Downstream synthetic route of 203662-51-5

The synthetic route of 203662-51-5 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.203662-51-5,4-Allyl-1-Boc-4-hydroxypiperidine,as a common compound, the synthetic route is as follows.

203662-51-5, tert-butyl (3RS)-3-hydroxy-1-oxa-8-azaspiro[4.5ldecane-8-carboxylate tert-butyl 4-allyl-4-hydroxypiperidine-1-carboxylate (1153 g, 4.8 mol) was dissolved in tert-butanol (10 L) and water (4 L). To the solution sodium periodate (1124 g, 5.3 mol, 1.1 eq) was added and the mixture was stirred at 50 0C for 30 minutes. At 50 0C a solution of Na2S2O5 (1007 g, 5.3 mol, 1.1 eq) in water (4.2 L) was added dropwise over 4 hours to the solution. After addition the reaction mixture was stirred for 7 hours at 50 0C and another 48 hours at RT. The mixture was transferred to an extraction vessel and the organic layer was separated from the aqueous layer. The aqueous layer was extracted (3x) with ethyl acetate. The organic layers were combined and washed with a saturated solution of Na2S2O3 (3x) to give a colorless solution. The solution was washed with brine and evaporated to give crude product (987 g, 80percent). The crude product was purified by flash chromatography (10-80percent EtOAc/Heptane) to give the title compound (287 g, 35percent). m/z 158 (MH+ minus Boc).

The synthetic route of 203662-51-5 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; PFIZER INC.; LONG, Scott Allen; MEYERS, Marvin Jay; PELC, Matthew James; SCHWEITZER, Barbara Ann; THORARENSEN, Atli; WANG, Lijuan Jane; WO2010/58318; (2010); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem