Litigating Monetization and Patent Trolls: Evidence from the Patent Market

1H-isochromene-1-ones and isoquinoline-1(2H)-ones with carbonyl group in position 3: Features of synthetic approaches and transformation

“…Cyclization of ketone 100 formed from benzamide 101 (scheme 36) resulted in the formation of 3acetylisoquinolone 102. 60,61 Moreover, two methods are described for the transformation of product 100 into product 101 -through rearrangement of epoxide 103 (scheme 36a) 60 and oxidative cleavage of β-diketone 104 (Scheme 35b). 61 Scheme 36.…”

“…60,61 Moreover, two methods are described for the transformation of product 100 into product 101 -through rearrangement of epoxide 103 (scheme 36a) 60 and oxidative cleavage of β-diketone 104 (Scheme 35b). 61 Scheme 36. Synthesis of 3-acetyl-8-chloro-2-phenylisoquinolin-1(2H)-one (102).…”

“…The formation of the Schiff base based on the acetyl group of isoquinolone 135 followed by asymmetric reduction of the imine was patented as a method for the synthesis of Duvelisib 136 -leukemia and lymphoma treatment drug (Scheme 47). 60,61 Moreover, two alternative methods for reducing imine 137 in the presence of chiral catalysts were developed: catalytic hydrogenation 60 and the action of trichlorosilane. 61 3-kinase (PI3K) inhibitors, which mentions the possibility of introducing new substituents into the isoquinoline fragment by coupling at positions 1 and 4 and reductive amination of the carbonyl group.…”