Reaktion #41467

Reaktionsgleichung

(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

Lösungsmittel

NMP

Reaktionsbedingungen

Aufarbeitung

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

Vorschrift

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.

Quelle