976-71-6Relevant articles and documents
Preformulation studies of spironolactone: Effect of pH, two buffer species, ionic strength, and temperature on stability
Pramar,Gupta
, p. 551 - 553 (1991)
Using a stability-indicating HPLC assay method, the effect of pH, two buffer species (citrate and phosphate), ionic strength, and temperature on the stability of spironolactone in 20% solution of ethyl alcohol in water has been studied. The optimum pH of stability appears to be ~4.5. On increasing the buffer concentration, both species hastened the decomposition of spironolactone. The ionic strength did not affect the stability of the drug. The energy of activation has been estimated to be ~78.8 kJ/mol at pH 4.3. The un-ionized spironolactone is subject to general acid-base catalysis. The K(h) and K(oh) values at 40 °C have been estimated to be 1.63 and 2.8 x 105 day-1, respectively. The HPO4-2 ion had ~10 times more catalytic effect than the H2PO4-1 ion. This data will be used to develop a stable oral liquid dosage form of the drug.
Synthesis and reactions of 2-methylene-canrenone
Gorlitzer,Moormann,Pollow,Schaffrath
, p. 149 - 155 (1995)
Starting from the Mannich salt 1 of the aldosterone antagonist canrenone or from 2-methylene-canrenone (2) the A-ring annulated hetero- and carbocycles 5, 6, 8-13 were prepared. Receptor (estradiol, progesterone, androgen, gluco- and mineralocorticoid) binding studies and competition studies with the serum proteins SHBG and CBG were carried out using the compounds 2, 3, 4b, 5, 6b, 8 and 12. The relative binding affinities with CBG are below 1%, in all other cases lower than 0.01%.
Method for preparing spirolactone intermediate canrenone
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Paragraph 0019-0033, (2021/10/20)
The invention provides a method for preparing spirolactone intermediate canrenone. The method comprises the following operation steps: a lactone substance (I) is dissolved in an organic solvent, a catalyst and an auxiliary agent are added, and the mixture is stirred at 50-80 DEG C to prepare the canrenone (II), wherein the organic solvent is at least one of cyclohexane, toluene or methyl tetrahydrofuran; the auxiliary agent is at least one of dimethyl formamide, N,N - dimethyl acetamide and N-methyl pyrrolidone; and the catalyst is poly-4-vinylpyridine. The reaction route is shown in the specification. Compared with the prior art, the method has the advantages that the reaction temperature is low, pressurization is not needed, the quality of canrenone can be improved, the energy consumption can be effectively reduced, and the production cost can be reduced.
Synthesis process of steroid compound, canrenone and spirolactone
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Paragraph 0126-0127; 0129-0140; 0142-0144; 0146, (2020/11/23)
The invention relates to the technical field of medicine synthesis, in particular to a synthesis process of a steroid compound, canrenone and spirolactone. An embodiment of the invention provides thesteroid compound. The steroid compound has a structural formula as shown in the specification. In the structural formula, R is selected from H or an alkyl group. The steroid compound can be used for synthesizing canrenone and spirolactone, synthesis conditions are mild, synthesis efficiency is high, the amount of wastewater is small, the quality of the formed products is high, and production costcan be effectively reduced.