Abstract: The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/?O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

Abstract: A novel process for the preparation of compounds of formula I and optionally converting a compound of formula I into a pharmaceutically acceptable salt is disclosed. The compounds of formula I and the corresponding salts, e.g. the sodium salts, are pharmaceutically active substances. Processes for the creation of intermediates are also disclosed.

Abstract: The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described herein which comprises the steps of a) reacting a compound of formula with a compound of formula to form a compound of formula b) converting the OH/?O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl3, PBr3, MeI and (F3CSO2)2O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; c) substituting R2 for the leaving group P by reacting compound XV with HR2 to form a compound of formula and d) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula I The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

Abstract: A novel process for the preparation of compounds of formula I 1

Abstract: The present invention provides a process for the manufacture of pyrimidines of formula I: wherein R1, R2, R3 each independently represent hydrogen, C1-7-alkyl, or C1-7-alkoxy, A signifies —CN, a carbanionic R4-alkynyl residue, in which R4 is hydrogen or C1-7-alkyl, or a carbanionic residue of the malonic acid derivative of formula III  in which B and B′ independently represent —CN, —COOR5, or —C(O)R5, wherein R5 is alkyl or aryl.