Reacción #41467

Ecuación de reacción

(1R,2S)-1-(3,4-dimethylphenyl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-amine

5-methyl-1,3-thiazole-2-carboxylic acid

HATU

DIEA

→

N-[(1R,2S)-1-(3,4-dimethylphenyl)-1-[1-(4-fluorophenyl)indazol-5-yl]oxy-propan-2-yl]-5-methyl-1,3-thiazole-2-carboxamide

Disolventes

NMP

Condiciones de reacción

Tratamiento posterior

1. 1
   Otroprepared analogously to Example 6a with corresponding starting material)
2. 2
   workup.ADDITIONwas added
3. 3
   Otrowas evaporated under reduced pressure
4. 4
   Otropurified by semi-prep

Procedimiento

5-methyl-1,3-thiazole-2-carboxylic acid (29 mg, 0.2 mmol) was dissolved in NMP (1 mL) together with HATU (76 mg, 0.2 mmol) and DIEA (133 uL, 0.8 mmol). The mixture was stirred in r.t. for 5 min before (1R,2S)-1-(3,4-dimethylphenyl)-1-(1-(4-fluorophenyl)-1H-indazol-5-yloxy)propan-2-amine (58 mg, 0.15 mmol, prepared analogously to Example 6a with corresponding starting material) was added. The reaction mixture was stirred in r.t. overnight before it was evaporated under reduced pressure and purified by semi-prep. HPLC.

Fuente