etc.
Bifunctional Chiral Auxiliaries 5: The Synthesis of 1,3-Diacylimidazolidine-2-thiones and 1,3-Diacylimidazolidin-2-ones from 1,2-Diamines
Davies, Stephen G.,Mortlock, Andrew A.
, p. 4419 - 4438 (2007/10/02)
Although 1,2-diamines fail to cyclise with urea, phosgene or 1,1'-carbonyl diimidazole, they react with carbon disulphide to give the corresponding imidazolidine-2-thiones.These undergo clean diacylation to give 1,3-diacylimidazolidine-2-thiones which are
Bifunctional chiral auxiliaries 2: The synthesis of 1,3-diacylimidazolidin-2-ones from 1,2-diamines
Davies,Mortlock
, p. 4791 - 4794 (2007/10/02)
The title compounds are readily prepared in three steps via the corresponding 1,3-diacylimidazolidine-2-thiones. The final step involves the novel use of mercury (II) acetate for the conversion of thioureas to ureas.
2,4,5-Trisubstituted imidazolines and pharmaceutical compositions containing same
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, (2008/06/13)
Compounds of the formula STR1 in which R1 and R2 independently of one another are substituted or unsubstituted aryl or hetero-aryl groups, R3 is hydrogen or lower alkyl and R4 is a substituted or unsubstituted a
