2-(Pyrrolidin-1-yl)acetic acid hydrochloride → (S)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)-2-(2-(pyrrolidin-1-yl)acetamido)propanamide

HRID 1630109

反応式

HRID 1630109 の反応式
Cl.[N:2]1([CH2:7][C:8]([OH:10])=O)[CH2:6][CH2:5][CH2:4][CH2:3]1.[NH2:11][C@@H:12]([CH2:30][O:31][CH2:32][C:33]1[CH:38]=[CH:37][CH:36]=[CH:35][CH:34]=1)[C:13]([NH:15][C:16]1[CH:21]=[CH:20][C:19]([O:22][C:23]2[CH:28]=[CH:27][C:26]([F:29])=[CH:25][CH:24]=2)=[CH:18][CH:17]=1)=[O:14]>>[CH2:32]([O:31][CH2:30][C@H:12]([NH:11][C:8](=[O:10])[CH2:7][N:2]1[CH2:3][CH2:4][CH2:5][CH2:6]1)[C:13]([NH:15][C:16]1[CH:21]=[CH:20][C:19]([O:22][C:23]2[CH:28]=[CH:27][C:26]([F:29])=[CH:25][CH:24]=2)=[CH:18][CH:17]=1)=[O:14])[C:33]1[CH:38]=[CH:37][CH:36]=[CH:35][CH:34]=1

参加物

3

反応物 2

HCID 130220162-(Pyrrolidin-1-yl)acetic acid hydrochlorideHCID 67009137(S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide

生成物 1

HCID 67009486(S)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)-2-(2-(pyrrolidin-1-yl)acetamido)propanamide収率 74.8%

実験手順

Proceeding as in Example 1, but substituting 2-(pyrrolidin-1-yl)acetic acid hydrochloride and (S)-2-amino-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)propanamide, gave Compound 215, (S)-3-(benzyloxy)-N-(4-(4-fluorophenoxy)phenyl)-2-(2-(pyrrolidin-1-yl)acetamido)propanamide (29.4 mg, 74.8%); Major isomer: 1H-NMR (400 MHz, DMSO-D6): σ 10.21 (s, 1H), 7.92 (d, 1H), 7.60 (d, 2H), 7.27-7.31 (m, 5H), 7.21 (d, 2H), 6.99-4.03 (m, 4H), 4.72 (m, 1H), 4.52 (s, 2H), 3.70-3.75 (m, 2H), 3.12 (d, 2H), 2.55 (d, 4H), 1.72 (m 4H). MS (EI) for C28H30FN3O4. found 492.5 (MH+).

出典と根拠

ORDレコード
ord-a139cc2c0cd7407ca40df9361d5d514a
出典データセット
uspto-grants-2014_07
特許番号
US08791102B2

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