118738-91-3Relevant academic research and scientific papers
4 - (4 - ((9H - purine - 6 - yl) thio) phenyl) thiazolyl - 2 - amine derivative and its preparation and use
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, (2017/08/04)
The invention belongs to the field of chemical medicine and particularly relates to a 4-(4-((9H-purine-6-base)sulphur)phenyl)thiazolyl-2-amine derivative and a preparation method and application thereof. The structure of the 4-(4-((9H-purine-6-base)sulphur)phenyl)thiazolyl-2-amine derivative is shown in the formula I. The preparation method of the 4-(4-((9H-purine-6-base)sulphur)phenyl)thiazolyl-2-amine derivative and the application of the 4-(4-((9H-purine-6-base)sulphur)phenyl)thiazolyl-2-amine derivative in preparation of medicine for treating tumors are further provided. The synthetic route is short, reaction conditions are simple, the yield is high, and derivatization is easy. A series of compounds have good anti-tumor activity and low toxicity. A new choice is provided for preparation of the anti-tumor medicine. See the formula in the specification.
Protiodeacylation of 4-Substituted 1-Acetyl-2,6-dimethylbenzenes in Sulphuric Acid: Kinetics and Mechanism
Al-Ka'bi, Ja'far,Farooqi, Jameel A.,Gore, Peter H.,Nassar, Ahmed M. G.,Saad, Esmat F.,at al.
, p. 943 - 950 (2007/10/02)
In 89.8percent (w/w) sulphuric acid rate coefficients (1E4k1/s-1) for the protiodeacetylation of 4-substituted (X) 1-acetyl-2,6-dimethylbenzenes (1) were, at 25 deg C; X=Br, 0.468; I, 0.509; Cl, 0.635; H, 1.345; F, 2.52; Ph, 31.5; t-Bu, 38.6; and Me, 47.2.At 25 deg C the reaction of the ketone (1; X=OMe) was too fast, and at 80 deg C reactions of the ketones (1; X=CONH2 or CO2H) were too slow, for convenient measurement.The carboxy nitrile (X=CN) underwent hydratation to the amide (X=CONH2) rather than protiodeacetylation.The rate coefficients at 25 deg C of eight ketones (1) gave an accurate Hammett correlation, with ?+ constants, giving ρ = -4.64+/-0.05.The reaction of 1-acetyl-2,4,6-trimethylbenzene (1; X=Me) was studied of a range of acidity (73.6-99.9percent sulphuric acid), and a maximum was found near 86.0percent acid.Rates were also measured in D2SO4-D2O.The mechanism is discussed.
