Diisopropylethylamine → (R)-3-(4-(3-Aminopyrrolidine-1-carbonyl)-2-(cyclopropylmethyl)-1-oxo-1,2-dihydroisoquinolin-6-yl)-N-cyclopropyl-4-methylbenzamide

HRID 907275ノート

反応式

HRID 907275 の反応式
[CH:1]1([NH:4][C:5]([C:7]2[CH:8]=[CH:9][C:10]([CH3:31])=[C:11]([C:13]3[CH:14]=[C:15]4[C:20](=[CH:21][CH:22]=3)[C:19](=[O:23])[N:18]([CH2:24][CH:25]3[CH2:27][CH2:26]3)[CH:17]=[C:16]4[C:28](O)=[O:29])[CH:12]=2)=[O:6])[CH2:3][CH2:2]1.[NH:32]1[CH2:36][CH2:35][C@@H:34]([NH2:37])[CH2:33]1.C(N(CC)C(C)C)(C)C.CN(C(ON1N=NC2C=CC=NC1=2)=[N+](C)C)C.F[P-](F)(F)(F)(F)F>CN(C=O)C>[NH2:37][C@@H:34]1[CH2:35][CH2:36][N:32]([C:28]([C:16]2[C:15]3[C:20](=[CH:21][CH:22]=[C:13]([C:11]4[CH:12]=[C:7]([CH:8]=[CH:9][C:10]=4[CH3:31])[C:5]([NH:4][CH:1]4[CH2:2][CH2:3]4)=[O:6])[CH:14]=3)[C:19](=[O:23])[N:18]([CH2:24][CH:25]3[CH2:27][CH2:26]3)[CH:17]=2)=[O:29])[CH2:33]1

参加物

6

反応物 4

HCID 81531DiisopropylethylamineHCID 1519352(3R)-pyrrolidin-3-amineHCID 9886157Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)HCID 575517606-(5-(Cyclopropylcarbamoyl)-2-methylphenyl)-2-(cyclopropylmethyl)-1-oxo-1,2-dihydroisoquinoline-4-carboxylic acid

生成物 1

HCID 25020019(R)-3-(4-(3-Aminopyrrolidine-1-carbonyl)-2-(cyclopropylmethyl)-1-oxo-1,2-dihydroisoquinolin-6-yl)-N-cyclopropyl-4-methylbenzamide

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒

実験手順

To a solution of the product of step v) (100 mg), (R)-pyrrolidin-3-amine (20 mg) and N,N-diisopropylethylamine (0.13 mL) in DMF (2 mL) was added HATU (140 mg) and the reaction stirred at room temperature for 10 minutes. The reaction mixture was filtered and purified by HPLC to yield the title compound as a solid (65 mg).

後処理

  1. filtrationThe reaction mixture was filtered
  2. custompurified by HPLC

出典と根拠

ORDレコード
ord-87f04dd011a9481f9fca6a3d1746adea
出典データセット
uspto-grants-2011_09
特許番号
US08012979B2

反応ノート

読み込み中…