تفاعل #47915

ord-c5c8838fa6d540bc9becc3ac0dc4c426

معادلة التفاعل

FC(F)(F)c1ccc(Nc2ncnc3c2CNCC3)cc1
(5,6,7,8-Tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(4-trifluoromethylphenyl)amine
OB(O)c1ccccc1
phenylboronic acid
CCN(CC)CC
triethylamine
FC(F)(F)c1ccc(Nc2ncnc3c2CN(c2ccccc2)CC3)cc1
desired compound
المردود 6.4%
FC(F)(F)c1ccc(Nc2ncnc3c2CN(c2ccccc2)CC3)cc1
N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydro-6-phenylpyrido[4,3-d]pyrimidin-4-amine
المردود 6.4%

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىthe solvent was removed under the vacuum
  2. 2
    أخرىThe residue was purified

الإجراء التجريبي

The (5,6,7,8-Tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(4-trifluoromethylphenyl)amine (100 mg, 0.34 mmol) was dissolved in anhydrous THF (2 mL). To the mixture was added phenylboronic acid (83 mg, 0.68 mmol), Cu(OAc)2 (124 mg, 0.68 mmol) and triethylamine (0.68 g, 0.095 mL). The mixture was agitated for 6 h and the solvent was removed under the vacuum. The residue was purified using a gradient of ethyl acetate:hexane (0-100%) to give the desired compound as reddish powder (8.0 mg, 6.0%).

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US07745451B2uspto-grants-2010_06