With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.4801-58-5,Piperidin-1-ol,as a common compound, the synthetic route is as follows.
To a solution of compound 33a (140mg, 0.588 mmol) in DCM (15 mL) and DIPEA (206 ml, 1.18 mmol) was added dropwise at r.t a solution of triphosgene (69.8 mg, 0.235 mmol) in 5 mL of DCM. After 5 min. a solution of 1-hydroxypiperidine (89.2mg, 0.882 mmol) and DIPEA (103 ml, 0.59 mmol) were added. After stirring overnight at r.t. the reaction mixture was diluted with DCM, the organic layer separated, dried over sodium sulphate and evaporated to dryness. Purification by automated flash chromatography with a Biotage Isolera, FLASH 12+ column, using a gradient from PE : EtOAc 2:8 to EtOAc 100% afforded 13 mg of a white gummy solid, which was repurified on a SNAP 12 RP column with a gradient from NH4HCO3 buffer:ACN 6:4 to NH4HCO3 buffer:ACN 1:1.6 mg of the title compound was obtained as a gummy solid. UPLC-MS [M+H]+ = 366.79 (0376) 1H NMR (400 MHz, CDCl3) d ppm 1.28 (s, 1 H), 1.65 (br. s., 1 H), 1.74 – 1.88 (m, 4 H), 2.39 (s, 3 H), 2.70 (br. s., 2 H), 3.46 (br. s., 2 H), 3.97 (t, 2 H), 4.14 (t, 2 H), 4.91 (s, 2 H), 7.20 – 7.36 (m, 2 H), 7.36 – 7.46 (m, 2 H), 4801-58-5
The synthetic route of 4801-58-5 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; RECORDATI INDUSTRIA CHIMICA E FARMACEUTICA S.P.A; GRAZIANI, Davide; RIVA, Carlo; MENEGON, Sergio; TAZZARI, Valerio; (98 pag.)WO2019/145214; (2019); A1;,
Piperidine – Wikipedia
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