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(1H-indol-5-yl)methanamine → 2-[3-({[(2R)-1-Cyclopentylpyrrolidinyl]methyl}amino)-6-methyl-2-oxo-1(2H)-pyrazinyl]-N-(1H-indol-5-ylmethyl)acetamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (1H-indol-5-yl)methanamine | HCID 54791 | — |
| 反応物 | 2-[3-({[(2R)-1-cyclopentylpyrrolidinyl]methyl}amino)6-methyl-2-oxo-1(2H)-pyrazinyl]acetic acid hydrochloride | HCID 69961888 | — |
| 生成物 | Ammonia | HCID 222 | — |
| 生成物 | 2-[3-({[(2R)-1-Cyclopentylpyrrolidinyl]methyl}amino)-6-methyl-2-oxo-1(2H)-pyrazinyl]-N-(1H-indol-5-ylmethyl)acetamide | HCID 59900526 | 16% |
反応手順
The title compound was prepared from 2-[3-({[(2R)-1-cyclopentylpyrrolidinyl]methyl}amino)6-methyl-2-oxo-1(2H)-pyrazinyl]acetic acid hydrochloride (preparation 145) and 1H-indol-5-ylmethylamine (preparation 8), following the procedure described in preparation 45. The crude product was purified by chromatography using a Biotage™ (KP-Sil™ 60 Å silica gel) cartridge and dichloromethane:methanol:0.88 ammonia (95:5:0.5) as eluant. The product was further purified using preparative tlc and dichloromethane:methanol:0.88 ammonia (90:10:1) as eluant to afford the title compound, (11 mg, 16%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06180627B2 |
| 出典データセット | uspto-grants-2001_01 |
| ORD ID | ord-867200dd73ab49e59e6b532efd6603a7 |
| 出典メモ | uspto-grants-2001_01 |