SU539901A1 - The method of obtaining reactive copolymers - Google Patents

Description

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The invention relates to the synthesis of reactive polymers.

It is known that, along with the methods of attaching drug compounds to plasma macromolecule macromolecules, reactions of functional groups can be obtained by preparing polymers for medicinal purposes by another method — joint polymerization. Of particular interest in this regard are N-vinylpyrrolidone copolymers containing active groups capable of adding medicinal drugs 1, 2, 3 ,. These groups include the following: -OH, -COOH, -NHa, -CONHa, -Hal,

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The introduction of groups with chemical and biological activity into the polymer chain is of great interest for the synthesis of physiologically active and medicinal preparations. A known method for the preparation of polymeric drugs by copolymerization of N-vipilpyrrolidone with azomethine derivatives of p-aminosalicylic acid sodium salt containing vinyl, methacryl and crotyl primers 5.

It is known that a number of the most important medicinal preparations of central action belong to the indole derivatives: reserpine, a-yohimbin, 1 -cyclohexylmethyl-1,2,3,4 - tetrahydronorgarman, aymalia, serpentine, raubazin, vincamine; stimulators of the central nervous system — analogues of tryptamine, etc. 4,5,6,7-Tetrahydroindole is widely used as a synthetic matrix or synthetic key in the preparation of many valuable psychotropic drugs of the indole series.

To broaden the range of polymer reactive bases for the synthesis of drugs, a method is proposed.

method of obtaining a copolymer of N-vinylpyrrolidone with N-vinyltetrahydroindole

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containing chemically and biologically active 4,5,6,7-tetrahydroindole system.

Claims (5)

The copolymerization reaction is carried out with or without a solvent at 60-80 ° C in the presence of azo-bis-isobutyric acid dinitrile. Synthesized copolymers are purified by precipitating from a benzene solution into a mixture of ethyl and petroleum ethers taken in a 3: 1 ratio. The structure of a fragment of the obtained product can be represented as follows: -Hong-OH -,. ((, 4 - iX) The copolymers are white or Slightly yellowish powders, soluble in dioxane, benzene, chloroform, in water (with a high content in copolymer N-vinyl pyrrolidone) insoluble in heptane, diethyl n petroleum ether, ethanol. The molecular weight of copolymers ranges from 2000 to 10,000. The presence of copolymerization is confirmed by the nature of the solubility of the synthesized products. The proposed method is simple. Moreover, it does not require sp Special monomer purification, special conditions of the process. By varying the initial monomer ratio, copolymers with a given composition and molecular weight can be obtained Example 1. Copolymerization of N-vinylpyrroldone (I) with N-Winnltetrahydroindole (I). A. With a ratio of monomers of 1: P 0.5: 0.5 (mol. Fractions) of the copolymerization was carried out in sealed glass ampoules at 60 ° C for 20 hours. 4.35 g of N-vinyl pyrrolidone, 5.65 g of N-excnl tetragndroindole and 0, 2 g of dinentril of azo-bis-hydroxybutyric acid (2 wt. %). The copolymer was isolated by reprecipitation from benzene to a mixture of dimethyl and petroleum ethers in the ratio 3: 1, dried in vacuum to a constant weight. 7.92 g of copolymer are obtained with a yield of 79.2%, mol. weight 8000. The composition of the copolymer is determined by the intensity of the CO absorption band of the N-vinylnirrolidone group (I: And 0.378:: 0.622). B. When the ratio of monomers is 1:11 0.5:: 0.5 (mol. Shares in benzene) take 4.35 g N-vinyl pyrrolidone, 5.65 g N-vinyl tetrahydraindole, 5 ml benzene and 0.2 g initiator. The mixture is heated for 20 hours prn 60 ° C. The resulting product is treated analogously to example 1A. 7.69 g of copolymer are obtained with a yield of 77.9%, mol. weight 3900. The composition of the copolymer: 1: P 0.404: 0.596. B. When the ratio of monomers is 1: P 0.25: 0.75 (mol. Fractions), 2.0 g N-vinyl pyrrolidone, 7.96 g N-vinyl tetrahydroindole, 0.2 g initiator, 5 ml benzene are heated for 15 hours 80 ° C. The copolymer is treated analogously to example 1A. 6.6 g of copolymer are obtained with a yield of 66.0%, mol. weight 1800. The composition of the sonolymer I: P 0.321: 0.679 (mol. share). Thus, according to the proposed method, reactive copolymers of N-vinylpyrroldone are obtained with monomers containing active groups suitable for chemical combination with dosage forms and possessing physiological activity. Claims The method of producing reactive copolymers by copolymerizing N-vinylpyrrolidone with a vinyl monomer, is characterized in that, in order to expand the range of reactive polymeric bases for the synthesis of drugs, N-vinyltetrahydroindole is used as the vinyl monomer. Sources of information taken into account in the examination: 1. USSR author's certificate number 221228, M. Kl.2 C 08F 226/10, 1969. 2. USSR Author's Certificate No. 316703, M. Cl.2 C 08F 226/10, 1970. 3. USSR Author's Certificate No. 373278, M. CL. 08F 226/10, 1971. 4. USSR author's certificate number 403694, M. Kl.2S08R226 / 10, 1972. 5. USSR author's certificate No. 384839, M. Kl.2 With 08F 226/10, 1971 (prototype).