(R)-4-Difluoromethoxybenzyl 2-ethylpiperazine-1-carboxylate fumarate → (R)-2,6-Difluoro-4-difluoromethoxybenzyl 2-methylpiperazine-1-carboxylate fumarate

HRID 1794108

反応式

HRID 1794108 の反応式
[F:1][C:2]1[CH:9]=[C:8]([O:10][CH:11]([F:13])[F:12])[CH:7]=[C:6]([F:14])[C:3]=1[CH2:4][OH:5].[C:15]([OH:22])(=[O:21])/[CH:16]=[CH:17]/[C:18]([OH:20])=[O:19].[CH2:23]([C@@H:25]1[CH2:30][NH:29][CH2:28][CH2:27][N:26]1[C:31](OCC1C=CC(OC(F)F)=CC=1)=[O:32])C>>[C:15]([OH:22])(=[O:21])/[CH:16]=[CH:17]/[C:18]([OH:20])=[O:19].[CH3:23][C@@H:25]1[CH2:30][NH:29][CH2:28][CH2:27][N:26]1[C:31]([O:5][CH2:4][C:3]1[C:2]([F:1])=[CH:9][C:8]([O:10][CH:11]([F:12])[F:13])=[CH:7][C:6]=1[F:14])=[O:32]

参加物

3

反応物 2

HCID 21021913(R)-4-Difluoromethoxybenzyl 2-ethylpiperazine-1-carboxylate fumarateHCID 69140944Benzenemethanol, 4-(difluoromethoxy)-2,6-difluoro-

生成物 1

HCID 21021906(R)-2,6-Difluoro-4-difluoromethoxybenzyl 2-methylpiperazine-1-carboxylate fumarate

実験手順

(R)-2,6-Difluoro-4-difluoromethoxybenzyl 2-methylpiperazine-1-carboxylate fumarate was prepared from 2,6-difluoro-4-difluoromethoxybenzyl alcohol and (R) 1-chlorocarbonyl-2-methyl-4-tert-butoxycarbonylpiperazine according to the methods described for Examples 54 to give the product as a white solid (2.9%); HPLC (XTERRA, 50/80, 220 nm) 86.0% (1.55 min); NMR δH (400 MHz, DMSO-d6) 1.154(3H, d, J 7.0 Hz), 2.639(1H, bm), 2.863(2H, bm), 3.007(2H, bm), 3.714(1H, bd), 4.122(1H, bs), 5.106(2H, q), 6.590(2H, s), 7.108(2H, d, J 8.5 Hz) and 7.360(1H, t, J 73 Hz).

出典と根拠

ORDレコード
ord-65257b6269064f838d395e6d8a3a4749
出典データセット
uspto-grants-2006_04
特許番号
US07022707B2

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