22820-08-2Relevant academic research and scientific papers
Synthesis, structure and transformations of 2-iminoimidazolidines into novel fused heterocyclic ring systems
Kornicka, Anita,Saczewski, Franciszek,Gdaniec, Maria
, p. 687 - 699 (2006)
Reaction of 2-chloro-4,5-dihydroimidazole (1) with 2-aminobenzylamines (2a-d) afforded 2-[(imidazolidin-2-ylideneamino)methyl]-anilines (3a-d) which upon treatment with carbon disulfide gave 2,3-dihydro-12H-imidazo[2′,1′:4,5][1,3,5]thiadiazino[2,3-b]quinazolin-5-thiones (4a-d) and 3,4-dihydro-1H-quinazolin-2-thiones (5a-c). Analogous reaction of 1 with 2-aminobenzyl alcohol (6) led to the formation of [2-(4,5-dihydro-1H-imidazol-2-ylamino)phenyl]methanol hydrochloride (7) which was transformed into 1-(4H-3,1-benzoxazin-2-yl)imidazolidin-2-thione (8).{A figure is presented}.
Synthesis and immunomodulating activity of 5H-thiazolo[2,3-b]quinazolin-3(2H)-one
Bennett,Radov,Trusso,Georgiev St.
, p. 633 - 634 (1987)
The synthesis and immunomodulating activity of 5H-thiazolo[2,3-b]quinazolin-3(2H)-one (7) are described. When tested in the Kennedy plaque assay, 7 exerted immunosuppressive activity on IgM production in female C3H mice sensitized with sheep erythrocytes.
Synthesis and Adrenergic Blocking Effects of 2-(Alkylamino)-3,4-dihydroquinazolines
Grosso, John A.,Nichols, David E.,Nichols, Maxine B.,Yim, George K. W.
, p. 1261 - 1264 (1980)
Based on the known biological activity of a variety of guanidine-containing agents, several N-substituted 3,4-dihydroquinazolines were synthesized.These compounds can be considered to be rigid analogues of phenylguanidines.In anesthetized rats the compounds decreased blood pressure and were antagonist of the pressor response to norepinephrine.
One-step construction of unsymmetrical thioureas and oxazolidinethiones from amines and carbon disulfide: Via a cascade reaction sequence
Ding, Chaochao,Wang, Shaoli,Sheng, Yaoguang,Dai, Qian,Zhao, Yunjie,Liang, Guang,Song, Zengqiang
, p. 26768 - 26772 (2019/09/06)
A concise and versatile method for the construction of unsymmetrical thioureas and oxazolidinethiones from amines and carbon disulfide has been achieved in DMSO without addition of extra reagents. The present protocol is compatible with various secondary amines and primary amines, and suitable for intermolecular and intramolecular reactions. Diverse unsymmetrical thioureas and oxazolidinethiones were efficiently obtained in good to excellent yields via a cascade reaction sequence.
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.
SPECIFIC INHIBITORS OF METHIONYL-TRNA SYNTHETASE
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Paragraph 0311, (2016/03/13)
The present disclosure is generally directed to compositions useful in the inhibition of MetRS and methods for treating diseases that are ameliorated by the inhibition of MetRS.
Fragment based search for small molecule inhibitors of HIV-1 Tat-TAR
Zeiger, Mirco,Stark, Sebastian,Kalden, Elisabeth,Ackermann, Bettina,Ferner, Jan,Scheffer, Ute,Shoja-Bazargani, Fatemeh,Erdel, Veysel,Schwalbe, Harald,G?bel, Michael W.
supporting information, p. 5576 - 5580 (2015/01/08)
Basic molecular building blocks such as benzene rings, amidines, guanidines, and amino groups have been combined in a systematic way to generate ligand candidates for HIV-1 TAR RNA. Ranking of the resulting compounds was achieved in a fluorimetric Tat-TAR
Lanthanide-catalyzed cyclocarbonylation and cyclothiocarbonylation: A facile synthesis of benzannulated 1,3-diheteroatom five- and six-membered heterocycles
Jing, Yufeng,Liu, Ruiting,Lin, Yanghui,Zhou, Xigeng
, p. 1117 - 1125 (2014/08/18)
La[N(SiMe3)2]3 proves to be an efficient catalyst system for the cyclocarbonylation of 1,2-disubstituted benzenes with isocyanates. In this approach, aryl/alkyl isocyanates react with o-phenylenediamine, o-aminophenol, o-aminothiophenol, catechols and anilines ortho-substituted by CH2NH2 and CONH2 to form, respectively, the corresponding benzimidazolones, benzoxazolones, benzothiazolones, benzodioxolones, 3,4-dihydroquinazolin-2(1H)-one, and quinazolinediones. These results represent the first example of lanthanide-catalyzed carbonylation. This methodology is also applicable for the preparation of various benzannulated 1,3-diheteroatom cyclic thioketones starting from aryl/alkyl isothiocyanates or CS2 in good to excellent yields. Based on the results of experiments performed using an o-aminobenzamido dianion lanthanide complex, a general mechanism, involving the tandem reaction of two lanthanide-ligand bonds with one heterocumulene molecule, is proposed as well.
(3,4-Dihydro-quinazolin-2-yl)-(2-aryloxy-ethyl)-amine
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Page/Page column 7, (2008/06/13)
The present invention relates to compounds of formula I wherein R, R1, R2, R3, R4, aryl, n, and m are as defined in the specification and pharmaceutically acceptable acid addition salts and tautomeric forms thereof. Such compounds have good activity on the 5-HT5A receptor. Therefore, the invention provides methods for the treatment of certain CNS disorders with such compounds.
(3,4-Dihydro-quinazolin-2-yl)-indan-1-yl-amines
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Page/Page column 6-7, (2010/11/24)
The present invention relates to compounds of formula wherein R1, R2, and n are as defined herein and to pharmaceutically acceptable acid addition salts thereof. The compounds of formula I have a good activity on the 5-HT5A receptor. Therefore, the invention provides the use of a compound of formula I for 5-HT5A receptor related diseases, such as anxiety, depression, sleep disorders and schizophrenia.
