tert-Butyl 4-(benzylamino)-3,3-difluoropiperidine-1-carboxylate synthesis

9synthesis methods

Product Name:tert-Butyl 4-(benzylamino)-3,3-difluoropiperidine-1-carboxylate
CAS Number:1067914-82-2
Molecular formula:C17H24F2N2O2
Molecular Weight:326.38

tert-butyl 3,3-difluoro-4-oxopiperidine-1-carboxylate

1215071-17-2
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100-46-9 Synthesis

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tert-Butyl 4-(benzylamino)-3,3-difluoropiperidine-1-carboxylate

1067914-82-2
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Yield:1067914-82-2 48%

Reaction Conditions:

with sodium tris(acetoxy)borohydride in dichloromethane at 20;

Steps:

[0253] To a solution of III-3-1 (750 mg, 3.2 mmol) in DCM (20 mL) were added phenylmethanamine (440 mg, 4.1mmol) and NaBH(OAc)3 (298 mg, 15.0 mmol). The reaction mixture was stirred at room temperature overnight. The reaction mixture was treated with saturated NaHCO3, extracted with DCM. The combined organic extracts were dried over Na2SO4 and concentrated. The residue was purified by silica gel column (PE/EA= 5:1) to give III-3-2 (500 mg, yield: 48%) as a colorless oil. ESI-MS m/z :327(M+H).

References:

WO2018/106818,2018,A1 Location in patent:Paragraph 0253