Aminopyrimidine derivatives as protein kinases inhibitors. Molecular design,synthesis, and biologic activity

The review compiles the strategies and methods of development of aminopyrimidine derivatives as targeted antitumor pharmaceuticals. The advances in organic and heterocyclic chemistry are considered in the targeted synthesis of aminopyrimidine derivatives whose series contains the most demanded and efficient antitrumor pharmaceuticals. The problems of preparation of compounds with multikinase activity profile and the construction of chimeric molecules are discussed.     

The cooperative effect of electromigration and non-equilibrium vacancies on reactive phase growth

Phase formation under a direct current was analysed for a binary system with non-equilibrium vacancy distribution. It was shown that the non-equilibrium vacancy distribution diminishes the effect of electromigration on the phase formation process: if the electric current augments the phase growth, the resulting vacancy concentration gradient delays it; if the current opposes phase growth, the vacancy concentration gradient maintains it. A comparative analysis is presented involving the results obtained within Gösele and Tu theory (taking into consideration the finiteness of the reaction rate at interfaces).     

Synthesis of maleopimaric and citraconopimaric acids N-[3-(pyrimidin-2-yl)aryl]amides

Acylation of 6-methyl-N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine, 4-methyl-N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine, and N-[4-(pyridin-3-yl)pyrimidin-2-yl]benzene-1,3-diamine with maleopimaric and citraconopimaric acid chlorides, with benzotriazolyl maleopimarate afforded N-[3-(pyrimidin-2-yl)aryl]amides of maleopimaric and citraconopimaric acids. By the reaction of substituted N-arylamides of maleopimaric acid with methanesulfonic acid biologically active methanesulfonates were obtained.     

Charge grating kinetics in photorefractive crystals subjected to an electric field

The kinetics of charge gratings induced by a standing light wave in a photorefractive crystal in the presence of an electric field is described correctly. It obeys an ordinary differential equation of the fourth order that has two pairs of complex conjugate solutions. A general solution to this equation that satisfies a given initial condition is derived. The field-related mechanism causing charge oscillations and extending the time the gratings take to pass into the steady state is revealed. A relation between these oscillations and space-charge waves is found.     

On crossing of a level by processes defined by sums of a random number of terms

We study the joint distribution of boundary functionals related to the crossing of a positive (negative) level by a process consisting of a homogeneous Poisson process and a process defined by sums of a random number of continuously distributed terms.Translated from Ukrainskii Matematicheskii Zhurnal, Vol. 47, No. 7, pp. 897–914, July, 1995.     

Vanillin esters of aromatic carboxylic acids in the synthesis of benzo[a]acridine and benzo[b][4,7]phenanthroline derivatives

By condensation of vanillin esters of substituted benzoic acids with 2-naphthylamine and 6-quinolylamines and also with cyclic β-diketones (1,3-cyclohexanedione and dimedone) 2-methoxy-4-(11-oxo-7,8,9,10,11,12-hexahydrobenzo[a]acridin-12-yl)-and 2-methoxy-4-(11-oxo-7,8,9,10,11,12-hexahydrobenzo[b][4,7]-phenanthrolin-12-yl)phenyl benzoates were prepared.     

Three component condensation of 6-quinolylamine with aromatic aldehydes and cyclohexyl 1,3-diketones

A three component condensation of 6-quinolylamine with 4-bromo-or 4-methoxybenzaldehyde, and 1,3-cyclohexanedione or dimedone gave 12-(4-bromophenyl)-and 12-(4-methoxyphenyl)-9,9-dimethyl-8,9,10,12-tetrahydro-7H-benzo[b][4,7]phenanthrolin-11-ones. The reaction intermediates obtained were N-arylmethylene-6-quinolylamines, 2-arylmethylenebis(1,3-cyclohexanediones), 3-(6-quinolylamino)-2-cyclohexenone, and 5,5-dimethyl-3-(6-quinolylamino)-2-cyclohexenone. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No 6, pp. 877–885, June, 2007.     

Three-component condensation of 2-naphthylamine with aromatic aldehydes and 5-(2-furyl)-1,3-cyclohexanedione

Three-component condensation of 5-(2-furyl)-1,3-cyclohexanedione with 2-naphthylamine and aromatic or heteroaromatic aldehydes afforded 12-aryl(hetaryl)-9-(2-furyl)-7,8,9,10,11,12-hexahydrobenzo[a]-acridin-11-ones possessing two asymmetric carbon atoms (C⁹ and C¹²). The products were found to be formed as mixtures of diastereoisomers.     

5-Methyl-1,3-cydohexanedione in the synthesis of benzo[a]phenanthridine derivatives

By condensation of arylmethylene-2-naphthylamines with 5-methyl-l,3-cyclohexanedione 5-aryl-2-methyl-1,2,3,4,5,6-hexahydrobenzo[a]phenanthridin-4-ones were synthesizes.