Dimethylformamide → HCID 53358567, 화합물

HRID 1807310노트

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HRID 1807310 반응식
[Cl:1][C:2]1[C:3]([F:38])=[C:4]([C@@H:8]2[C@:12]([C:15]3[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][C:16]=3[F:22])([C:13]#[N:14])[C@H:11]([CH2:23][C:24]([CH3:27])([CH3:26])[CH3:25])[NH:10][C@H:9]2[C:28]([NH:30][C:31]2[CH:36]=[CH:35][C:34](I)=[CH:33][N:32]=2)=[O:29])[CH:5]=[CH:6][CH:7]=1.CN(C=O)C.C(=O)([O-])[O-].[K+].[K+]>C([O-])(=O)C.[Pd+2].C([O-])(=O)C.O>[N:32]1[CH:33]=[CH:34][CH:35]=[CH:36][C:31]=1[NH:30][C:28]([C@H:9]1[C@H:8]([C:4]2[CH:5]=[CH:6][CH:7]=[C:2]([Cl:1])[C:3]=2[F:38])[C@:12]([C:15]2[CH:20]=[CH:19][C:18]([Cl:21])=[CH:17][C:16]=2[F:22])([C:13]#[N:14])[C@H:11]([CH2:23][C:24]([CH3:27])([CH3:26])[CH3:25])[NH:10]1)=[O:29]

참가 물질

6

반응물 3

HCID 6228DimethylformamideHCID 11430Potassium CarbonateHCID 53358685HCID 53358685, 화합물

생성물 1

HCID 53358567HCID 53358567, 화합물

시약·촉매·용매 2

HCID 167845palladium(II) acetate촉매HCID 962Water용매

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온도
70 °C

실험 절차

In a 50 ml pressure tube, (2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-N-(5-iodopyridin-2-yl)-5-neopentylpyrrolidine-2-carboxamide (87 mg, 130 μmol, Eq: 1.00) was combined with DMF (3.48 ml) and water (174 μl). Potassium carbonate (35.9 mg, 260 μmol, Eq: 2) was added. The mixture was bubbled with nitrogen and then palladium (II) acetate (3.48 mg, 15.5 μmol, Eq: 0.119) was added. The tube was subjected to CO atmosphere at 40 PSI and stirred for 3 hours at 70° C.

후처리

  1. customThe mixture was bubbled with nitrogen

출처 및 근거

ORD 기록
ord-51716c88e7664ab296b4a0ebf4d76994
출처 데이터셋
uspto-grants-2013_01
특허 번호
US08354444B2

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