IP Library › Granted Patent US 10,435,386
Granted Patent B2
US 10,435,386 · App. 15/419,618 · Granted Oct 8, 2019

Regioselective N-2 arylation of indazoles

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Quick Facts
Patent No.
US 10,435,386
App. No.
15/419,618
Granted
Oct 8, 2019
Kind
B2
Abstract

A novel process is provided for the efficient preparation of an asymmetric compound of structural formula I: comprising a copper-catalyzed, carbon-nitrogen cross-coupling step. The process described as part of the present invention can be used to manufacture poly (ADP-ribose) polymerase (PARP) inhibitors, which may be useful for the treatment of cancer. In particular, the present invention describes a process for the manufacture of the PARP inhibitor, 2-{4-[(3S)-piperidin-3-yl]phenyl}-2H-indazole-7-carboxamide.

Claims (4)

1. A compound of formula II:

wherein R 1 is

2. A compound of formula II:

wherein R 1 is

Assignments (1)
MERGER Recorded Aug 8, 2022
From: MERCK SHARP & DOHME CORP.
To: MERCK SHARP & DOHME LLC
Reel/Frame 061102/0145 →