1-benzyl-3,3-difluoropiperidin-4-ol synthesis

6synthesis methods

Product Name:1-benzyl-3,3-difluoropiperidin-4-ol
CAS Number:1239596-53-2
Molecular formula:C12H15F2NO
Molecular Weight:227.25

4,4-Piperidinediol, 3,3-difluoro-1-(phenylmethyl)-

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Yield:1239596-53-2 97.1%

Reaction Conditions:

with methanol;sodium tetrahydroborate at 0 - 5; for 0.25 h;

Steps:

1.5 Step 5:

To a solution of B5 (34 g, 139 mmol) in methanol (730 mL) was added sodium borohydride (7.9 g, 209 mmol) in portions at 0-5 °C. After stirring at 0-5 °C for an additional 15 minutes, an aqueous solution of sodium bicarbonate (0.1 mole, 54 mL) was added and the mixture was stirred for 5 minutes. The mixture was dried over sodium sulfate, concentrated and purified by silica gel column ethyl acetate/n-hexane = 1/20 to 1/10) to give product B6 as a colorless oil (30 g, yield 97.1%).

References:

EP3438107,2019,A1 Location in patent:Paragraph 0165; 0170

23583-21-3 Synthesis

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References

N-(1H-Benzotriazol-1-ylmethyl)-N-(phenylmethyl)-beta-alanine ethyl ester

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References

ethyl 3-(benzyl(3-ethoxy-3-oxopropyl)aMino)-2,2-difluoropropanoate

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ethyl 1-benzyl-5,5-difluoro-4-oxopiperidine-3-carboxylate

1067915-34-7
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References