تفاعل #53377

ord-caf4dde1c11c45898643f7297c5d373e

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    workup.STIRRINGthe mixture was stirred
  2. 2
    درجة الحرارةat reflux for 3 h
  3. 3
    درجة الحرارةThe solution was then cooled to room temperature
  4. 4
    أخرىthe supernatant was isolated
  5. 5
    أخرىThe solvent was evaporated
  6. 6
    غسيلthe residual oil was washed with ether (2×50 mL), ethyl acetate (50 mL)
  7. 7
    workup.ADDITIONtreated with 20 ml of 10% HCl
  8. 8
    أخرىThe obtained solid was isolated by filtration
  9. 9
    أخرىthe precipitation of a yellow solid
  10. 10
    أخرىwhich was isolated by centrifugation
  11. 11
    غسيلwashed with ethyl acetate
  12. 12
    أخرىdried under vacuum

الإجراء التجريبي

Triethylamine (8 mL) was added to suspension of compound 14 (0.470 g, 2 mmol) in THF (40 mL) and the mixture was stirred at room temperature for 15 min. After this time 1-(3,5-diamino-6-chloropyrazinoyl-2-methyl-pseudothiourea hydroiodide (0.15 g, 0.4 mmol) was added and the mixture was stirred at reflux for 3 h. The solution was then cooled to room temperature and the supernatant was isolated. The solvent was evaporated and the residual oil was washed with ether (2×50 mL), ethyl acetate (50 mL) and treated with 20 ml of 10% HCl. The obtained solid was isolated by filtration and dissolved in MeOH (approx. 50 mL). Addition of ethyl acetate (20 mL) to the solution caused the precipitation of a yellow solid, which was isolated by centrifugation, washed with ethyl acetate and dried under vacuum to give compound 15 (48 mg, 31%) as a yellow solid. 1H NMR (300 MHz, DMSO-d6) δ1.80 (br s, 2H), 2.58 (m, 2H), 3.95 (br s, 4H), 6.70 (d, 2H), 7.03 (d, 2H), 7.48 (br. s, 2H), 8.80 (br s, 1H), 8.93 (br s, 1H), 9.32 (br s, 2H), 10.52 (s, 1H). APCI MS m/z=364 [C15H18ClN7O2+H]+.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US06858614B2uspto-grants-2005_02