Morpholine → 4-[2-(4,4-Dimethylcyclohexyl)-4-morpholin-4-ylphenyl]piperazine-1-carboxylic acid t-butyl ester

HRID 32140

반응식

HRID 32140 반응식
[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[CH:19]=[CH:18][C:17](Br)=[CH:16][C:15]=2[CH:21]2[CH2:26][CH2:25][C:24]([CH3:28])([CH3:27])[CH2:23][CH2:22]2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2].[NH:29]1[CH2:34][CH2:33][O:32][CH2:31][CH2:30]1.CC(C)([O-])C.[Na+].F[B-](F)(F)F.C([PH+](C(C)(C)C)C(C)(C)C)(C)(C)C>C([O-])(=O)C.[Pd+2].C([O-])(=O)C.C1(C)C(C)=CC=CC=1>[C:1]([O:5][C:6]([N:8]1[CH2:13][CH2:12][N:11]([C:14]2[CH:19]=[CH:18][C:17]([N:29]3[CH2:34][CH2:33][O:32][CH2:31][CH2:30]3)=[CH:16][C:15]=2[CH:21]2[CH2:26][CH2:25][C:24]([CH3:28])([CH3:27])[CH2:23][CH2:22]2)[CH2:10][CH2:9]1)=[O:7])([CH3:4])([CH3:3])[CH3:2]

참가 물질

7

반응물 4

HCID 8083MorpholineHCID 2734635Tri-tert-butylphosphine tetrafluoroborateHCID 23676156Sodium t-butoxideHCID 597694184-[4-Bromo-2-(4,4-dimethylcyclohexyl)phenyl]piperazine-1-carboxylic acid t-butyl ester

생성물 1

HCID 597693984-[2-(4,4-Dimethylcyclohexyl)-4-morpholin-4-ylphenyl]piperazine-1-carboxylic acid t-butyl ester

시약·촉매·용매 2

HCID 167845palladium(II) acetate촉매HCID 7237O-Xylene용매

반응 조건

온도
100 °C

실험 절차

A mixture of 4-[4-bromo-2-(4,4-dimethylcyclohexyl)phenyl]piperazine-1-carboxylic acid t-butyl ester (1 g, 2.22 mmol) prepared in Example (3e), morpholine (290 mg, 3.32 mmol), sodium t-butoxide (533 mg, 5.55 mmol), palladium(II) acetate (50 mg, 0.222 mmol), tri-t-butylphosphonium tetrafluoroborate (193 mg, 0.666 mmol) and xylene (10 mL) was stirred at an external temperature of 100° C. for 1 hour and 15 minutes under a nitrogen atmosphere.

출처 및 근거

ORD 기록
ord-f8115643e41243a5b6904d2d00786913
출처 데이터셋
uspto-grants-2008_09
특허 번호
US07425554B2

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