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2-Methoxy-4-morpholinoaniline → 3-Methoxy-2-[4-(2-methoxy-4-morpholin-4-yl-phenylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 2-Methoxy-4-morpholinoaniline | HCID 414960 | — |
| 反応物 | 2-(4-Chloro-5-trifluoromethyl-pyrimidin-2-ylamino)-3-methoxy-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one | HCID 86634054 | — |
| 生成物 | 3-Methoxy-2-[4-(2-methoxy-4-morpholin-4-yl-phenylamino)-5-trifluoromethyl-pyrimidin-2-ylamino]-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one | HCID 66830218 | 9% |
反応手順
In an analogous manner to Example 1513, the product was prepared from 2-(4-Chloro-5-trifluoromethyl-pyrimidin-2-ylamino)-3-methoxy-5-methyl-8,9-dihydro-5H-7-oxa-5-aza-benzocyclohepten-6-one and 2-Methoxy-4-morpholin-4-yl-phenylamine. Product isolated as a white solid (8.0 mg, 9%). mp: 232-234° C., MS (ESI+): 575 (M+H), 1H-NMR (CDCl3, 400 MHz) δ 8.31 (s, 1H), 8.22 (s, 1H), 7.95 (m, 1H), 7.70 (s, 1H), 7.25 (s, 1H), 6.69 (s, 1H), 6.54 (s, 1H), 6.49 (d, J=8 Hz, 1H), 4.44 (t, J=6 Hz, 2H), 3.92 (s, 4H), 3.90 (s, 6H), 3.40 (s, 3H), 3.16 (t, J=5 Hz, 4H), 2.78 (m, 2H).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08552186B2 |
| 出典データセット | uspto-grants-2013_10 |
| ORD ID | ord-f129f9d39b4a4eaf83fbb5067032a00b |
| 出典メモ | uspto-grants-2013_10 |