Sep 2021 News Brief introduction of (S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate

314741-40-7, The synthetic route of 314741-40-7 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.314741-40-7,(S)-tert-Butyl 3-(hydroxymethyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.

A solution of iert-butyldimethylsilyl chloride (1.53 g, 10.17 mmol) in DCM (10 ml) was added dropwise to (5)-4-A/-Boc-2-hydroxymethyl-piperazine (2 g, 9.25 mmol) and triethylamine (2.58 ml, 18.49 mmol) in DCM (50 ml) at 20C over a period of 5 minutes under air. The resulting solution was stirred at 20C for 16 hours then evaporated to dryness. The residue was purified by flash silica chromatography, elution gradient 0 to 5% EtOH in EtOAc. Pure fractions were evaporated to dryness to afford te/t-butyl (S)-3-(((ieri-butyldimethylsilyl)oxy)methyl)piperazine-l-carboxylate (2.84 g, 93%) as a colourless oil. 1H NM (500 MHz, CDCI3) 0.00 (s, 6H), 0.84 (s, 9H), 1.40 (s, 9H), 2.48 (s, 1H), 2.6 – 2.87 (m, 3H), 2.92 (d, J = 11.5 Hz, 1H), 3.41 (dd, J = 7.2, 9.8 Hz, 1H), 3.52 (s, 1H), 3.85 (s, 2H).

314741-40-7, The synthetic route of 314741-40-7 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ASTRAZENECA AB; KETTLE, Jason, Grant; BAGAL, Sharanjeet, Kaur; BOYD, Scott; EATHERTON, Andrew, John; FILLERY, Shaun, Michael; ROBB, Graeme, Richard; RAUBO, Piotr, Antoni; (144 pag.)WO2018/206539; (2018); A1;,
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