With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.832715-51-2,Isopropyl 4-hydroxypiperidine-1-carboxylate,as a common compound, the synthetic route is as follows.
832715-51-2, 4,6-Dichloro-5-methylpyrimidine (1) (2.4235 Kg, 1.000 equivalents) and 4-hydroxypiperidine-1-carboxylic acid isopropyl ester (2) (2.8182 Kg, 1.012 equivalents) were dissolved in tetrahydrofuran (THF, 25.0028 Kg), and the resulting solution was cooled to -15 to -10 C. To the cold solution, potassium-tert-butoxide in tetrahydrofuran (1 M, 12.6051 Kg, 0.9399 equivalents) was added at a rate sufficiently slow to maintain the reaction mixture below 0 C. with reactor jacket cooling. The reaction mixture was then stirred at about -5 C. for about 2 hours before an additional portion of potassium-tert-butoxide in tetrahydrofuran (1 M, 0.5692 Kg, 0.0424 equivalents) was added to achieve >97% conversion of the pyrimidine after an additional hour of stirring at about -5 C. Most of the solvent was then removed by distillation at 30-65 C., 80 torr. Addition of water (19.9681 Kg) to the evaporation residue precipitated the product. Distillative removal of THF was then completed at 30-65 C., 80 torr, and the resulting stirred slurry was cooled to 0 C. for an hour. The solids were then collected by suction filtration, washed with water (8.011 Kg, 4 C.), and vacuum dried to constant weight at 50 C., 40 torr to provide product (3) (4.491 Kg, 96.3% yield).
As the paragraph descriping shows that 832715-51-2 is playing an increasingly important role.
Reference£º
Patent; Gharbaoui, Tawfik; Fritch, John R.; Krishnan, Ashwin M.; Throop, Beverly Wolgast; Kato, Naomi S.; US2006/155129; (2006); A1;,
Piperidine – Wikipedia
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