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Diisopropylethylamine → methyl (2S)-2-({[2-amino-4-(4-methylpiperazin-1-yl)quinazolin-7-yl]carbonyl}amino)-3-biphenyl-4-ylpropanoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Diisopropylethylamine | HCID 81531 | — |
| 反応物 | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| 反応物 | (S)-Methyl 3-([1,1'-biphenyl]-4-yl)-2-aminopropanoate | HCID 15714801 | — |
| 反応物 | 2-Amino-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxylic acid | HCID 59496649 | — |
| 溶媒 | Dimethylformamide | HCID 6228 | — |
| 生成物 | methyl (2S)-2-({[2-amino-4-(4-methylpiperazin-1-yl)quinazolin-7-yl]carbonyl}amino)-3-biphenyl-4-ylpropanoate | HCID 49779038 | 13.6% |
反応手順
N,N,N′,N′-Tetramethyl-O-(7-azabenzotriazol-1-yl)uronium hexafluorophosphate (42 mg, 0.11 mmol) was added to a solution of 2-amino-4-(4-methylpiperazin-1-yl)quinazoline-7-carboxylic acid (20 mg, 0.07 mmol) in N,N-dimethylformamide (2 mL) and N,N-diisopropylethylamine (24 uL, 0.14 mmol). The methyl (2S)-2-amino-3-biphenyl-4-ylpropanoate (36 mg, 0.14 mmol) was added. The reaction was stirred for 2 h. at r.t., and was purified by RP-HPLC (pH=2) to afford the desired product (5 mg, 10%) as a white solid TFA salt. Analytical LCMS (M+H)+: m/z=525.1.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08481732B2 |
| 出典データセット | uspto-grants-2013_07 |
| ORD ID | ord-51148be0f5ee4680ae5583e36fb1948b |
| 出典メモ | uspto-grants-2013_07 |