Reaktion #1340962

Reaktionsgleichung

5-cyclopentyl-6-(2,2,2-trifluoro-ethoxy)-pyridin-3-ylamine

5-methyl-4-oxazolecarboxylic acid

DIPEA

HATU

→

title compound

Ausbeute 21.4%

5-methyl-oxazole-4-carboxylic acid [5-cyclopentyl-6-(2,2,2-trifluoro-ethoxy)-pyridin-3-yl]-amide

Ausbeute 21.4%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   workup.STIRRINGthe reaction mixture was stirred at 25° C. for 12 h
2. 2
   SonstigeVolatiles were removed in vacuo
3. 3
   Sonstigethe resultant residue was purified by prep-HPLC

Vorschrift

To a solution of 5-methyl-4-oxazolecarboxylic acid (CAN 103879-58-9) (73 mg, 0.57 mmol) in DMF (4 mL) were added DIPEA (0.1 mL, 1.15 mmol) and HATU (219 mg, 0.57 mmol) at 25° C. The reaction mixture was stirred for 30 min at 25° C. Then, 5-cyclopentyl-6-(2,2,2-trifluoro-ethoxy)-pyridin-3-ylamine (Example 1c) (100 mg, 0.38 mmol) was added and the reaction mixture was stirred at 25° C. for 12 h. Volatiles were removed in vacuo and the resultant residue was purified by prep-HPLC to get the title compound (30 mg, 21.3%) as off-white solid. MS (ESI): 370 [M+H]+.

Quelle