3-tert-Butyl-4-methoxy-benzenesulfonyl chloride → (7R,8aS)-2-[(6-tert-butylpyridin-2-yl)sulfonyl]-7-{[5-(prop-1-en-2-yl)-pyrazin-2-yl]oxy}octahydropyrrolo[1,2-a]pyrazine

HRID 240452노트

반응식

HRID 240452 반응식
[CH:1]1([C:4]2[N:5]=[CH:6][C:7]([O:10][C@H:11]3[CH2:19][N:14]4[CH2:15][CH2:16][NH:17][CH2:18][C@@H:13]4[CH2:12]3)=[N:8][CH:9]=2)[CH2:3][CH2:2]1.[C:20]([C:24]1[N:29]=[C:28]([S:30](Cl)(=[O:32])=[O:31])[CH:27]=[CH:26][CH:25]=1)([CH3:23])([CH3:22])[CH3:21].C(C1C=C(S(Cl)(=O)=O)C=CC=1OC)(C)(C)C>>[C:20]([C:24]1[N:29]=[C:28]([S:30]([N:17]2[CH2:16][CH2:15][N:14]3[CH2:19][C@H:11]([O:10][C:7]4[CH:6]=[N:5][C:4]([C:1]([CH3:2])=[CH2:3])=[CH:9][N:8]=4)[CH2:12][C@H:13]3[CH2:18]2)(=[O:32])=[O:31])[CH:27]=[CH:26][CH:25]=1)([CH3:23])([CH3:21])[CH3:22]

참가 물질

4

반응물 3

HCID 110652633-tert-Butyl-4-methoxy-benzenesulfonyl chlorideHCID 86680449(7R,8aS)-7-[(5-cyclopropylpyrazin-2-yl)oxy]octahydropyrrolo[1,2-a]pyrazineHCID 866804616-Tert-butylpyridine-2-sulfonyl chloride

생성물 1

HCID 86680460(7R,8aS)-2-[(6-tert-butylpyridin-2-yl)sulfonyl]-7-{[5-(prop-1-en-2-yl)-pyrazin-2-yl]oxy}octahydropyrrolo[1,2-a]pyrazine

실험 절차

The title compound was prepared according to the procedure described in Example 57, substituting the product from Example 202C (82 mg, 0.28 mmol) for the product from Example 27B, and substituting the product from Example 58B for 3-tert-butyl-4-methoxybenzene-1-sulfonyl chloride. The title compound was obtained as a colorless solid (79 mg, 62%). 1H NMR (300 MHz, CDCl3) δ ppm 1.39 (s, 9H), 1.78-2.06 (m, 2H), 2.17 (s, 3H), 2.31-2.49 (m, 2H), 2.50-2.62 (m, 1H), 2.61-2.74 (m, 1H), 2.91-3.06 (m, 2H), 3.69 (dd, J=9.92, 6.74 Hz, 1H), 3.85-3.96 (m, 1H), 4.02-4.13 (m, 1H), 5.22 (t, J=1.59 Hz, 1H), 5.32-5.42 (m, 1H), 5.77-5.81 (m, J=1.59 Hz, 1H), 7.51 (dd, J=7.54, 1.19 Hz, 1H), 7.71-7.84 (m, 2H), 8.15 (d, J=1.59 Hz, 1H), 8.20 (d, J=1.19 Hz, 1H).

후처리

  1. customThe title compound was prepared

출처 및 근거

ORD 기록
ord-23cceb29458144f0b1fe5cbf6a6081da
출처 데이터셋
uspto-grants-2014_02
특허 번호
US08648074B2

반응 노트

불러오는 중…