Process for preparation of pyridine derivatives

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C544S060000, C544S124000, C544S360000

Reexamination Certificate

active

10888912

ABSTRACT:
The present invention relates to a process for the manufacture of compounds of formulawherein the substituents are as described hereinwhich comprises the steps ofa) reacting a compound of formulawith a compound of formulato form a compound of formulab) 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 formulawherein P is halogen or trifluoromethanesulfonate;c) substituting R2for the leaving group P by reacting compound XV with HR2to form a compound of formulaandd) hydrolyzing the nitrile function in an acidic medium selected from H2SO4, HCl and acetic acid, to form a compound of formula IThe compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

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