تفاعل #49694

ord-1ba716dc820347e494732209b62094f7

معادلة التفاعل

Clc1ccc2c(c1)CCc1cccnc1C2N1CCNCC1
(-)-8-chloro-6,11-dihydro-11-(4-piperazinyl)-5H-benzo[5,6]cyclohepta-[1,2-b]pyridine
[O-][n+]1ccc(CO)cc1
4-pyridylcarbinol N-oxide
BrC(Br)(Br)Br
carbon tetrabromide
CCN(CC)CC
triethylamine
c1ccc(P(c2ccccc2)c2ccccc2)cc1
triphenylphosphine
Clc1ccc2c(c1)CCc1cccnc1C2N1CCN(Cc2ccncc2)CC1
(-)-8-chloro-6,11-dihydro-11-[4 -(4-pyridinylmethyl)-1-piperazinyl]-5h-benzo[5,6]cyclohepta-[1,2-b]pyridine
المردود 45.3%

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    غسيلwashed once with 0.5M aqueous sodium bicarbonate
  2. 2
    تجفيفThe organic portion was dried over sodium sulfate
  3. 3
    ترشيحfiltered
  4. 4
    تركيزconcentrated in vacuo
  5. 5
    أخرىThe residue was purified via flash chromatography (4% methanol saturated with ammonia in methylene chloride)

الإجراء التجريبي

To a mixture of 188 mg (1.50 mmol) of 4-pyridylcarbinol N-oxide and 497 mg (1.50 mmol) of carbon tetrabromide in 12 mL of dry methylene chloride at room temperature and under an argon atmosphere was added in one portion 393 mg (1.50 mmol) of triphenylphosphine. After 40 minutes, 313 mg (0.997 mmol) of (-)-8-chloro-6,11-dihydro-11-(4-piperazinyl)-5H-benzo[5,6]cyclohepta-[1,2-b]pyridine was added followed by 209 mL (1.57 mmol) of triethylamine. The reaction mixture was then allowed to stir at room temperature for 3 hr, after which it was taken up in methylene chloride and washed once with 0.5M aqueous sodium bicarbonate and then brine. The organic portion was dried over sodium sulfate, filtered and concentrated in vacuo. The residue was purified via flash chromatography (4% methanol saturated with ammonia in methylene chloride) to provide 183 mg of (-)-8-chloro-6,11-dihydro-11-[4 -(4-pyridinylmethyl)-1-piperazinyl]-5h-benzo[5,6]cyclohepta-[1,2-b]pyridine, N-oxide as a glass: MS (CI) m/z 421 (M+ +1);

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US05422351uspto-grants-1995_06