1-(2-Hydroxyethyl)-2-pyrrolidinone → 3-Fluoro-N-{4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-1-naphthyl}-5-piperidin-1-ylbenzamide

HRID 1171364

反応式

HRID 1171364 の反応式
[OH:1][C:2]1[C:11]2[C:6](=[CH:7][CH:8]=[CH:9][CH:10]=2)[C:5]([NH:12][C:13](=[O:19])OC(C)(C)C)=[CH:4][CH:3]=1.[F:20][C:21]1[CH:22]=[C:23]([CH:27]=[C:28]([N:30]2[CH2:35][CH2:34][CH2:33][CH2:32][CH2:31]2)[CH:29]=1)C(O)=O.O[CH2:37][CH2:38][N:39]1[CH2:43][CH2:42][CH2:41][C:40]1=[O:44]>>[F:20][C:21]1[CH:22]=[C:23]([CH:27]=[C:28]([N:30]2[CH2:31][CH2:32][CH2:33][CH2:34][CH2:35]2)[CH:29]=1)[C:13]([NH:12][C:5]1[C:6]2[C:11](=[CH:10][CH:9]=[CH:8][CH:7]=2)[C:2]([O:1][CH2:37][CH2:38][N:39]2[CH2:43][CH2:42][CH2:41][C:40]2=[O:44])=[CH:3][CH:4]=1)=[O:19]

参加物

4

反応物 3

HCID 769801-(2-Hydroxyethyl)-2-pyrrolidinoneHCID 10923237tert-Butyl (4-hydroxynaphthalen-1-yl)carbamateHCID 595531803-Fluoro-5-piperidinylbenzoic acid

生成物 1

HCID 595533033-Fluoro-N-{4-[2-(2-oxopyrrolidin-1-yl)ethoxy]-1-naphthyl}-5-piperidin-1-ylbenzamide

実験手順

Compound is prepared from tert-butyl (4-hydroxy-1-naphthyl)carbamate, 3-fluoro-5-piperidin-1-yl-benzoic acid and 1-(2-hydroxyethyl)-pyrrolidin-2-one according to conditions described in general procedure D. A white solid is produced (27 mg). Mp: 161-162° C.; 1H NMR (300 MHz, CDCl3) δ 1.62-1.70 (m, 6H), 1.99-2.09 (m, 2H), 2.35-2.44 (m, 2H), 3.16-3.27 (m, 2H), 3.63-3.68 (m, 2H), 3.84 (d, J=5.1Hz, 2H), 4.26 (d, J=4.8 Hz, 2H), 6.73-6.79 (m, 2H), 6.70 (d, J=8.4 Hz, 1H), 7.32 (s, 1H), 7.49-7.58 (m, 2H), 7.68 (d, J=8.1Hz, 1H), 7.84 (d, J=7.8 Hz, 1H), 8.03 (s, 1H), 8.24-8.27 (m, 1H); MS 476 (M+1).

後処理

  1. customA white solid is produced (27 mg)

出典と根拠

ORDレコード
ord-77b8fb0bf6a8499ebb2cb5b34d4ade63
出典データセット
uspto-grants-2010_11
特許番号
US07829560B2

関連ノート

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