Morpholin-4-ylmalononitrile → 2-[1-(2-Fluorobenzyl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazol-3-yl]-5-(morpholin-4-yl)pyrimidine-4,6-diamine

HRID 1482925ノート

反応式

HRID 1482925 の反応式
[F:1][C:2]1[CH:19]=[CH:18][CH:17]=[CH:16][C:3]=1[CH2:4][N:5]1[C:9]2[CH2:10][CH2:11][CH2:12][C:8]=2[C:7]([C:13](=[NH:15])[NH2:14])=[N:6]1.[N:20]1([CH:26]([C:29]#[N:30])[C:27]#[N:28])[CH2:25][CH2:24][O:23][CH2:22][CH2:21]1>[Au].C(Cl)Cl>[F:1][C:2]1[CH:19]=[CH:18][CH:17]=[CH:16][C:3]=1[CH2:4][N:5]1[C:9]2[CH2:10][CH2:11][CH2:12][C:8]=2[C:7]([C:13]2[N:14]=[C:27]([NH2:28])[C:26]([N:20]3[CH2:21][CH2:22][O:23][CH2:24][CH2:25]3)=[C:29]([NH2:30])[N:15]=2)=[N:6]1

参加物

5

反応物 2

HCID 9898879Morpholin-4-ylmalononitrileHCID 866920921-(2-Fluorobenzyl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole-3-carboximidamide

生成物 1

HCID 900131242-[1-(2-Fluorobenzyl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazol-3-yl]-5-(morpholin-4-yl)pyrimidine-4,6-diamine

試薬・触媒・溶媒 2

HCID 23985Gold触媒HCID 6344Dichloromethane溶媒

反応条件

温度
105 °C

実験手順

75 mg of 1-(2-fluorobenzyl)-1,4,5,6-tetrahydrocyclopenta[c]pyrazole-3-carboximidamide 1-2-4 (0.29 mmol, 1.0 eq.) and 44 mg morpholin-4-ylmalononitrile [0.29 mmol, 1.0 eq.; for preparation see: H. Gold and O. Bayer, Chem. Ber. 94, 2594 (1961)] were suspended in a small amount of DCM and the resulting suspension was evaporated to dryness. The residue was heated for one h at 105° C. The crude product was purified by flash chromatography yielding 86 mg (0.21 mmol, 72%) of analytically pure target compound.

後処理

  1. customfor preparation
  2. customthe resulting suspension was evaporated to dryness
  3. customThe crude product was purified by flash chromatography
  4. customyielding 86 mg (0.21 mmol, 72%) of analytically pure target compound

出典と根拠

ORDレコード
ord-663f5e82f3074c0e979d5eca389876bd
出典データセット
uspto-grants-2016_08
特許番号
US09416125B2

反応ノート

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