- Synthetic method of amifostine
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The invention discloses a synthetic method of amifostine. The method includes the following steps that 1, a compound shown in the formula (IV) reacts with hydrogen in the presence of rhodium oxide, gold oxide and raney nickel to obtain a compound shown in formula (III); 2, the compound shown in formula (III) reacts with hydrogen bromide in a mixed solvent formed by water and C1-5 alcohol solventsto obtain a compound shown in the formula (II) at 0-20 DEG C; 3, the compound shown in formula (II) reacts with sodium thiophosphate to obtain amifostine shown in the formula (I). Through the method,high-yield and high-purity products can be obtained, the process is simple, and the method is suitable for industrial production.
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Paragraph 0031; 0032-0033; 0036-0037; 0040-0041
(2019/07/10)
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- Synthesis and radioprotective activity of WR-1065 derivatives: N-(2-acetylthioethyl)-1,3-propanediamine and N,N'-bis(2-acetylthioethyl)-1,3-propanediamine
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N-(2-Acetylthioethyl)-1,3-propanediamine (13a, as its 2HBr salt, or 13b, as its 2CF3CO2H salt) and N,N'-bis(2-acetylthioethyl)-1,3-propanediamine (16, as its 2CF3CO2H salt) have been prepared and evaluated as potential radioprotectors in mice.Their toxicity and radioprotective activity (survival rate) have been determined and compared with that of WR-2721.Intermediate N-(2-acetylthioethyl)-N,N'-bis(Z or Boc)-1,3-propanediamines were prepared in two ways from the corresponding alcohols.The most convenient method (the Mitsunobu procedure) was used to obtain theN,N'-bis(2-acetylthioethylated) derivative from the corresponding diol.Surprisingly, none of these compounds possesses radioprotective activity. N-(2-acetylthioethyl)-1,3-propanediamine / N,N'-bis(2-acetylthioethyl)-1,3-propanediamine / WR-2721 / WR-1065 / radioprotector
- Oiry, J.,Pue, J. Y.,Laval, J. D.,Fatome, M.,Imbach, J. L.
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- NUCLEOPHILIC CLEAVAGE AND FORMATION OF SATURATED HETEROCYCLES. XII. REACTIVITY OF SMALL HETEROCYCLES TOWARD AMINOLYSIS AND HYDROLYSIS
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The cleavage of four-membered saturated heterocycles proceeds via a more product-like transition state than that of three-membered rings.General acid catalysis is characteristic of oxygen heterocycles, but in the case of nitrogen heterocycles catalysis is specific.The reactivity of amines in the cleavage of azetidines is linearly dependent on their pKa values, primary and secondary amines comprising separate reaction series.
- Bobylev, V. A.,Veselkov, N. Yu.,Dalin, A. R.,Sharikov, F. Yu.
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p. 1700 - 1713
(2007/10/02)
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