Triethylamine → N,N'-Di-tert-butoxycarbonyl-7-(1-acetimidoylpiperidin-4-ylmethoxy)-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine

HRID 412568ノート

反応式

HRID 412568 の反応式
[C:1]([O:5][C:6]([NH:8][C:9]([N:18]1[CH2:27][CH2:26][C:25]2[C:20](=[CH:21][C:22]([O:28][CH2:29][CH:30]3[CH2:35][CH2:34][NH:33][CH2:32][CH2:31]3)=[CH:23][CH:24]=2)[CH2:19]1)=[N:10][C:11]([O:13][C:14]([CH3:17])([CH3:16])[CH3:15])=[O:12])=[O:7])([CH3:4])([CH3:3])[CH3:2].[CH2:36]([N:38](CC)CC)[CH3:37].Cl.C(OC(=N)C)C.C(OCC)(=O)C>O1CCCC1.C(O)C.C(OCC)C>[C:14]([O:13][C:11]([NH:10][C:9]([N:18]1[CH2:27][CH2:26][C:25]2[C:20](=[CH:21][C:22]([O:28][CH2:29][CH:30]3[CH2:35][CH2:34][N:33]([C:36](=[NH:38])[CH3:37])[CH2:32][CH2:31]3)=[CH:23][CH:24]=2)[CH2:19]1)=[N:8][C:6]([O:5][C:1]([CH3:2])([CH3:3])[CH3:4])=[O:7])=[O:12])([CH3:17])([CH3:16])[CH3:15]

参加物

8

反応物 4

HCID 8471TriethylamineHCID 8857Ethyl AcetateHCID 2724290Ethanimidic acid, ethyl ester, hydrochloride (1:1)HCID 60064218N,N'-ditert-butoxycarbonyl-7-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine

生成物 1

HCID 60064189N,N'-Di-tert-butoxycarbonyl-7-(1-acetimidoylpiperidin-4-ylmethoxy)-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine

試薬・触媒・溶媒 3

HCID 702Ethanol溶媒HCID 3283Diethyl Ether溶媒HCID 8028Tetrahydrofuran溶媒

実験手順

To a solution of N,N′-di-tert-butoxycarbonyl-7-(piperidin-4-ylmethoxy)-1,2,3,4-tetrahydroisoquinoline-2-carboxamidine (100 mg) in a mixture of tetrahydrofuran (1.5 ml) and ethanol (1.5 ml) were added triethylamine (0.086 ml) and ethylacetoimidate hydrochloride (38 mg), and the mixture was stirred at room temperature for 18 hours. After completion of the reaction, ethyl acetate and diethyl ether were added and insoluble material was removed. The solvent was evaporated and the residue was dried under reduced pressure to give the title compound (120 mg).

後処理

  1. additionwere added
  2. custominsoluble material was removed
  3. customThe solvent was evaporated
  4. customthe residue was dried under reduced pressure

出典と根拠

ORDレコード
ord-c4326ccf40c14ac58687e6ad59e15d51
出典データセット
uspto-grants-2003_05
特許番号
US06562828B1

反応ノート

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