تفاعل #75934

ord-e0c7ff00a2bb40d1a7fb4b190f05e632

معادلة التفاعل

OO
hydrogen peroxide
COc1ccc(B(O)O)cc1
4-Methoxy-benzeneboronic acid
Cc1oc(-c2ccc(C(F)(F)F)cc2)nc1-c1ccc(Br)cc1
4-(4-bromo-phenyl)-5-methyl-2-(4-trifluoromethyl-phenyl)-oxazole
O=C([O-])[O-].[Na+].[Na+]
sodium carbonate
COc1ccc(-c2ccc(-c3nc(-c4ccc(C(F)(F)F)cc4)oc3C)cc2)cc1
solid
المردود 82.2%
COc1ccc(-c2ccc(-c3nc(-c4ccc(C(F)(F)F)cc4)oc3C)cc2)cc1
4-(4′-Methoxy-biphenyl-4-yl)-5-methyl-2-(4-trifluoromethyl-phenyl)-oxazole
المردود 82.2%

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    درجة الحرارةThe reaction mixture was refluxed for 12 hours
  2. 2
    استخلاصextracted with ethyl acetate
  3. 3
    تجفيفThe organic extracts were dried over MgSO4
  4. 4
    أخرىEvaporation and crystallization from hexanes/ethyl ether

الإجراء التجريبي

4-Methoxy-benzeneboronic acid (1.44 g, 7.19 mmol) in ethyl alcohol (5 mL) was added into a mixture of 4-(4-bromo-phenyl)-5-methyl-2-(4-trifluoromethyl-phenyl)-oxazole (2.5 g, 6.54 mmol), sodium carbonate (2N, 6.5 mL), tetrakis(triphenylphosphine)palladium(0) (0.23 g, 0.196 mmol), and toluene (200 mL). The reaction mixture was refluxed for 12 hours, cooled to room temperature, and treated with hydrogen peroxide (30%, 5 mL) for 1 hour. Then, the mixture was poured into water and extracted with ethyl acetate. The organic extracts were dried over MgSO4. Evaporation and crystallization from hexanes/ethyl ether gave a white solid (2.2 g, 82% yield): mp 167-168° C.; MS m/e 409 (M+);

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US06699896B1uspto-grants-2004_03