23826-47-3Relevant academic research and scientific papers
COMPOSITIONS AND METHODS COMPRISING SUBSTITUTED 2-AMINOIMIDAZOLES
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Paragraph 0189, (2018/10/25)
The present invention presents 2-(acylamino)imidazoles with therapeutic activity, including selective activity against cancer cells, and compositions comprising them. Methods of using and preparing the 2-(acylamino)imidazoles are also presented.
COMPOUNDS USEFUL AS MODULATORS OF TRPM8
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Paragraph 0871-0872, (2016/03/29)
The present invention includes compounds useful as modulators of TRPM8, such as compounds of Formulae (Ia), (Ib) and (Ic), and the subgenus and species thereof; personal products containing those compounds; and the use of those compounds and the personal products, particularly the use of increasing or inducing chemesthetic sensations, such as cooling or cold sensations.
ZnCl2-promoted asymmetric hydrogenation of β-secondary-amino ketones catalyzed by a P-chiral rh-bisphosphine complex
Hu, Qiupeng,Zhang, Zhenfeng,Liu, Yangang,Imamoto, Tsuneo,Zhang, Wanbin
supporting information, p. 2260 - 2264 (2015/02/19)
A new catalytic system has been developed for the asymmetric hydrogenation of β-secondary-amino ketones using a highly efficient P-chiral bisphosphine-rhodium complex in combination with ZnCl2 as the activator of the catalyst. The chiral γ-secondary-amino alcohols were obtained in 90-94% yields, 90-99% enantioselectivities, and with high turnover numbers (up to 2000 S/C; S/C = substrate/catalyst ratio). A mechanism for the promoting effect of ZnCl2 on the catalytic system has been proposed on the basis of NMR spectroscopy and HRMS studies. This method was successfully applied to the asymmetric syntheses of three important drugs, (S)-duloxetine, (R)-fluoxetine, and (R)-atomoxetine, in high yields and with excellent enantioselectivities.
Synthesis of polycarpine, a cytotoxic sulfur-containing alkaloid from the ascidian Polycarpa Aurata, and related compounds
Radchenko, Oleg S.,Novikov, Vyacheslav L.,Willis, Richard H.,Murphy, Peter T.,Elyakov, George B.
, p. 3581 - 3584 (2007/10/03)
Polycarpine 1, a highly cytotoxic marine natural product, has been synthesized in three steps from p-methoxyphenacyl bromide 4 in 57% overall yield. The key reaction for construction of the symmetrically substituted disulfide linkage of polycarpine is the treatment of 2-amino-4-(4-methoxyphenyl)-1-methylimidazole 17 with S2Cl2 in acetic acid. In a similar way ten related compounds, including three thiazole analogues, have been prepared. Most of them exhibit high cytotoxic activities against an array of human cancer cell lines.
SYNTHESIS, STEREOCHEMISTRY, AND ISOMERIC TRANSFORMATIONS OF 4-ARYL-5-AROYL-2-METHYLTHIO-2-IMIDAZOLINES
Konovalov, V. A.,Bubel', O. N.,Tishchenko, I. G.
, p. 1229 - 1233 (2007/10/02)
The corresponding 4-aryl-5-aroyl-2-methylthio-2-imidazolines were obtained by the reaction of complexes of cis- and trans-3-aroylaziridines and boron trifluoride with methyl thiocyanate.It is shown on the basis of spectral data that the aziridine ring is opened regiospecifically at the C(2) atom and stereospecifically with inversion of the configuration.
SYNTHESIS AND STEREOCHEMISTRY OF 2,2,3-TRIMETHYL-5-ARYL-4-AROYLOXYZOLIDINES
Tishchenko, I. G.,Bubel', O. N.,Konovalov, V. A.
, p. 29 - 33 (2007/10/02)
cis-2,2,3-Trimethyl-5-aryl-4-aroyloxazolidines were obtained by heating complex boron trifluoride salts of trans-1-methyl-2-aryl-3-aroylaziridines with acetone.The reaction of complex boron trifluoride salts of cis-1-methyl-2-aryl-3-aroylaziridines leads to substituted benzaldehydes and ω-N-methylaminoacetophenones.
