Methyl 9-benzyloxy-2-(3-chlorobenzyl)-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxylate → Methyl 2-(3-chlorobenzyl)-1,8-dioxo-9-hydroxy-1,3,4,8-tetrahydro-2h-pyrido[1,2-a]pyrazine-7-carboxylate

HRID 1349497ノート

反応式

HRID 1349497 の反応式
C(OC1C(=O)C(Br)=CN2CCN(CC3C=CC=C(Cl)C=3)C(=O)C=12)C1C=CC=CC=1.C([O:37][C:38]1[C:39](=[O:61])[C:40]([C:57]([O:59][CH3:60])=[O:58])=[CH:41][N:42]2[CH2:47][CH2:46][N:45]([CH2:48][C:49]3[CH:54]=[CH:53][CH:52]=[C:51]([Cl:55])[CH:50]=3)[C:44](=[O:56])[C:43]=12)C1C=CC=CC=1>>[Cl:55][C:51]1[CH:50]=[C:49]([CH:54]=[CH:53][CH:52]=1)[CH2:48][N:45]1[CH2:46][CH2:47][N:42]2[CH:41]=[C:40]([C:57]([O:59][CH3:60])=[O:58])[C:39](=[O:61])[C:38]([OH:37])=[C:43]2[C:44]1=[O:56]

参加物

3

実験手順

By subjecting 9-benzyloxy-7-bromo-2-(3-chlorobenzyl)-3,4-dihydro-2H-pyrido[1,2-a]pyrazine-1,8-dione (600 mg) produced by the same method as in Example 249, Step 1 to a reaction operation similar to that in Example 161, Step 3, a mixture of methyl 9-benzyloxy-2-(3-chlorobenzyl)-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxylate and methyl 2-(3-chlorobenzyl)-1,8-dioxo-9-hydroxy-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxylate was obtained (13 mg). This mixture was dissolved in dimethylformamide (17 ml) and treated with benzyl bromide (1.36 g) and potassium carbonate (1.75 g) and purified by silica gel column chromatography (ethyl acetate-chloroform:methanol=10:1) to give methyl 9-benzyloxy-2-(3-chlorobenzyl)-1,8-dioxo-1,3,4,8-tetrahydro-2H-pyrido[1,2-a]pyrazine-7-carboxylate (480 mg).

後処理

  1. customproduced by the same method as in Example 249, Step 1 to a reaction operation similar to that in Example 161, Step 3

出典と根拠

ORDレコード
ord-35beb3b9099b4af6a8333c8e64adfadd
出典データセット
uspto-grants-2007_05
特許番号
US07211572B2

反応ノート

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