(S)-1-(Tetrahydro-2H-pyran-4-yl)pyrrolidin-3-aMine synthesis

Yield:791758-82-2 90%

Reaction Conditions:

with trifluoroacetic acid in water at 25; for 1 h;

Steps:

4.b

11.66 g (43.12 mmol) tert-butyl [(S)-1-(tetrahydro-pyran-4-yl)-pyrrolidin-3-yl]-carbamate are dissolved in 80 ml trifluoroacetic acid while cooling with water. The mixture is stirred for 1 h at 25° C. and the solvent is then eliminated in vacuo. The residue is dissolved in a mixture of ether and isopropanol. This solution is combined with isopropanolic hydrochloric acid. A precipitate settles out. This is suction filtered and dried. Yield: 9.47 g (38.97 mmol, 90%) MS (ESI): 171 (M+H)⁺

References:

US2006/47118,2006,A1 Location in patent:Page/Page column 10