1-(tert-Butoxycarbonyl)-3-pyrrolidinol

24424-99-5

40499-83-0

83220-73-9

The general procedure for the synthesis of 1-tert-butoxycarbonyl-3-hydroxy-pyrrolidine from di-tert-butyl dicarbonate and 3-hydroxy-pyrrolidine was carried out as follows: firstly, (R)-3-pyrrolidinol (539 mg, 6.19 mmol) was converted to compound 16b to afford the colorless oily material (1.3 g, 100% yield). The spectral data of this compound were consistent with the expected structure and in accordance with literature reports (see Kucznierz, R. et al. J. Med. Chem. 1998, 41, 4983-4994). Subsequently, compound 16b was converted by reaction to compound 16c, again as a colorless oil. Next, compound 16c was converted by a two-step reaction to compound 16e, still a colorless oily substance. Finally, compound 16e was reacted to produce the target compound 16, which was rendered as a yellow oily substance.