反応式
FC(F)(F)C([NH:5]C1C=CC(CC(O)=O)=CC=1)=O.[C:18]([NH:21][C:22]1[CH:27]=[CH:26][C:25](CC(O)=O)=[CH:24][CH:23]=1)(=[O:20])[CH3:19].N1C=CC(=O)NC1=O>>[N:5].[C:18]([NH:21][C:22]1[CH:27]=[CH:26][CH:25]=[CH:24][CH:23]=1)(=[O:20])[CH3:19]参加物
実験手順
This compound was prepared by a method similar to that described in example 11 (method 1) except that [4-(2,2,2-trifluoro-acetylamino)-phenyl]-acetic acid (prepared by the method of K. D. Janda et al, as described in J. Amer. Chem. Soc. 1991, 113, 291) was used in place of (4-acetylamino-phenyl)-acetic acid. A mixture of products arising from mono-alkylation at the 1 position of the 1H-pyrimidine-2,4-dione and bis-alkylation at both the 1 position of the 1H-pyrimidine-2,4-dione and acetanilide nitrogen were obtained. When this mixture of compounds was directly subjected to the conditions used to effect cyclization to the xanthine the trifluoroacetyl groups were removed by hydrolysis. A 2:1 mixture of 8-(amino-benzyl)-3-butyl-1-(2-fluorobenzyl)-3,7-dihydro-purine-2,6-dione and 3-butyl-8-(4-butylamino-benzyl)-1-(2-fluorobenzyl)-3,7-dihydro-purine-2,6-dione was obtained which was separated by chromatography using silica gel eluted with 96:4 chloroform/methanol. MS, m/z(M+)=421.1914.
後処理
- customThis compound was prepared by a method similar to
- customprepared by the method of K
- additionA mixture of products
出典と根拠
- ORDレコード
- ord-092549754f244f38977d3dbefa233536
- 出典データセット
- uspto-grants-2006_11
- 特許番号
- US07135475B2
関連ノート
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