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 240452ノート

反応式

HRID 240452 の反応式
[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]

参加物

4

反応物 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

生成物 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

実験手順

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).

後処理

  1. customThe title compound was prepared

出典と根拠

ORDレコード
ord-23cceb29458144f0b1fe5cbf6a6081da
出典データセット
uspto-grants-2014_02
特許番号
US08648074B2

反応ノート

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