[2,4-dioxo-1,3 - bis (5-methyl-3-tyuhexjl) -6-methyl-1,2,3, 4 - tetrahydropyrimidin-s,s] cis-dichloroplatinum showing immunotropic activity

 

(57) Abstract:

Usage: in medicine as a means of manifesting immunotropic activity. The inventive product -[2,4-dioxo - 1,3-bis(5-methyl-3-tyuhexjl)-6-methyl -1,,2,3,4-Tetra hydropyridine - S,S]CIS - dichloroplatinum. Yield 35 g (90% ). Reagent 1: an aqueous solution of K2PtCl4Reagent 2: 1,3-bis(isopotential)-6-methyluracil in acetone. table 1.

The invention relates to organic chemistry, specifically to a new chemical compound - complex PtCl2with 1,3-bis(isopotential)-6-methyluracil formula

showing immunotropic activity.

This complex synthesis method and its properties are not described in literature.

Similar in structure and purpose is a 4-cisplatin.

It is known that 4-cisplatin (1)

exhibits antitumor activity, inhibits DNA synthesis, used in breast cancer, prostate cancer, ovarian cancer. However, immunotropic activity not described (GST and AOK).

It is also known that the platinum-containing coordination compounds lot - so Dyachenko S. A. with co (2) received complex compounds of Pt (II) and Pd (II) with 5-aminouracil and its methyl producing CLASS="ptx2">

Known (3) CIS-Pt(NH3)2(I-MeY)2and (NH3)2Pt(I-MeY)2Pt(en)NO35H2O

(4), but their immunotropic activity has not been studied.

Of these complexes could be taken as a structural analogue, for example, coordination compounds (NH3)2Pt(I-MeY)2but it immunotropic activity has not been studied, no LD50. Therefore was taken as the equivalent of hydrocortisone, immunotropic properties of which are studied.

The aim of the invention is the expansion of means of influence on a living organism characterized by pronounced immunotropic activity.

This goal is achieved by a new compound - complex PtCl2with 1,3-bis(isopotential)-6-methyluracil. How to obtain it is through the interaction of K2PtCl4in odnourovnevoi environment with 1,3-bis(isopotential)-6-methyluracil at room temperature for 3 hours

P R I m e R 1. In a flat-bottomed flask with a capacity of 50 ml asleep 1 g K2PtCl4, dissolved in 10 ml of water and the resulting solution was added dropwise with stirring on a magnetic stirrer 0,86 g (0,0024 mole) of 1,3-bis(isopotential)-6-methyluracil in 10 ml of acetone. When intense shutovskoy funnel, washed with water from salts, pererastayut in chloroform and obtain 1.35 g (90%) of the chloride complex of platinum with 1,3-bis(isopotential)-6-methyluracil soluble in chloroform and acetone.

Found,%: C 32,90; H 4,81; Cl To 12.44; S 10,32; Pt 31,43; N 4,35.

C17H30N2O2S2PtCl2.

Calculated, % : C 32,69; H 4,84; N 4,48; Cl 11,35; S 10,27; Pt 31,24; O 5,12.

IR spectrum (cm-1): 320, 330 (YPtCl); 305 (YPtS).

In the work Dyachenko et al. (2) the obtained complex compounds of Pt (II) and Pd (II) with 5-aminouracil and its methyl derivatives with monodentate coordination of the ligands only through the nitrogen atom ekzoticheskoy amino group.

The structure of the proven IR spectra.

(3) the obtained complex compounds connected through the N3-platinum pyrimidine-2,4-dioxy and the second ligand through ekzoticeski oxygen atom.

(4) a series of dual complexes (X2)PtL2M(Y2)ZnH2O; L = (-MeUC5H5P2O2or-Met, C6H7N2O2) link Pt N3position and the second metal through the O4- position. X2and Y2= (NH3)2, Ethylenediamine, EN: 2,21-beparis (NH3)2Pt(I-MeU)Pd(en)(NO3)6H2O by X-ray analysis.

In this case, the complex is formed by communication with gray.

The structure of the target product 2,4-dioxo-1,3-bis(5-methyl-3-tyuhexjl)-6-methyl-1,2,3,4 - tetrahydropyrimidin-S, S-CIS-dichloroplatinum proven IR and PMRN spectra.

In the IR spectrum of compound has absorption bands in the region 318, 332 cm-1related to the stretching vibrations due PtCl2and clearly indicating the formation of coordination compounds of the type CIS-PtCl2L (9). Absorption bands in the region 307 cm-1refer to the stretching vibrations of communication PtS. The absorption band of stretching vibrations of (N-1)N is absent. Absorption bands in the region 1660, 1720 cm-1characteristic ring of uracil (C=ON - C = 0).

That the complexation is carried out by forming a coordination Pt-S spectrum shows AMRN complex, which in comparison with the spectrum of the ligand greatest additional chemical shift, there are signals of protons of methylene groups at the sulfur atom in the weak field 0.7-0.8 M. D.

It is established that CIS-PtCl2(1,3-CH2CH2SCH2CH(CH3)2< / BR>


 

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