4-Chloroisoquinoline → 1-[(4-Chloro-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride

反応式

[Cl:1]C1C2C(=CC=CC=2)C=NC=1.[Cl:12][C:13]1[C:22]2[C:17](=[CH:18][CH:19]=[CH:20][C:21]=2[S:23](Cl)(=[O:25])=[O:24])[CH:16]=[N:15][CH:14]=1.C(OC([N:34]1[CH2:40][CH2:39][CH2:38][NH:37][CH2:36][CH2:35]1)=O)(C)(C)C>>[ClH:1].[ClH:12].[Cl:12][C:13]1[C:22]2[C:17](=[CH:18][CH:19]=[CH:20][C:21]=2[S:23]([N:34]2[CH2:40][CH2:39][CH2:38][NH:37][CH2:36][CH2:35]2)(=[O:25])=[O:24])[CH:16]=[N:15][CH:14]=1

参加物

反応物 3

HCID 6409744-Chloroisoquinoline

HCID 2756058Tert-butyl 1,4-diazepane-1-carboxylate

HCID 221219084-Chloroisoquinoline-5-sulfonyl chloride

生成物 1

HCID 221219391-[(4-Chloro-5-isoquinolinyl)sulfonyl]-hexahydro-1H-1,4-diazepine dihydrochloride

実験手順

Using 2.08 g of 4-chloroisoquinoline (synthesized in accordance with J. Org. Chem., 1961, 26, 468), 4-chloro-5-chlorosulfonylisoquinoline was synthesized as in Reference Example 1. Then, 1.30 g of this compound was reacted with 1.20 g of 1-(tert-butoxycarbonyl)-hexahydro-1H-1,4-diazepine and the reaction mixture was after-treated in the same manner as in Example 1 to provide 0.80 g of the objective compound (white crystals).