Methylamine → 2-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine

HRID 2370237

反応式

HRID 2370237 の反応式
[Cl:1][C:2]1[N:3]=[C:4](Cl)[C:5]2[CH2:10][CH2:9][CH:8]([C:11]3[CH:12]=[N:13][C:14]([C:17]([F:20])([F:19])[F:18])=[CH:15][CH:16]=3)[C:6]=2[N:7]=1.[CH3:22][NH2:23]>CN1C(=O)CCC1>[Cl:1][C:2]1[N:3]=[C:4]([NH:23][CH3:22])[C:5]2[CH2:10][CH2:9][CH:8]([C:11]3[CH:12]=[N:13][C:14]([C:17]([F:20])([F:19])[F:18])=[CH:15][CH:16]=3)[C:6]=2[N:7]=1

参加物

4

反応物 2

HCID 6329MethylamineHCID 580757202,4-dichloro-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine

生成物 1

HCID 580756152-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine収率 24.64%

試薬・触媒・溶媒 1

HCID 13387N-methyl-2-pyrrolidone溶媒

実験手順

To a solution of 2,4-dichloro-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidine (33 mg, 0.099 mmol) in NMP (Volume: 5 mL) was added methanamine (0.247 mL, 0.494 mmol). The reaction mixture was stirred at room temperature for 2 h. The product was partitioned between ethyl acetate & water. The organic layers were combined and dried in vacuum to afford 2-chloro-N-methyl-7-(6-(trifluoromethyl)pyridin-3-yl)-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-amine (8 mg, 0.024 mmol, 24.64% yield). LC-MS (M+H)+=329.0.

後処理

  1. customThe product was partitioned between ethyl acetate & water
  2. customdried in vacuum

出典と根拠

ORDレコード
ord-02c9919fff1c4ec9b212cb1a562389d3
出典データセット
uspto-grants-2014_04
特許番号
US08710061B2

関連ノート

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