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4,4-Difluoro-L-proline Methyl ester trifluoroacetate synthesis

4synthesis methods
-

Yield:915230-14-7 77%

Reaction Conditions:

for 0.5 h;

Steps:

50(C)

(S)-4,4-Difluoro-N-Boc-pyrrolidine-2-carboxylic acid methyl ester (1.08 g, 4.07 mmol) was dissolved in TFA (5 mL) and stirred under N2 for 30 min. The solvent was removed under vacuum and the residue dissolved in MeOH5 loaded onto an SCX ion exchange column, washed with MeOH and DCM then eluted with 5% NH3 in MeOH. The solvent was removed to give the product as a pale brown oil. Yield: 77%; LCMS (RT): 0.63 min (Method A); MS (ES+) gave m/z: 166 (MH+).

References:

WO2006/123257,2006,A2 Location in patent:Page/Page column 71