Reaktion #73351

Reaktionsgleichung

5-(5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidin-4-yloxy)-indole-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide

bromo tert-butylacetate

→

title compound

{4-[1-(3-Trifluoromethyl-phenylcarbamoyl)-1H-indol-5-yloxy]-5,8-dihydro-6H-pyrido[3,4-d]pyrimidin-7-yl}-acetic acid tert-butyl ester

Lösungsmittel

ACN

Reaktionsbedingungen

Aufarbeitung

1. 1
   Sonstigecompletion of the reaction the contents of the flask
2. 2
   Sonstigeare partitioned between DCM and brine
3. 3
   TrocknenOrganic layer is dried over anhydrous Na2SO4
4. 4
   Einengenconcentrated
5. 5
   Sonstigethe residue is separated via FCC (50-100% EtOAc/heptane)

Vorschrift

A solution of 5-(5,6,7,8-tetrahydro-pyrido[3,4-d]pyrimidin-4-yloxy)-indole-1-carboxylic acid (3-trifluoromethyl-phenyl)-amide, Example 33-C, (250 mg, 0.55 mmol), bromo tert-butylacetate (204 μL, 1.38 mmol), TEA (384 μL, 2.76 mmol) and ACN (5 mL) is stirred at room temperature. Following completion of the reaction the contents of the flask are partitioned between DCM and brine. Organic layer is dried over anhydrous Na2SO4, concentrated, and the residue is separated via FCC (50-100% EtOAc/heptane) to give the title compound. MS (ESI) m/z 568.1 (M+1).

Quelle