(1S)-1-[4-(Trifluoromethyl)phenyl]ethylamine → benzyl 4-[({(1S)-1-[4-(trifluoromethyl)phenyl]ethyl}amino)methyl]benzoate

反応式

[CH:1]([C:3]1[CH:18]=[CH:17][C:6]([C:7]([O:9][CH2:10][C:11]2[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=2)=[O:8])=[CH:5][CH:4]=1)=O.[F:19][C:20]([F:31])([F:30])[C:21]1[CH:26]=[CH:25][C:24]([C@@H:27]([NH2:29])[CH3:28])=[CH:23][CH:22]=1>>[F:19][C:20]([F:30])([F:31])[C:21]1[CH:22]=[CH:23][C:24]([C@@H:27]([NH:29][CH2:1][C:3]2[CH:18]=[CH:17][C:6]([C:7]([O:9][CH2:10][C:11]3[CH:16]=[CH:15][CH:14]=[CH:13][CH:12]=3)=[O:8])=[CH:5][CH:4]=2)[CH3:28])=[CH:25][CH:26]=1

参加物

反応物 2

HCID 2779052(1S)-1-[4-(Trifluoromethyl)phenyl]ethylamine

HCID 11528845Benzyl 4-formylbenzoate

生成物 1

HCID 67187817benzyl 4-[({(1S)-1-[4-(trifluoromethyl)phenyl]ethyl}amino)methyl]benzoate収率 83%

実験手順

The same procedure as employed in the preparation of Example 226 (step a) but using benzyl 4-formylbenzoate and (1S)-1-[4-(trifluoromethyl)phenyl]ethylamine gave the title compound as a pale yellow oil (83%). M+(LC/MS(ESI)): 414.3. HPLC (Condition A), Rt: 3.77 min (HPLC purity: 99.1%).

後処理

customThe same procedure as employed in the preparation of Example 226 (step a) but

出典と根拠

ORDレコード: ord-1c9a1a790907498685ef3ef83e25445a
出典データセット: uspto-grants-2009_09
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US07592477B2

反応ノート

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