Patent ID: 8039637
Filing Date: 2011-10-18
Classification: A61P,C07C,C07D

Abstract:
1. A process for preparing a compound of Formula Ia-1 and salts and solvates thereof, wherein: Z is —C(═O)OR or a moiety that can be transformed into any one of said Z groups; R R X X R or R R R R or R said method comprising: nitrating a compound having the Formula wherein X treating said compound of Formula II optionally at elevated temperatures and/or pressure with two or more equivalents of (i) a reagent that contains or generates ammonia, (ii) a primary or secondary amine other than an aromatic amine or (iii) a reagent that delivers a group that can subsequently be converted into an amine to provide a compound of Formula VI-11 wherein A is —NR wherein R reducing said compound of Formula VI-11 or VI-12 to provide a compound of Formula VIIa-1 wherein when A of Formula VI-11 or VI-12 is —NH-benzyl, —NHOR when R when R wherein X 6 is F, Cl, Br, I, —OSO 2 CF 3 , alkyl sulfonate, aryl sulfonate, alkylaryl sulfonate, —B(OR 8 ) 2 , —BF 3 or —Bi(R 1 ) 2 , optionally either (i) at elevated temperature and optionally in the presence of a base, or (ii) in the presence of a metal-based catalyst and a base, to provide said compound of Formula Ia-1.