With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.125995-03-1,Atorvastatin lactone,as a common compound, the synthetic route is as follows.
To lactone intermediate (V) ( 100 g, 0.185 mol) dissolved in methanol ( 500 ml ) was slowly added sodium hydroxide ( 8.0 g dissolved in 80 ml water ) at 25 to 30 0C and the reaction mass was stirred at 45 to 5O0C for 2 hrs when the HPLC indicated the reaction to be complete. Methanol was distilled off under vacuum, water (100.0 ml) and methanol (100.0 ml) were added and the solution was extracted twice with methyl tertiary butyl ether ( 500 ml and 125 ml each), the combined MTBE layer was washed with a mixture of water ( 90 ml) and methanol (10 ml). The pH of the combined aqueous layer was adjusted to 7.8 to “6.2 with 6N hydrochloric acid and the mixture was diluted with methanol (1.0 It ) and then suspension of calcium acetate (16.0 g in 1.0 It water) was added to the reaction mixture at 25 to 3O0C. The mixture was then poured into water ( 2.0 It ), extracted with dichloromethane ( 2 x 1.5 It) and the combined dichloromethane layer was concentrated at 40 to 42 0C to approx 700 ml. The concentrated solution was fine filtered through Whatman filter, cooled to 10 to 150C and diisopropyl ether (3.0 It) was slowly added keeping the temperature below 150C. The mixture was stirred for 15 min at 10 to 150C, centrifuged, washed with cold diisopropyl ether (100 ml) and dried under vacuum at 55 to 6O0C for 24 hrs to obtain amorphous Atorvastatin calcium as a white to off white powder. Yield: 98.72 g (92.21 %); Purity (HPLC): 99.45 %, Assay (HPLC): 99.1%. Calcium content: 3.30 %; Moisture content (by K.F):1.12 %; Residual solvents: Methanol < 0.05 %, THF < 0.05 %, Dichloromethane < 0.02 %, Diisopropyl ether < 0.02 %., 125995-03-1
The synthetic route of 125995-03-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; MOREPEN LABORATORIES LIMITED; WO2006/48893; (2006); A2;,
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