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US 9,790,206 B2Granted
Intermediates for use in the preparation of indazole derivatives and processes for the preparation thereof
AssigneeArray BioPharma Inc.
InventorsC. Todd Eary, Bruno P. Hache, Derrick Juengst, Stacey Renee Spencer, Peter J. Stengel, Daniel John Watson
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Abstract
Provided herein are novel processes for preparing a compound of Formula (I) to the use of said compound as an intermediate in novel processes for the synthesis of indazole derivatives, and to indazole intermediates and derivatives prepared by the processes described herein.
Claims35
A process for the preparation of a compound of formula I
- comprising:
- (a) reacting a compound of formula (2)
- where X is Br or I, with 2-hydrazinylethanol in the presence of a base and a transition metal catalyst to provide a compound of formula (3)
- and
- (b) reducing the nitrile group of compound (3) to provide said compound of Formula I.
2 more elements
A process for preparing a Compound (A) having the formula
- comprising:
- (a) reacting a compound of formula (2)
- where X is Br or I, with 2-hydrazinylethanol in the presence of a base and a transition metal catalyst to provide a compound of formula (3)
- (b) reducing the nitrile group of compound (3) to provide a compound of Formula I
- (c) coupling said compound of Formula I with a compound of formula (4)
- where Z represents a leaving group, to provide said Compound (A);
- and
- (c) optionally treating the product of Step (d) with HCl to isolate Compound (A) as the monohydrochloride salt.
5 more elements
Dependencies are inferred from the claim text.