Triethylamine → N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydro-6-p-tolylpyrido[4,3-d]pyrimidin-4-amine

HRID 19640

반응식

HRID 19640 반응식
[F:1][C:2]([F:21])([F:20])[C:3]1[CH:8]=[CH:7][C:6]([NH:9][C:10]2[C:11]3[CH2:19][NH:18][CH2:17][CH2:16][C:12]=3[N:13]=[CH:14][N:15]=2)=[CH:5][CH:4]=1.B(O)(O)[C:23]1[CH:24]=[CH:25][C:26]([CH3:29])=[CH:27][CH:28]=1.C(N(CC)CC)C>C1COCC1.CC([O-])=O.CC([O-])=O.[Cu+2]>[F:21][C:2]([F:1])([F:20])[C:3]1[CH:8]=[CH:7][C:6]([NH:9][C:10]2[C:11]3[CH2:19][N:18]([C:23]4[CH:28]=[CH:27][C:26]([CH3:29])=[CH:25][CH:24]=4)[CH2:17][CH2:16][C:12]=3[N:13]=[CH:14][N:15]=2)=[CH:5][CH:4]=1

참가 물질

6

반응물 3

HCID 8471TriethylamineHCID 79799Tolylboronic acidHCID 59346476(5,6,7,8-Tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(4-trifluoromethylphenyl)amine

생성물 1

HCID 59346575N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydro-6-p-tolylpyrido[4,3-d]pyrimidin-4-amine수율 10%

시약·촉매·용매 2

HCID 8895Cupric acetate촉매HCID 8028Tetrahydrofuran용매

실험 절차

N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydropyrido[4,3-d]pyrimidin-4-amine (100 mg, 0.34 mmol) was dissolved in anhydrous THF (2 mL). To the mixture was added p-tolylboronic acid (92 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 a vacuum. The residue was purified using a gradient of ethyl acetate:hexane (0-100%) to give the desired compound as reddish powder (12.8 mg, 10%).

후처리

  1. customthe solvent was removed under a vacuum
  2. customThe residue was purified

출처 및 근거

ORD 기록
ord-e68bec18c32d459c942382960dc28569
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07745451B2

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