With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1768-64-5,4-Chlorotetrahydropyran,as a common compound, the synthetic route is as follows.
4- (Pheyiylmethyl) morpholin-2-ylj (tetrahydro-2H-pyran-4-yl) methanone (8b); An inerted 6L reactor is charged with THF (242.5 mL), magnesium (54.47 g, 2240mmol) and 5% of the total amount of 4-chlorotetrahydropyran (12.28 mL, 112 mmol). Then, a small amount of methyl iodide (0.5 mL) and one iodine crystal is added. The reaction mixture is stirred and heated up to 64-66C. After initiation, the remaining 4- chlorotetrahydropyran (233.22 mL, 2127 mmol) diluted in THF (890 mL) is slowly added over 135 mins. The mixture is heated up for 30 additional minutes before being cooled to 0C. Then, the Weinreb amide 2b (370 g, 1400 mmol) diluted in THF (2777 mL) is added over 180 mins between 0-4C and the mixture is stirred for a further 60 mins. Then, acetic acid (48 mL, 0.83 mmol) is added to the mixture followed by a 55/45 : v/v : saturated NH4Cl/Ha0 mixture (2590 mL) keeping the temperature below 9C. The organic layer is washed with a 60/40: v/v: saturated NH4CI/H20 mixture (500 mL) and, after separation, toluene (1800 mL) and water (1800 mL) is added to the organic solution. Then after extraction, water (1100 mL) is added to the toluene mixture which is basified with 3.68 M Na2CO3aq (148 mL). The organic layer is dried over MgS04, filtered and concentrated under reduced pressure to dryness to yield compound 8b as the free base (400. 8 g, 98. 6% yield).
1768-64-5, As the paragraph descriping shows that 1768-64-5 is playing an increasingly important role.
Reference£º
Patent; ELI LILLY AND COMPANY; WO2005/47272; (2005); A1;,
Tetrahydropyran – Wikipedia
Tetrahydropyran – an overview | ScienceDirect Topics