With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.140645-24-5,(S)-3-(Aminomethyl)-1-N-Boc-piperidine,as a common compound, the synthetic route is as follows.
A solution of (S)-1-Boc-3-(aminomethyl)piperdine (429 mg, 2.0 mmol, CAS [140645-24-5], CHN Technologies, Woburn Mass., USA) in dichloromethane (10 mL) was treated with a 37% aqueous formaldehyde solution (551 muL, 20.0 mmol) followed by sodium triacetoxyborohydride (4.23 g, 20.0 mmol). The mixture was stirred for 4 h then quenched with dichloromethane (10 mL) and saturated aqueous solution of NaHCO3 (50 mL). The organic portion was further washed with a brine solution (10 mL), then dried over MgSO4, filtered, and evaporated in vacuo to afford product as an oil. LC/MS 1.10 min, [M+1]+ 243. The methylated intermediate was dissolved in 1,4-dioxane (5 mL) and treated with a 4 N solution of hydrogen chloride in 1,4,-dioxane (5 mL) and stirred for 2 hr, after which time product had precipitated out of solution. The reaction mixture was evaporated in vacuo and filtered with the aid of ethyl ether. The resulting solids were air dried to afford product as a colorless solid (290 mg, 67% overall). LC/MS 0.60 min, [M+1]+ 143.
140645-24-5, 140645-24-5 (S)-3-(Aminomethyl)-1-N-Boc-piperidine 1502022, apiperidines compound, is more and more widely used in various fields.
Reference：
Patent; Helicon Therapeutics, Inc.; US2009/62252; (2009); A1;,
Piperidine – Wikipedia
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