Dichloromethane methanol → 4-({cis-4-[(2,3-Dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)amino]-3-fluoro-1-piperidinyl}methyl)-3-fluoro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one Hydrochloride

HRID 15335

反応式

HRID 15335 の反応式
[NH2:1][C@H:2]1[CH2:7][CH2:6][N:5]([CH2:8][CH:9]2[C:13]3=[C:14]([F:22])[CH:15]=[N:16][C:17]4[CH:18]=[CH:19][C:20](=[O:21])[N:11]([C:12]=43)[CH2:10]2)[CH2:4][C@H:3]1[F:23].[O:24]1[C:33]2[CH:32]=[C:31]([CH:34]=O)[N:30]=[CH:29][C:28]=2[O:27][CH2:26][CH2:25]1.[Cl:36]CCl.CO>>[ClH:36].[O:24]1[C:33]2[CH:32]=[C:31]([CH2:34][NH:1][C@H:2]3[CH2:7][CH2:6][N:5]([CH2:8][CH:9]4[C:13]5=[C:14]([F:22])[CH:15]=[N:16][C:17]6[CH:18]=[CH:19][C:20](=[O:21])[N:11]([C:12]=65)[CH2:10]4)[CH2:4][C@H:3]3[F:23])[N:30]=[CH:29][C:28]=2[O:27][CH2:26][CH2:25]1

参加物

4

反応物 3

HCID 21226129Dichloromethane methanolHCID 218736682,3-Dihydro[1,4]dioxino[2,3-c]pyridine-7-carbaldehydeHCID 686856724-{[cis-4-amino-3-fluoro-1-piperidinyl]methyl}3-fluoro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one

生成物 1

HCID 686854954-({cis-4-[(2,3-Dihydro[1,4]dioxino[2,3-c]pyridin-7-ylmethyl)amino]-3-fluoro-1-piperidinyl}methyl)-3-fluoro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one Hydrochloride収率 82%

実験手順

The free base of the title compound was prepared from 4-{[cis-4-amino-3-fluoro-1-piperidinyl]methyl}3-fluoro-4,5-dihydro-7H-pyrrolo[3,2,1-de]-1,5-naphthyridin-7-one and 2,3-dihydro[1,4]dioxino[2,3-c]pyridine-7-carboxaldehyde (for a synthesis see WO2004058144, Example 2(c)) according to the general method of Example 2(h), chromatographing with dichloromethane/methanol/0.88 ammonia 95:5:0.5, in 82% yield.

出典と根拠

ORDレコード
ord-abecd2ee907843208d511a526fc821ee
出典データセット
uspto-grants-2010_06
特許番号
US07732461B2

関連ノート

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