Ammonia → 1-[2-(2-Chloro-benzylamino)-pyrido[4,3-d]pyrimidin-5-yl]-piperidine-4-carboxylic acid ethyl ester

HRID 41483ノート

反応式

HRID 41483 の反応式
[Cl:1][C:2]1[CH:20]=[CH:19][CH:18]=[CH:17][C:3]=1[CH2:4][NH:5][C:6]1[N:7]=[CH:8][C:9]2[C:15](Cl)=[N:14][CH:13]=[CH:12][C:10]=2[N:11]=1.[CH2:21]([O:23][C:24]([CH:26]1[CH2:31][CH2:30][NH:29][CH2:28][CH2:27]1)=[O:25])[CH3:22].N.O>C1COCC1>[CH2:21]([O:23][C:24]([CH:26]1[CH2:31][CH2:30][N:29]([C:15]2[C:9]3[CH:8]=[N:7][C:6]([NH:5][CH2:4][C:3]4[CH:17]=[CH:18][CH:19]=[CH:20][C:2]=4[Cl:1])=[N:11][C:10]=3[CH:12]=[CH:13][N:14]=2)[CH2:28][CH2:27]1)=[O:25])[CH3:22]

参加物

6

反応物 4

HCID 222AmmoniaHCID 962WaterHCID 70770Ethyl 4-piperidinecarboxylateHCID 58450134(2-Chloro-benzyl)-(5-chloro-pyrido[4,3-d]pyrimidin-2-yl)-amine

生成物 1

HCID 584501201-[2-(2-Chloro-benzylamino)-pyrido[4,3-d]pyrimidin-5-yl]-piperidine-4-carboxylic acid ethyl ester

試薬・触媒・溶媒 1

HCID 8028Tetrahydrofuran溶媒

反応条件

温度
100 °C

実験手順

(2-Chloro-benzyl)-(5-chloro-pyrido[4,3-d]pyrimidin-2-yl)-amine 9 (500 mg, 1.64 mmol), Piperidine-4-carboxylic acid ethyl ester 12 (0.51 mL, 3.28 mmol) and NH3 (25% solution in water, 0.22 mL, 3.28 mmol) were dissolved in THF (5 mL) and stirred at 100° C. in a high pressure flask for 15 hours. To the mixture water (5 mL) was added and the precipitate formed was filtered off and dried in vacuo. The obtained colorless solid (583 mg, 1.37 mmol, 84%) was used without further purification.

後処理

  1. customthe precipitate formed
  2. filtrationwas filtered off
  3. customdried in vacuo

出典と根拠

ORDレコード
ord-1172c2765278437091facd59836387e8
出典データセット
uspto-grants-2013_09
特許番号
US08530650B2

反応ノート

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