Process for the preparation of 4-(4-(4-(hydroxybiphenyl)-1-piperidinyl)-1-hydroxybutyl)- alpha , alpha -dimethylphenylacetic acid and phosphorylated derivatives

摘要

The invention relates to the preparation of the compound 4-(4-(4-(hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)- alpha , alpha -dimethylphenylacetic acid and its phosphorylated derivatives. These compounds can be prepared from alpha -(p-tert-butylphenyl)-4-( alpha -hydroxy- alpha -phenylbenzyl)-1-piperidinylbutanol with the aid of fungi of the genus Cunninghamella or Absidia. The compounds according to the present invention can be used as pharmaceuticals for the treatment of allergic disorders, allergic rhinitis or asthma. Compounds of the formula II in which R1 is -CH2-O-P(O)(OH)2 and R2 is -OH; R1 is -CH3 and R2 is -O-P(O)(OH)2; or R1 is -COOH and R2 is -O-P(O)(OH)2 are produced by the process according to the present invention and are suitable as pharmaceuticals with antihistamine action.