Methyl 4-(1-aminocyclopropyl)benzoate hydrochloride → Methyl 4-(1-(2-(3-(3,4-difluorophenoxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinamido)cyclopropyl)benzoate

HRID 72521

反応式

HRID 72521 の反応式
[F:1][C:2]1[CH:3]=[C:4]([CH:23]=[CH:24][C:25]=1[F:26])[O:5][CH:6]1[CH2:9][N:8]([C:10]2[N:18]=[CH:17][C:16]([C:19]([F:22])([F:21])[F:20])=[CH:15][C:11]=2[C:12](O)=[O:13])[CH2:7]1.Cl.[NH2:28][C:29]1([C:32]2[CH:41]=[CH:40][C:35]([C:36]([O:38][CH3:39])=[O:37])=[CH:34][CH:33]=2)[CH2:31][CH2:30]1>>[F:1][C:2]1[CH:3]=[C:4]([CH:23]=[CH:24][C:25]=1[F:26])[O:5][CH:6]1[CH2:9][N:8]([C:10]2[N:18]=[CH:17][C:16]([C:19]([F:22])([F:20])[F:21])=[CH:15][C:11]=2[C:12]([NH:28][C:29]2([C:32]3[CH:41]=[CH:40][C:35]([C:36]([O:38][CH3:39])=[O:37])=[CH:34][CH:33]=3)[CH2:31][CH2:30]2)=[O:13])[CH2:7]1

参加物

3

反応物 2

HCID 66824369Methyl 4-(1-aminocyclopropyl)benzoate hydrochlorideHCID 679582442-(3-(3,4-Difluorophenoxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinic acid

生成物 1

HCID 67958495Methyl 4-(1-(2-(3-(3,4-difluorophenoxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinamido)cyclopropyl)benzoate収率 54.7%

実験手順

The title compound (D179) (80 mg) was prepared according to the experimental procedure described in Description 144 starting from 2-(3-(3,4-difluorophenoxy)azetidin-1-yl)-5-(trifluoromethyl)nicotinic acid (D128) (100 mg, 0.267 mmol) and methyl 4-(1-aminocyclopropyl)benzoate (D7) (60.83 mg, 0.267 mmol).

出典と根拠

ORDレコード
ord-44201a5a0e804396bed9aec492e2a6ab
出典データセット
uspto-grants-2014_09
特許番号
US08828987B2

関連ノート

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