New learning discoveries about 125995-03-1

125995-03-1 Atorvastatin lactone 6483036, aTetrahydropyrans compound, is more and more widely used in various.

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.

50.0 g of atorvastatin lactone was suspended in a mixture of 150 a of t-butyl methyl ether and 100 ml of acetone, and 3.7 g of strontium hydroxide dissolved in 200 ml of water was slowly added thereto over 30 minutes, and stirred at room temperature for 3 hours. After removing the organic layer, 150 ml of t-butyl methyl ether was added to the aqueous layer, followed by stirring at room temperature for 10 minutes. The organic layer was again removed, and 200 ml of acetone was added to the aqueous layer. The mixture was warmed to 50 C., to which 10.2 g of strontium acetate dissolved in 250 ml of water was slowly added over 2 hours, stirred at 50 C. for 8 hours, and the resulting solution was cooled to room temperature. The precipitate formed was filtered, washed with a mixture of 60 ml of acetone and 90 ml of water and dried in air, to obtain 50.7 g of the title compound (yield: 85%) as a white crystalline powder.Moisture content (Karl-Fisher titrator): about 6.9%Based on the result of such moisture content analysis, the crystalline powder obtained above was confirmed to be the pentahydrate form of formula (Ia), and its XRPD result showed that it is a crystal having distinctively characteristic main peaks (those having I/Io of at least 10%), as shown in Table 1. Accordingly, the crystalline powder obtained above is designated Form I.

125995-03-1 Atorvastatin lactone 6483036, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; HANMI PHARM. CO., LTD.; US2010/120888; (2010); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics

Downstream synthetic route of 125995-03-1

125995-03-1 Atorvastatin lactone 6483036, aTetrahydropyrans compound, is more and more widely used in various.

125995-03-1, Atorvastatin lactone is a Tetrahydropyrans compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

Compound 42 (100 mg, 185 muiotaetaomicron) was dissolved (0514) in ammonia (7Nin MeOH, 1.32 mL, 6.18 mmol) and the (0515) solution was stirred at rt for 24 h. The mixture was (0516) concentrated under reduced pressure. Purification by (0517) flash chromatography (CH2Cl2:MeOH = 95:5? 90: 10) (0518) afforded 43 as a white foam (73 mg, 71%). NMR (0519) (400 MHz, CDCls) delta 7.24-6.95 (m, 14H), 6.88 (br s, 1H), 5.73 (br s, 1H), 5.44 (br s, 1H), 4.42 (br s, 1H), 4.20-4.05 (m, 2H), 4.01-3.90 (m, 1H), 3.79-3.71 (m, 1H), 3.63-3.48 (m, 2H), 2.34-2.23 (m, 2H), 1.74-1.41 (m, 9H), 1.28-1.14 (m, 1H).

125995-03-1 Atorvastatin lactone 6483036, aTetrahydropyrans compound, is more and more widely used in various.

Reference£º
Patent; STICHTING KATHOLIEKE UNIVERSITEIT; SCHIRRIS, Tom Johan Joseph; RITSCHEL, Tina; RUTJES, Floris Petrus Johannes Theodorus; SMEITINK, Johannes Albertus Maria; RUSSEL, Francois Gerard Marie; (92 pag.)WO2017/137469; (2017); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics