1220-00-4Relevant articles and documents
New chemistry of N,N′-Bis(aryl)-ethane-1,2-diylidenediamines towards carbon disulfide and phenyl isothiocyanate
Aly, Ashraf A.,Mohamed, Nasr K.,Mourad, Aboul-Fetouh E.
, p. 1 - 10 (1999)
N,N′-Bis(aryl)-ethane-1,2-diylidenediamine (1a,b) reacts with carbon disulfide to give 5-hydroxy-2-arylamino-3N-arylamino-4H-1, 3-thiazoline-2-thione (2a,b) in addition to N-aryl-thiourea derivatives 3-5. The reaction of phenyl isothiocyanate with 1a,b pr
Trapping Reactive Intermediates by Mechanochemistry: Elusive Aryl N-Thiocarbamoylbenzotriazoles as Bench-Stable Reagents
?trukil, Vjekoslav,Gracin, Davor,Magdysyuk, Oxana V.,Dinnebier, Robert E.,Fri??ic, Tomislav
, p. 8440 - 8443 (2015)
Monitoring of mechanochemical thiocarbamoylation by in situ Raman spectroscopy revealed the formation of aryl N-thiocarbamoylbenzotriazoles, reactive intermediates deemed unisolable in solution. The first-time isolation and structural characterization of these elusive molecules demonstrates the ability of mechanochemistry to access otherwise unobtainable intermediates and offers a new range of masked isothiocyanate reagents.
Synthesis and crystal structure of N,N′-bis(4-chlorophenyl)thiourea N,N-dimethylformamide
Ajibade, Peter A.,Mbese, Johannes Z.,Odularu, Ayodele T.,Oyedeji, Opeoluwa O.,Puschmann, Horst
, p. 511 - 517 (2021)
This study is about the synthesis of N,N′-bis(4-chlorophenyl)thiourea N,N-dimethylformamide (C16H17Cl2N3OS) compound. Single crystals of the compound were obtained by slow evaporation of N,N′-bis(4-chlorophenyl)thiourea (C13H10Cl2N2S) in N,N-dimethylforma
Di-tert-butyl peroxide (DTBP)-mediated synthesis of symmetrical N,N′-disubstituted urea/thiourea motifs from isothiocyanates in water
Chen, Ling,Dong, Yibo,Wu, Yangjie,Yang, Jinchen,Zhang, Jinli
supporting information, (2021/12/01)
ABATRACT: A direct approach to N,N′-disubstituted urea/thiourea from the self-condensation reactions of isothiocyanates in water has been developed. This access tolerated a wide range of functional groups on the aromatic ring, providing a practical and environment-friendly process to N,N′-disubstituted urea/thiourea in moderate to excellent yields from safe and easily available starting materials. A plausible mechanism of the desulfurization self-condensation reaction for urea was also proposed and the role of di-tert-butyl peroxide (DTBP) and copper catalyst in the present strategy was demonstrated with the help of ESI mass spectrometry of intermediate studies.
A facile method for the preparation of carbodiimides from thioureas and (Boc)2O
Wu, He,Sun, Yan-Fang,Zhang, Chen,Miao, Chun-Bao,Yang, Hai-Tao
supporting information, p. 739 - 742 (2018/01/27)
A concise method for the preparation of carbodiimides from thioureas using di-tert-butyl dicarbonate [(Boc)2O] as the dehydrosulfurizative reagent has been developed. Using DMAP as the catalyst, a variety of symmetric and asymmetric 1,3-diaryl thioureas were converted into the corresponding carbodiimides efficiently in a short time.
Palladium catalyzed carbonylative annulation of the C(sp2)-H bond of N,1-diaryl-1H-tetrazol-5-amines and N,4-diaryl-4H-triazol-3-amines to quinazolinones
Chandrasekhar, Attoor,Ramkumar, Venkatachalam,Sankararaman, Sethuraman
supporting information, p. 8629 - 8638 (2018/12/12)
Pd(ii) catalyzed direct C-H carbonylative annulation of N,1-diaryl-1H-tetrazol-5-amines and N,4-diaryl-4H-1,2,4-triazol-3-amines gave the corresponding triazole and tetrazole fused quinazolinones in good yields. This methodology offers a convenient method for the synthesis of these important heterocyclic scaffolds in a highly atom economical process. On the mechanistic aspect weakly nucleophilic triazole and tetrazole moieties function as both directing as well as intramolecular nucleophiles. The catalytically active C-H activated intermediate dimeric Pd complex was isolated and characterized which on exposure to CO gas gave the corresponding tetrazole fused quinazolinone derivative. On the basis of isolation of the intermediate and observed kinetic isotope effects, a mechanism has been proposed for the C-H activated direct carbonylative annulation reaction.
Nickle Catalysis Enables Access to Thiazolidines from Thioureas via Oxidative Double Isocyanide Insertion Reactions
Yuan, Wen-Kui,Liu, Yan Fang,Lan, Zhenggang,Wen, Li-Rong,Li, Ming
supporting information, p. 7158 - 7162 (2018/11/25)
An efficient synthesis of thiazolidine-2,4,5-triimine derivatives was developed via Ni-catalyzed oxidative double isocyanide insertion to thioureas under air conditions, in which thioureas play three roles as a substrate, a ligand, and overcoming isocyanide polymerization. The reaction is featured by employing a low-cost and low loading Ni(acac)2 catalyst, without any additives, and high atom economy. This is the first example to directly apply a Ni(II) catalyst in oxidative double isocyanide insertion reactions.
Novel non-peptidic small molecule inhibitors of secreted aspartic protease 2 (SAP2) for the treatment of resistant fungal infections
Dong, Guoqiang,Liu, Yang,Wu, Ying,Tu, Jie,Chen, Shuqiang,Liu, Na,Sheng, Chunquan
supporting information, p. 13535 - 13538 (2019/01/05)
Targeting secreted aspartic protease 2 (SAP2), a kind of virulence factor, represents a new strategy for antifungal drug discovery. In this report, the first-generation of small molecule SAP2 inhibitors was rationally designed and optimized using a structure-based approach. In particular, inhibitor 23h was highly potent and selective and showed good antifungal potency for the treatment of resistant Candida albicans infections.
CERAMIDE GALACTOSYLTRANSFERASE INHIBITORS FOR THE TREATMENT OF DISEASE
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Paragraph 000703; 000704; 000745; 000746, (2018/01/17)
Described herein are compounds, methods of making such compounds, pharmaceutical compositions and medicaments containing such compounds, and methods of using such compounds to treat or prevent diseases or disorders associated with the enzyme ceramide galactosyltransferase (CGT), such as, for example, lysosomal storage diseases. Examples of lysosomal storage diseases include, for example, Krabbe disease and Metachromatic Leukodystrophy.
Synthesis and biological evaluation of 2-arylimino-3-pyridin-thiazolineone derivatives as antibacterial agents
Cai, Ming-Guang,Wu, Yang,Chang, Jun
supporting information, p. 2517 - 2520 (2016/07/07)
With an intention to find more potent antibacterial agents, four halogen disubstituted thiazolineone derivatives (2a-d), five halogen monosubstituted thiazolineone derivatives (2e-i), and eleven 2-arylimino-3-pyridin-thiazolineone derivatives (2j-t) were
