Trifluoroacetic acid → 6-fluoro-1-phenyl-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one

反応式

[F:1][C:2]1[CH:3]=[CH:4][C:5]2[N:6]([C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=3)[C:7](=[O:21])[N:8](CC3C=CC(OC)=CC=3)[CH2:9][C:10]=2[N:11]=1.C(O)(C(F)(F)F)=O>>[F:1][C:2]1[CH:3]=[CH:4][C:5]2[N:6]([C:22]3[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=3)[C:7](=[O:21])[NH:8][CH2:9][C:10]=2[N:11]=1

参加物

反応物 2

HCID 6422Trifluoroacetic acid

HCID 709803326-fluoro-3-(4-methoxy-benzyl)-1-phenyl-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one

生成物 1

HCID 709815066-fluoro-1-phenyl-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one収率 59.4%

実験手順

6-Fluoro-3-(4-methoxy-benzyl)-1-phenyl-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one (300 mg, 0.83 mmol) was deprotected according to the method of General procedure 1 (TFA deprotection). The free base was isolated and purified by column chromatography (SiO2, eluted with petrol—EtOAc 0-100%) to afford 6-fluoro-1-phenyl-3,4-dihydro-1H-pyrido[3,2-d]pyrimidin-2-one (120 mg). MS: [M+H]+=244.

後処理

customThe free base was isolated
custompurified by column chromatography (SiO2, eluted with petrol—EtOAc 0-100%)

出典と根拠

ORDレコード: ord-f3fb3e652b4c447eab8e1d6c23dfa9f8
出典データセット: uspto-grants-2015_10
DOI: 10.6084/m9.figshare.5104873.v1
特許番号: US09155743B2

反応ノート

読み込み中…

参加物