Diisopropylethylamine → HCID 68429730、化合物

HRID 335582

反応式

HRID 335582 の反応式
[Cl:1][C:2]1[CH:3]=[CH:4][C:5]2[O:9][C:8]([C:10]([OH:12])=O)=[CH:7][C:6]=2[CH:13]=1.CN(C(ON1N=[N:29][C:24]2[CH:25]=[CH:26][CH:27]=[N:28][C:23]1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F.[CH:38](N(CC)C(C)C)(C)[CH3:39]>CN(C=O)C>[ClH:1].[N:28]12[CH2:27][CH2:26][CH:25]([CH2:38][CH2:39]1)[C@@H:24]([NH:29][C:10]([C:8]1[O:9][C:5]3[CH:4]=[CH:3][C:2]([Cl:1])=[CH:13][C:6]=3[CH:7]=1)=[O:12])[CH2:23]2

参加物

5

反応物 3

HCID 81531DiisopropylethylamineHCID 9378385-Chloro-1-benzofuran-2-carboxylic acidHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)

生成物 1

HCID 68429730HCID 68429730、化合物

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

190 mg (0.98 mmol) of 5-chlorobenzofuran-2-carboxylic acid, 200 mg (0.98 mmol) of R-3-aminoquinuclidine dihydrochloride, 450 mg (1.18 mmol) of HATU, 460 mg (3.54 mmol) of N,N-diisopropylethylamine and 2.0 ml of DMF are reacted according to the general procedure (variant B). The reaction mixture is purified by preparative HPLC. An excess of 1N hydrochloric acid is then added to the product. The solvent is removed under reduced pressure. 145 mg (43% of theory) of the title compound are isolated.

後処理

  1. customThe reaction mixture is purified by preparative HPLC
  2. additionAn excess of 1N hydrochloric acid is then added to the product
  3. customThe solvent is removed under reduced pressure

出典と根拠

ORDレコード
ord-2a78db2ef83b4ae09bc5cd713a59f4ba
出典データセット
uspto-grants-2014_11
特許番号
US08884017B2

関連ノート

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