Morpholine → 1-(Pyrazin-2-YL)cyclopropan-1-amine

HRID 1040477ノート

反応式

HRID 1040477 の反応式
C(OC(=O)[NH:6][C:7]1([C:10]2[CH:15]=[N:14][CH:13]=[CH:12][N:11]=2)[CH2:9][CH2:8]1)C=C.N1CCOCC1>C1COCC1.C1C=CC([P]([Pd]([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)([P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)[P](C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)(C2C=CC=CC=2)C2C=CC=CC=2)=CC=1>[N:11]1[CH:12]=[CH:13][N:14]=[CH:15][C:10]=1[C:7]1([NH2:6])[CH2:9][CH2:8]1

参加物

5

反応物 2

HCID 8083MorpholineHCID 58431049HCID 58431049、化合物

生成物 1

HCID 584310771-(Pyrazin-2-YL)cyclopropan-1-amine収率 14.3%

試薬・触媒・溶媒 2

HCID 178418397HCID 178418397、化合物触媒HCID 8028Tetrahydrofuran溶媒

反応条件

温度
50 °C

実験手順

To a solution of (1-Pyrazin-2-yl-cyclopropyl)-carbamic acid allyl ester (67 mg, 0.31 mmol) and morpholine (0.31 mL, 3.1 mmol) in THF (3 mL) was added Pd(PPh3)4 (27 mg, 0.02 mmol) and the yellow mixture was stirred at 50° C. for 3 h. The solvent was removed under a stream of N2 and the residue was purified by flash chromatography (silica, 4→7% MeOH/CH2Cl2) to give 6 mg of the title compound as an orange oil, m/z 136.04 [M+1]+.

後処理

  1. customThe solvent was removed under a stream of N2
  2. customthe residue was purified by flash chromatography (silica, 4→7% MeOH/CH2Cl2)

出典と根拠

ORDレコード
ord-29d9822820974a11b891301e874e7b48
出典データセット
uspto-grants-2013_10
特許番号
US08552205B2

反応ノート

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