4-Hydroxypyrrolidine → N-(1-(4-(4-(2,3-Dihydro-benzo(1,4)dioxin-6-ylsulfanyl)-3-trifluoromethyl-phenyl)-pyridin-2-yl)-pyrrolidin-3-yl)-acetamide

HRID 1246864

반응식

HRID 1246864 반응식
[O:1]1[C:6]2[CH:7]=[CH:8][C:9]([S:11][C:12]3[CH:17]=[CH:16][C:15]([C:18]4[CH:23]=[CH:22][N:21]=[CH:20][CH:19]=4)=[CH:14][C:13]=3[C:24]([F:27])([F:26])[F:25])=[CH:10][C:5]=2[O:4][CH2:3][CH2:2]1.OC1CCNC1.[C:34]([NH:37][C@@H:38]1[CH2:42][CH2:41][NH:40][CH2:39]1)(=[O:36])[CH3:35]>>[O:1]1[C:6]2[CH:7]=[CH:8][C:9]([S:11][C:12]3[CH:17]=[CH:16][C:15]([C:18]4[CH:19]=[CH:20][N:21]=[C:22]([N:40]5[CH2:41][CH2:42][CH:38]([NH:37][C:34](=[O:36])[CH3:35])[CH2:39]5)[CH:23]=4)=[CH:14][C:13]=3[C:24]([F:25])([F:26])[F:27])=[CH:10][C:5]=2[O:4][CH2:3][CH2:2]1

참가 물질

4

반응물 3

HCID 982104-HydroxypyrrolidineHCID 7016129(3R)-(+)-3-AcetamidopyrrolidineHCID 865858674-(4-(2,3-Dihydro-benzo(1,4)dioxin-6-ylsulfanyl)-3-trifluoromethyl-phenyl)-pyridine

생성물 1

HCID 9936333N-(1-(4-(4-(2,3-Dihydro-benzo(1,4)dioxin-6-ylsulfanyl)-3-trifluoromethyl-phenyl)-pyridin-2-yl)-pyrrolidin-3-yl)-acetamide

실험 절차

The title compound was prepared according to the procedures of Example 38E, substituting compound 76 with compound 118 (0.033 g, 0.0779 mmol) and 3-hydroxypyrrolidine with (3R)-(+)-3-acetamidopyrrolidine. A yellow solid 123 was obtained (0.0397 g, 78%). 1H-NMR (CDCl3, 400 MHz) δ 2.03 (s, 3H), 2.25–2.31 (m, 1H), 2.34–2.42 (m, 1H), 3.80–3.90 (m, 3H), 4.02–4.11 (m, 1H), 4.28–4.34 (m, 4H), 4.63–4.68 (m, 1H), 6.78 (s, 1H), 6.93–6.97 (m, 2H), 7.05 (dd, J=2.2 Hz, 8.4 Hz, 1H), 7.09–7.13 (m, 2H), 7.18 (brs, 1H), 7.53 (d, J=8.4 Hz, 1H), 7.83 (s, 1H), 8.07 (d, J=6.6 Hz, 1H); MS (APCI) m/z 516 (M+H)+.

출처 및 근거

ORD 기록
ord-377511fbbbfd4c3eaf5f10cef3597eb8
출처 데이터셋
uspto-grants-2006_10
특허 번호
US07129247B2

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