1,4-Dioxane hydrochloride → (4-Aminomethyl-2-fluoro-phenyl)-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulen-9-yl)-methanone Hydrochloride

HRID 220943Notes

Reaction equation

HRID 220943 reaction equation
C(OC(=O)[NH:7][CH2:8][C:9]1[CH:14]=[CH:13][C:12]([C:15]([N:17]2[CH2:26][C:25]3[CH:24]=[N:23][N:22]([CH3:27])[C:21]=3[NH:20][C:19]3[CH:28]=[CH:29][CH:30]=[CH:31][C:18]2=3)=[O:16])=[C:11]([F:32])[CH:10]=1)(C)(C)C.[ClH:34].O1CCOCC1>>[ClH:34].[NH2:7][CH2:8][C:9]1[CH:14]=[CH:13][C:12]([C:15]([N:17]2[CH2:26][C:25]3[CH:24]=[N:23][N:22]([CH3:27])[C:21]=3[NH:20][C:19]3[CH:28]=[CH:29][CH:30]=[CH:31][C:18]2=3)=[O:16])=[C:11]([F:32])[CH:10]=1

Participants

3

Reactant 2

HCID 204431481,4-Dioxane hydrochlorideHCID 136128389[3-Fluoro-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzyl]-carbamic Acid Tert-butyl Ester

Product 1

HCID 136346643(4-Aminomethyl-2-fluoro-phenyl)-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulen-9-yl)-methanone HydrochlorideYield 97%

Procedure

[3-Fluoro-4-(3-methyl-4,10-dihydro-3H-2,3,4,9-tetraaza-benzo[f]azulene-9-carbonyl)-benzyl]-carbamic acid tert-butyl ester from Example E90.1 (1.25 g, 2.8 mmol) was re-acted with 4N HCl/dioxan using an analogous procedure to that described for Example E4.2 to yield the title compound (11.0 g, 97%).

Sources & evidence

ORD record
ord-8e7a2501a2774cb08ecff780806ebcfc
Source dataset
uspto-grants-2012_06
Patent number
US08202858B2

Reaction notes

Loading…