Methyl (R)-1-Boc-4,4-difluoropyrrolidine-2-carboxylate synthesis
- Product Name:Methyl (R)-1-Boc-4,4-difluoropyrrolidine-2-carboxylate
- CAS Number:647857-74-7
- Molecular formula:C11H17F2NO4
- Molecular Weight:265.25
256487-77-1
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647857-74-7
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Yield: 98%
Reaction Conditions:
with diethylamino-sulfur trifluoride in dichloromethane at -78 - 27; for 16 h;
Steps:
(R)-1-tert-Butyl 2-methyl 4-oxopyrrolidine-1,2-dicarboxylate (5.00 g, 20.5 mmol) was dissolved in DCM (15 mL) at -78 00 and DAST was added (8.1 mL, 30.8 mmol)dropwise. Reaction mixture was warmed to rt and stirred for 16 h. Reaction mixture diluted with DCM (100 mL) and washed with saturated NaHCO3 (aq) (2 x 100 mL),combined aqueous layers washed with DCM (100 mL), the organic layers were combined, dried (Na2SO4) and solvents were removed in vacuo to give (R)-1-tert-Butyl 2-methyl 4,4-difluoropyrrolidine-1,2-dicarboxylate (5.34 g, 98%) as an yellow oil.LCMS (Method F): m/z 210 (M+H-56) (ES), at 2.17 min UV inactive
References:
HEPTARES THERAPEUTICS LIMTED;BROWN, Giles Albert;CONGREVE, Miles Stuart;PICKWORTH, Mark;RACKHAM, Mark;TEHAN, Benjamin Gerald WO2017/21728, 2017, A1 Location in patent:Page/Page column 51; 52
114676-69-6
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647857-74-7
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114676-59-4
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647857-74-7
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2584-71-6
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647857-74-7
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135042-12-5
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647857-74-7
66 suppliers
$185.00/1g