Reaktion #1132688

Reaktionsgleichung

compound 276

5-(3-Amino-1-methyl-1H-indazol-6-yloxy)-3-(4-methoxy-benzyl)-3,4-dihydro-1H-pyrido[2,3-d]pyrimidin-2-one

1-(4-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid

N,N-diisopropylethylamine

→

278

Ausbeute 18.9%

1-(4-Fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylicacid{6-[3-(4-methoxy-benzyl)-2-oxo-1,2,3,4-tetrahydro-pyrido[2,3-d]pyrimidin-5-yloxy]-1-methyl-1H-indazol-3-yl}-amide

Ausbeute 18.9%

Lösungsmittel

DMF

Reaktionsbedingungen

Aufarbeitung

1. 1
   EinengenThe reaction was concentrated
2. 2
   workup.DISSOLUTIONredissolved in DMSO
3. 3
   Sonstigepurified via prep HPLC

Vorschrift

A solution of compound 276 (100.00 mg; 0.23 mmol; 1.00 eq.), 1-(4-fluoro-phenyl)-2-oxo-1,2-dihydro-pyridine-3-carboxylic acid (59.59 mg; 0.26 mmol; 1.10 eq.), pybop (157.16 mg; 0.30 mmol; 1.30 eq.), DMF (4.00 ml), and N,N-diisopropylethylamine (115.48 μl; 0.70 mmol; 3.00 eq.) was stirred at room temperature for 22 hours. The reaction was concentrated, redissolved in DMSO and purified via prep HPLC to afford 28 mg (16%) of 278 as an off-white solid. LC-MS (M+H=646, obsd.=646).

Quelle