4674-68-4Relevant articles and documents
Photochemical transformations of 5-methyltetrazole. Matrix isolation FTIR and DFT studies
Pagacz-Kostrzewa,Krupa,Wierzejewska
, p. 37 - 44 (2014)
In situ photolysis of 5-methyltetrazole (MT) isolated in low temperature argon matrices was induced by tunable UV laser radiation. The progress of the reactions was followed by FTIR spectroscopy that allowed for spectroscopic identification of three photo
THERAPEUTIC COMPOUNDS AND METHODS OF USE
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Paragraph 0912; 0913; 0914, (2021/05/21)
The invention relates to compounds and methods of using said compounds, as well as pharmaceutical compositions containing such compounds, for treating diseases and conditions mediated by TEAD, such as cancer.
Copper-catalyzed one-pot synthesis of unsymmetrical arylurea derivatives via tandem reaction of diaryliodonium salts with N -arylcyanamide
Li, Pengfei,Cheng, Guolin,Zhang, Hong,Xu, Xianxiang,Gao, Jingyuan,Cui, Xiuling
, p. 8156 - 8162 (2015/03/18)
An efficient "one-pot" approach to multiple substituted ureas from N-arylcyanamide and diaryliodonium salts has been presented. The two-step procedure involved the weak base-promoted chemoselective arylation of secondary amines with diaryliodonium and Cu-catalyzed nucleophilic addition of N-arylcyanamide with second diaryliodonium. The diverse unsymmetrical arylureas were obtained in up to 91% yield for 29 examples.
Novel and green protocol for the synthesis of 2-iminohydantoins
Kumar, Vinod,Rana, Hemlata,Kaushik, M. P.
, p. 6423 - 6425,3 (2012/12/12)
A novel and green protocol for the synthesis of N-1 and C-5 substituted 2-iminohydantoins has been developed. Methyl N-cyano-N-alkyl/aryl-aminoacetate reacts with aqueous ammonia at room temperature in 10-30 min. The developed protocol does not require any work-up for the isolation or purification of the products; simple filtration can lead to the pure products in good to excellent yields.
Targeting nitric oxide synthase with 99mTc/Re-tricarbonyl complexes containing pendant guanidino or isothiourea moieties
Oliveira, Bruno L.,Raposinho, Paula D.,Mendes, Filipa,Santos, Isabel C.,Santoes, Isabel,Ferreira, António,Cordeiro, Carlos,Freire, Ana P.,Correia, Jo?o D.G.
supporting information; experimental part, p. 1057 - 1065 (2011/04/25)
The visualization of inducible nitric oxide synthase (iNOS) in vivo with specific radioactive probes could provide a valuable insight into the diseases associated with upregulation of this enzyme. Aiming at that goal, we have synthesized a novel family of conjugates bearing a pyrazolyl-diamine chelating unit for stabilization of the fac-[M(CO)3]+ core (M = 99mTc, Re) and pendant guanidino (L1 = guanidine, L 2 = N-hydroxyguanidine, L3 = N-methylguanidine, L 4 = N-nitroguanidine) or S-methylisothiourea (L5) moieties for iNOS recognition. L1-L5 reacted with fac-[M(CO) 3(H2O)]+, yielding complexes of the type fac-[M(CO)3(k3-L)]+ (M = Re/99mTc; 1/1a, L = L1; 2/2a, L = L2; 3/3a, L = L3; 4/4a, L = L4; 5/5a, L = L5), which were fully characterized by the usual analytical methods in chemistry and radiochemistry, including X-ray diffraction analysis in the case of 1. The rhenium complexes 1-5 were prepared as "cold" surrogates of the 99mTc(I) complexes. Enzymatic assays with murine purified iNOS demonstrated that L1, L2, 1 and 2 are poor NO-producing substrates. These assays have also shown that metallation of L4 and L5 (Ki > 1000 μM) gave complexes with increased inhibitory potency (4, Ki = 257 μM; 5, Ki = 183 μM). The organometallic rhenium complexes permeate through LPS-treated RAW 264.7 macrophage cell membranes, interacting specifically with the target enzyme, as confirmed by the partial suppression of NO biosynthesis (ca. 20% in the case of 4 and 5) in this cell model. The analog 99mTc(I)-complexes 1a-5a are stable in vitro, being also able to cross cell membranes, as demonstrated by internalization studies in the same cell model with compound 4a (4h, 37 °C; 33.8% internalization). Despite not being as effective as the α-amino-acid-containing metal-complexes previously described by our group, the results reported herein have shown that similar 99mTc(I)/Re(I) organometallic complexes with pendant amidinic moieties may hold potential for targeting iNOS expression in vivo.
Alkoxy isothiocyanates as intermediates in the flash vacuum pyrolysis of alkoxythioureas
Pedersen, Carl Th.,Jensen, Frank,Flammang, Robert
experimental part, p. 69 - 74 (2009/07/18)
Methoxy isothiocyanate MeONCS 2b was detected by matrix isolation IR spectroscopy following flash vacuum pyrolysis (FVP) of N-methoxythioureas, N-tert-butyl-N′-methoxythiourea 1d being the best precursor. Isothiocyanates 3, amines, and aldehydes are also
2-AMINOPYRIMIDIN-4-ONES AND THEIR USE FOR TREATING OR PREVENTING Aβ-RELATED PATHOLOGIES
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Page/Page column 20-21; 26-27, (2008/06/13)
This invention relates to novel compounds having the structural formula (I) below: [Chemical formula should be inserted here. Please see paper copy] and to their pharmaceutically acceptable salt, compositions and methods of use. These novel compounds prov
Synthesis of isomelamines and isocyanurates and their biological evaluation
Niwa, Ryuji,Kamada, Hitoshi,Shitara, Eiki,Horiuchi, Jiro,Kibushi, Nobuyuki,Kato, Tetsuzo
, p. 2314 - 2317 (2007/10/03)
The reaction of cyanogen bromide (1) with primary amines (2a-p), including arylmethylamines (21-p), gave the corresponding cyanamides (3a- p). Trimerization of 3a-p gave 1,3,5-trisubstituted 2,4,6-triiminohexahydro- 1,3,5-triazines (isomelamines) (4a-p), which were treated with hydrochloric acid to give the corresponding 1,3,5-trisubstituted 2,4,6-trioxohexahydro- 1,3,5-triazines (isocyanurates) (5a-c, f) and 1,3,5-trisubstituted 2-imino- 4,6-dioxohexahydro-1,3,5- triazines (5b'-e'). Biological evaluation of 4a- p, 5a-c, f, and 5b'-e' was carried out, and some of these compounds showed bronchodilator and positive inotropic activities.
Application of of 5-Lithiotetrazoles in Organic Synthesis
Satoh, Yoshitaka,Marcopulos, Nicholas
, p. 1759 - 1762 (2007/10/02)
Lithiation of 1-benzyl and 1-p-methoxybenzyltetrazole at the 5-position with n-butyllithium followed by treatment with electrophiles gave functionalized 1-benzylic tetrazoles, which were converted into the 1-unsubstituted derivatives by debenzylation.
