| 摘要 |
<p>The present invention relates to a process for the manufacture of compounds of general formula wherein the substituents are as described in claim I characterized in that it comprises the steps of a) reacting a compound of formula (X), with a compound of formula (Xiii), to a compound of formula (XIVa), (XIV),b) converting the OH/=O function of compounds of formula XIV/XlVa into a leaving group P with a reagent containing a leaving group, selected from the group comprising POCl3, PBr3, Mel or (F3CS02)2O to form a compound of formula (XV), wherein P is halogen or trifluoromethanesulfonate, c) substituting the leaving group P by R2 with HR2 to form a compound of formula (XVI) d) hydrolyzing the nitrile function in an acidic medium comprising H2SO4, HCI or acetic acid, to a compound of formula (I)The compouds of formula I are valuable intermediate for the manufacture of therapeutically active compounds which have NK- I antagonist activity.</p> |
