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2-[(5-Chlorothiophen-2-yl)oxy]acetic acid → 1-(4-Amino-quinazolin-7-ylmethyl)-4-[(5-chloro-thiophen-2-yloxy)-acetyl]-3-(S)-propyl-piperazin-2-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-[(5-Chlorothiophen-2-yl)oxy]acetic acid | HCID 11183144 | — |
| 反応物 | 1-(4-Aminoquinazoline-7-ylmethyl)-3-propyl-piperazine-2-one | HCID 17985268 | — |
| 生成物 | 1-(4-Amino-quinazolin-7-ylmethyl)-4-[(5-chloro-thiophen-2-yloxy)-acetyl]-3-(S)-propyl-piperazin-2-one | HCID 9956530 | — |
反応手順
The title compound is prepared as described in EXAMPLE 123, using 1-(4-aminoquinazoline-7-ylmethyl)-3-propyl-piperazine-2-one, EXAMPLE 78 and 5-chloro-2-thienyloxyacetic acid, EXAMPLE 24. 1H NMR (d6-DMSO, 300 MHz) δ9.78 (bs, 2H), 8.81 (s, 1H), 8.35 (d, 1H), 7.60 (m, 2H), 7.51 (s, 1H), 6.69 (m, 1H), 6.21 (d, 1H), 4.91 (AB, 2H), 4.72 (m, 2H), 3.84 (m, 1H), 3.52 (m, 2H), 3.23 (m, 1H), 1.80 (m, 2H), 1.24 (m, 2H), 0.82 (m, 3H). MS (ion spray), m/z, 474, 476, (M+H) (Cl pattern). Elemental analysis, cal C22H22ClN5O2S.C2HF3O2.1.15H2O % C=47.31, % H=4.52, % N=11.50; found % C=47.39, % H=4.140, % N=11.19.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07612075B2 |
| 出典データセット | uspto-grants-2009_11 |
| ORD ID | ord-f0c8b4fbe35546b48878659b93b0e1c1 |
| 出典メモ | uspto-grants-2009_11 |