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

HRID 535360

反応式

HRID 535360 の反応式
[N:1]1[C:6]2[CH2:7][CH2:8][NH:9][CH2:10][C:5]=2[C:4]([NH:11][C:12]2[CH:17]=[CH:16][C:15]([C:18]([F:21])([F:20])[F:19])=[CH:14][CH:13]=2)=[N:3][CH:2]=1.[C:22]1(B(O)O)[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=1.C(N(CC)CC)C>C1COCC1.CC([O-])=O.CC([O-])=O.[Cu+2]>[F:21][C:18]([F:20])([F:19])[C:15]1[CH:14]=[CH:13][C:12]([NH:11][C:4]2[C:5]3[CH2:10][N:9]([C:22]4[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=4)[CH2:8][CH2:7][C:6]=3[N:1]=[CH:2][N:3]=2)=[CH:17][CH:16]=1

参加物

6

反応物 3

HCID 8471TriethylamineHCID 66827Phenylboronic AcidHCID 59346476(5,6,7,8-Tetrahydro-pyrido[4,3-d]pyrimidin-4-yl)-(4-trifluoromethylphenyl)amine

生成物 1

HCID 59346458N-(4-(Trifluoromethyl)phenyl)-5,6,7,8-tetrahydro-6-phenylpyrido[4,3-d]pyrimidin-4-amine収率 6.4%

試薬・触媒・溶媒 2

HCID 8895Cupric acetate触媒HCID 8028Tetrahydrofuran溶媒

実験手順

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 (0-400%) to give the desired compound as reddish powder (8.0 mg, 6.0%).

後処理

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

出典と根拠

ORDレコード
ord-4df0aec07f6d49e5b00e1365dd63b1eb
出典データセット
uspto-grants-2014_10
特許番号
US08859545B2

関連ノート

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