We herein report an asymmetric synthesis of α, α-disubstituted α-amino alcohol derivatives 3, key intermediates of a novel immunomodulator, using enzymatic desymmetrization of 2- alkyl-2-tert-butoxycarbonylamino-1, 3-propanediols 1a and 1b. This method makes it possible to prepare a chiral analogue of FTY720 4. These synthetic procedures allow for a broad structure variation in order to evaluate structure–activity relationships and the ...