تفاعل #60039

ord-8ed17032505b4da7991e349eff3a4437

المذيبات

ظروف التفاعل

درجة الحرارة
100°CELSIUS
الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىUpon completion, the reaction was partitioned with water (50 ml) and dichloromethane (250 ml)
  2. 2
    أخرىThe organic layer was separated
  3. 3
    غسيلwashed with water (2×50 ml), brine (50 ml), dried Na2SO4
  4. 4
    ترشيحfiltered
  5. 5
    تركيزconcentrated under reduced pressure
  6. 6
    أخرىThe product was purified by flash chromatography
  7. 7
    غسيلeluting with 10% methanol in dichloromethane
  8. 8
    أخرىdrying in vacuo

الإجراء التجريبي

4-[(2E)-3-(dimethylamino)-2-imidazolylprop-2-enoyl]benzenecarbonitrile (6 M) in NMP (5 ml) was added to a stirred mixture of N-[2-(amidinoamino)ethyl](tert-butoxy)carboxamide, hydrochloride (3 M) and Cs2CO3 (2.4) in NMP (15 ml). The reaction was heated to 100° C. for 48 hours. The reaction was followed by HPLC. Upon completion, the reaction was partitioned with water (50 ml) and dichloromethane (250 ml). The organic layer was separated and washed with water (2×50 ml), brine (50 ml), dried Na2SO4, filtered, and concentrated under reduced pressure. The product was purified by flash chromatography eluting with 10% methanol in dichloromethane. After stripping off the solvents and drying in vacuo, (tert-butoxy)-N-(2-{[4-(4-cyanophenyl)-5-imidazolylpyrimidin-2-yl]amino}ethyl)carboxamide was obtained as a dark red glass in 83% yield.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07425557B2uspto-grants-2008_09