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

HRID 72498ノート

反応式

HRID 72498 の反応式
[Cl:1][C:2]1[CH:3]=[N:4][C:5]([N:11]2[CH2:14][CH:13]([O:15][C:16]3[CH:21]=[CH:20][C:19]([F:22])=[CH:18][C:17]=3[F:23])[CH2:12]2)=[C:6]([CH:10]=1)[C:7]([OH:9])=O.Cl.[NH2:25][C:26]1([C:29]2[CH:38]=[CH:37][C:32]([C:33]([O:35][CH3:36])=[O:34])=[CH:31][CH:30]=2)[CH2:28][CH2:27]1>>[Cl:1][C:2]1[CH:3]=[N:4][C:5]([N:11]2[CH2:12][CH:13]([O:15][C:16]3[CH:21]=[CH:20][C:19]([F:22])=[CH:18][C:17]=3[F:23])[CH2:14]2)=[C:6]([CH:10]=1)[C:7]([NH:25][C:26]1([C:29]2[CH:38]=[CH:37][C:32]([C:33]([O:35][CH3:36])=[O:34])=[CH:31][CH:30]=2)[CH2:28][CH2:27]1)=[O:9]

参加物

3

反応物 2

HCID 66824369Methyl 4-(1-aminocyclopropyl)benzoate hydrochlorideHCID 679584225-Chloro-2-(3-(2,4-difluorophenoxy)azetidin-1-yl)nicotinic acid

生成物 1

HCID 67958349Methyl 4-(1-(5-chloro-2-(3-(2,4-difluorophenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate収率 44.6%

実験手順

The title compound (D154) (55 mg) was prepared according to the experimental procedure described in Description 144 starting from 5-chloro-2-(3-(2,4-difluorophenoxy)azetidin-1-yl)nicotinic acid (D108) (82 mg, 0.240 mmol) and methyl 4-(1-aminocyclopropyl)benzoate (D7) (54.79 mg, 0.240 mmol).

出典と根拠

ORDレコード
ord-bd62a4730b4b4d4baa0e50ecfa9f7c89
出典データセット
uspto-grants-2014_09
特許番号
US08828987B2

反応ノート

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