تفاعل #2446153

ord-c1ee5f8842994fdf86ae09aaa52663a9

معادلة التفاعل

O=C1CCc2cc(-c3cccnc3)ccc2N1
6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one
O=C1CCC(=O)N1Cl
N-chlorosuccinimide
O=C1CCc2cc(-c3cccnc3)cc(Cl)c2N1
8-Chloro-6-pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    استخلاصextracted with ethyl acetate (3×50 ml)
  2. 2
    غسيلThe combined organic layers were washed with water and brine
  3. 3
    تجفيفdried over MgSO4
  4. 4
    أخرىthe solvent was evaporated in vacuo

الإجراء التجريبي

To a solution of 6-Pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one (560 mg, 2.50 mmol) in 5 ml dry DMF was added N-chlorosuccinimide (368 mg, 2.75 mmol) in 5 ml dry DMF over a period 2 h at 65° C. After additional 3 h at 65° C., the mixture was poured into 75 ml ice water and extracted with ethyl acetate (3×50 ml). The combined organic layers were washed with water and brine, dried over MgSO4 and the solvent was evaporated in vacuo. 8-Chloro-6-pyridin-3-yl-3,4-dihydro-1H-quinolin-2-one was obtained after flash chromatography on silica gel (hexanes/ethyl acetate, 3/7, Rf=0.15) and crystallization from acetone/diethylether as colorless needles (225 mg, 0.87 mmol, 35%), mp (acetone/diethylether) 178° C. 1H-NMR (500 MHz, DMSO-d6): δ=2.54 (m, 2H), 3.01 (m, 2H), 7.45 (ddd, 3J=8.0 Hz, 3J=4.8 Hz, 5J=0.8 Hz, 1H), 7.60 (d, 4J=2.0 Hz, 1H), 7.69 (d, 4J=2.0 Hz, 1H), 8.06 (ddd, 3J=8.0 Hz, 4J=2.5 Hz, 4J=1.5 Hz, 1H), 8.53 (dd, 3J=4.8 Hz, 4J=1.5 Hz, 1H), 8.88 (dd, 4J=2.5 Hz, 5J=0.8 Hz, 1H), 9.64 (s, 1H). 13C-NMR (125 MHz, DMSO-d6): δ=25.3, 30.3, 119.7, 123.8, 125.0, 125.6, 127.4, 131.7, 133.7, 133.8, 134.8, 147.3, 152.4, 170.3. MS m/z 258.95 (M+).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US08685960B2uspto-grants-2014_04