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L-Serine → (2S)-N-[1-[(1-amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl]-3-hydroxy-2-[(2-naphthalenylsulfonyl)amino]propanamide hydrochloride
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | L-Serine | HCID 5951 | — |
| 反応物 | 2-Naphthalenesulfonyl chloride | HCID 7125 | — |
| 反応物 | (2S)-3-hydroxy-2-[(2-naphthalenylsulfonyl)amino]propanoic acid | HCID 14030411 | — |
| 反応物 | 1,1-Dimethylethyl 1-[(1-amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl-carbamate | HCID 22665607 | — |
| 反応物 | N-[1-[(1-Amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl]-2-[[(3,4-dihydro-2,2,5,7,8-pentamethyl-2H-1-benzopyran-6-yl)sulfonyl]amino]acetamide hydrochloride | HCID 22665631 | — |
| 生成物 | (2S)-N-[1-[(1-amino-6-isoquinolinyl)methyl]-2-oxo-2-(1-piperidinyl)ethyl]-3-hydroxy-2-[(2-naphthalenylsulfonyl)amino]propanamide hydrochloride | HCID 69781330 | — |
反応手順
The procedure described for 5c was used. Deprotection of 5a and coupling with (2S)-3-hydroxy-2-[(2-naphthalenyisulfonyl)amino]propanoic acid (prepared from L-serine and 2-naphthalenylsulfonylchloride using the procedure described for 5b) yielded 7. 1H-NMR 200 MHz (CD3OD) δ: 1.12-1.58 (6H, m), 2.57-2.69 (1H, m) 2.95-3.95 (8H, m), 4.9-5.1 (1H, m), 7.11-7.22 (1H, m), 7.43-8.16 (9H, m), 8.24-8.34 (1H, m), 8.41-8.45 (1H, m).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US06797710B2 |
| 出典データセット | uspto-grants-2004_09 |
| ORD ID | ord-44d0b00bd4054c32942da50141e4bd8d |
| 出典メモ | uspto-grants-2004_09 |