Methyl 2,5-Dichloronicotinate → Methyl 5-chloro-2-(3-(3-fluorophenoxy)pyrrolidin-1-yl)nicotinate

反応式

Cl[C:2]1[N:11]=[CH:10][C:9]([Cl:12])=[CH:8][C:3]=1[C:4]([O:6][CH3:7])=[O:5].[F:13][C:14]1[CH:15]=[C:16]([CH:23]=[CH:24][CH:25]=1)[O:17][CH:18]1[CH2:22][CH2:21][NH:20][CH2:19]1>>[Cl:12][C:9]1[CH:10]=[N:11][C:2]([N:20]2[CH2:21][CH2:22][CH:18]([O:17][C:16]3[CH:23]=[CH:24][CH:25]=[C:14]([F:13])[CH:15]=3)[CH2:19]2)=[C:3]([CH:8]=1)[C:4]([O:6][CH3:7])=[O:5]

参加物

反応物 2

HCID 2764318Methyl 2,5-Dichloronicotinate

HCID 450755013-(3-Fluorophenoxy)pyrrolidine

生成物 1

HCID 67958336Methyl 5-chloro-2-(3-(3-fluorophenoxy)pyrrolidin-1-yl)nicotinate収率 60.9%

実験手順

The title compound (D95) (250 mg) was prepared according to the experimental procedure described in Description 62 starting from methyl 2,5-dichloronicotinate (241.37 mg, 1.17 mmol) and 3-(3-fluorophenoxy)pyrrolidine (D60) (253 mg, 1.39 mmol).

出典と根拠

ORDレコード: ord-6acf5286cc4f4c5faa2b3998091409ca
出典データセット: uspto-grants-2014_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US08828987B2

反応ノート

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