Morpholine → [1-(2-Mercapto-3-morpholin-4-yl-propyl)-piperidin-4-yl]-carbamic acid tert-butyl ester

HRID 2279388

반응식

HRID 2279388 반응식
[NH:1]1[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1.[C:7]([O:11][C:12](=[O:24])[NH:13][CH:14]1[CH2:19][CH2:18][N:17]([CH2:20][CH:21]2[CH2:23][S:22]2)[CH2:16][CH2:15]1)([CH3:10])([CH3:9])[CH3:8]>C(O)C>[C:7]([O:11][C:12](=[O:24])[NH:13][CH:14]1[CH2:15][CH2:16][N:17]([CH2:20][CH:21]([SH:22])[CH2:23][N:1]2[CH2:6][CH2:5][O:4][CH2:3][CH2:2]2)[CH2:18][CH2:19]1)([CH3:9])([CH3:8])[CH3:10]

참가 물질

4

반응물 2

HCID 8083MorpholineHCID 86662008(1-Thiiranylmethyl-piperidin-4-yl)-carbamic acid tert-butyl ester

생성물 1

HCID 86662007[1-(2-Mercapto-3-morpholin-4-yl-propyl)-piperidin-4-yl]-carbamic acid tert-butyl ester수율 134.5%

시약·촉매·용매 1

HCID 702Ethanol용매

실험 절차

Morpholine (80 μL, 0.83 mmol, 1.5 eq) is added at room temperature to a stirred solution of (1-thiiranylmethyl-piperidin-4-yl)-carbamic acid tert-butyl ester (300 mg, 0.55 mmol, 1.0 eq) in ethanol (2 mL). The reaction mixture is irradiated under microwave conditions for 4 minutes at 140° C. and 80 W and then solvent is evaporated to afford [1-(2-mercapto-3-morpholin-4-yl-propyl)-piperidin-4-yl]-carbamic acid tert-butyl ester as an off-white semisolid (266 mg, 67% yield).

후처리

  1. customThe reaction mixture is irradiated under microwave conditions for 4 minutes at 140° C.
  2. custom80 W and then solvent is evaporated

출처 및 근거

ORD 기록
ord-6b9dca5142714058b31a97180c8b0cd0
출처 데이터셋
uspto-grants-2015_09
특허 번호
US09133219B2

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