Prepn. of 2,7-di:amino:tetralin mandelate(s) pure enantiomer - used to treat disorders of blood pressure, heart rhythm, prolactin secretion and central nervous system

摘要

Prepn. of enantiomerically pure (2R)-2,7-diaminotetraline-(R)-mandelate (Ia) or (2S)-2,7-diaminotetnaline (S)-mandelate (Ib) comprises: (a) dissolution or suspension of 2,7-diaminonapththalene (II) in an inert solvent, followed by hydrogenation of 80-120 deg.C and 1.1 x 10 power 7 - 1.4 x 10 power 7 Pa in the presence of a catalyst; (b) removal of the catalyst and treatment of the reaction soln. with a soln. of R(-)- or S(+)- mandelic acid in an inert solvent; and 9c) addn. of a non-solvent, cooling of the mixt. to -10 to 10 deg.C and isolation and purifcn. of the pptd. mandelate cpd. USE/ADVANTAGE - Ia and Ib are agents used to treat disorders of blood pressure, heart rhythm, prolactin secretion and esp. the central nervous system. The process is simple and avoids problems encountered in, e.g. EP-361300, such as low yield.