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4-Fluorobenzylamine → Benzyl (2-{[(4-fluorobenzyl)amino]carbonyl}-3-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)carbamate

HRID 547385
ノート
印刷プレビュー

反応式

HRID 547385 の反応式
[CH2:1]([O:8][C:9]([NH:11][C:12]1[C:17]2=[N:18][C:19]([C:24](OC)=[O:25])=[C:20]([OH:23])[C:21](=[O:22])[N:16]2[CH:15]=[CH:14][CH:13]=1)=[O:10])[C:2]1[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=1.[F:28][C:29]1[CH:36]=[CH:35][C:32]([CH2:33][NH2:34])=[CH:31][CH:30]=1>CO>[F:28][C:29]1[CH:36]=[CH:35][C:32]([CH2:33][NH:34][C:24]([C:19]2[N:18]=[C:17]3[C:12]([NH:11][C:9](=[O:10])[O:8][CH2:1][C:2]4[CH:7]=[CH:6][CH:5]=[CH:4][CH:3]=4)=[CH:13][CH:14]=[CH:15][N:16]3[C:21](=[O:22])[C:20]=2[OH:23])=[O:25])=[CH:31][CH:30]=1
参加物反応条件実験手順後処理出典と根拠反応ノート

参加物

4

反応物 2

HCID 673264-FluorobenzylamineHCID 54751204Methyl 9-{[(benzyloxy)carbonyl]amino}-3-hydroxy-4-oxo-4-H-pyrido[1,2-a]pyrimidine-2-carboxylate

生成物 1

HCID 86761308Benzyl (2-{[(4-fluorobenzyl)amino]carbonyl}-3-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidin-9-yl)carbamate

試薬・触媒・溶媒 1

HCID 887Methanol溶媒

反応条件

温度
80 °C

実験手順

To a suspension of methyl 9-{[(benzyloxy)carbonyl]amino}-3-hydroxy-4-oxo-4-H-pyrido[1,2-a]pyrimidine-2-carboxylate in MeOH was added p-fluorobenzylamine. The suspension was stirred at 80° C. and after 16 hours the solvent was removed under reduced pressure. The product was purified by preparative RP-HPLC, using water (0.1% TFA) and acetonitrile (0.1% TFA) as eluants (column: C18). The product was obtained after lyophilization of the pooled product fractions as bright yellow fluffy material.

後処理

  1. customwas removed under reduced pressure
  2. customThe product was purified by preparative RP-HPLC
  3. customThe product was obtained after lyophilization of the pooled product fractions as bright yellow fluffy material

出典と根拠

ORDレコード
ord-45db45cb4c164866a970a26e573cbc9f
出典データセット
uspto-grants-2011_05
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US07939537B2

反応ノート

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このページの内容参加物反応条件実験手順後処理出典と根拠反応ノート