Patent ID: 9556172
Date: 2017-01-31
CPC Classifications: C07D,C07F

Claim:
1. A process for the manufacture of a compound of formula 1, comprising a) reacting a compound of formula 2 in the presence of a palladium catalyst, a base, and a compound of formula 3 in a Suzuki-Miyaura reaction to give a compound of formula 4 b) reacting the compound of formula 4 in the presence of a halogenation reagent to give a compound of formula 5 wherein X is I (5a) or Br (5b); and c) reacting the compound of formula 5 c-1) with a compound of formula (D); or c-2) with a compound of formula 7 in a Sonogashira reaction and then with a strong base; to give a compound of formula 8 d) reacting the compound of formula 8 in the presence of a compound of formula 9 and under conditions of a Friedel-Crafts Acylation to give the compound of formula 1, wherein R 1 , R 2 , R 3 , and R 4 are all methyl, or together with the carbon atoms to which they are attached form a phenyl ring; and R 5 is —(C1-C6)alkyl or benzyl.