Cyclopropanemethanamine → (2-{5-[5-(4-Chloro-phenyl)-pyridin-2-ylethynyl]-indol-1-yl}-ethyl)-cyclopropylmethyl-amine

HRID 1916714ノート

反応式

HRID 1916714 の反応式
[CH:1]1([CH2:4][NH2:5])[CH2:3][CH2:2]1.CS(O[CH2:11][CH2:12][N:13]1[C:21]2[C:16](=[CH:17][C:18]([C:22]#[C:23][C:24]3[CH:29]=[CH:28][C:27]([C:30]4[CH:35]=[CH:34][C:33]([Cl:36])=[CH:32][CH:31]=4)=[CH:26][N:25]=3)=[CH:19][CH:20]=2)[CH:15]=[CH:14]1)(=O)=O>CN(C=O)C>[Cl:36][C:33]1[CH:32]=[CH:31][C:30]([C:27]2[CH:28]=[CH:29][C:24]([C:23]#[C:22][C:18]3[CH:17]=[C:16]4[C:21](=[CH:20][CH:19]=3)[N:13]([CH2:12][CH2:11][NH:5][CH2:4][CH:1]3[CH2:3][CH2:2]3)[CH:14]=[CH:15]4)=[N:25][CH:26]=2)=[CH:35][CH:34]=1

参加物

4

反応条件

温度
60 °C

実験手順

0.46 mL (5.4 mmol) C-cyclopropyl-methylamine are added to a solution of 2.03 g (4.5 mmol) 2-{5-[5-(4-chloro-phenyl)-pyridin-2-ylethynyl]-indol-1-yl}-ethyl methanesulphonate in 20 mL DMF and the reaction mixture is stirred for 4 h at 60° C. The mixture is evaporated down i. vac., the residue is stirred with DCM, the precipitate is suction filtered and dried in the air. The product is precipitated as the methanesulphonic acid salt.

後処理

  1. customThe mixture is evaporated down i
  2. stirring, the residue is stirred with DCM
  3. filtrationfiltered
  4. customdried in the air
  5. customThe product is precipitated as the methanesulphonic acid salt

出典と根拠

ORDレコード
ord-169827c5490b4291ba8f0f26bfe90d6d
出典データセット
uspto-grants-2013_12
特許番号
US08618132B2

反応ノート

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