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HRID 1010843作成日：2026年10月26日
Cesium carbonate → 4-[2-(5-Chloro-2-fluoro-phenyl)-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidin-4-ylamino]-nicotinic acid methyl ester
https://huagongshe.com/reaction/1010843
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Cesium carbonate | HCID 10796 | — |
| 反応物 | Methyl 4-aminopyridine-3-carboxylate | HCID 592353 | — |
| 反応物 | Binap, (A+-)- | HCID 634876 | — |
| 反応物 | 2-(5-Chloro-2-fluoro-phenyl)-4-iodo-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidine | HCID 21104309 | — |
| 触媒 | palladium(II) acetate | HCID 167845 | — |
| 溶媒 | 1,4-Dioxane | HCID 31275 | — |
| 生成物 | 4-[2-(5-Chloro-2-fluoro-phenyl)-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidin-4-ylamino]-nicotinic acid methyl ester | HCID 58866042 | 34% |
反応手順
To a solution of 2-(5-Chloro-2-fluoro-phenyl)-4-iodo-6,6-dimethyl-6,7-dihydro-5H-cyclopentapyrimidine (500 mg, 1.24 mmol), 4-amino-nicotinic acid methyl ester (208 mg, 1.37 mmol), Pd(OAc)2 (14 mg, 62.09 μmol) and Rac-BINAP (60 mg, 93.14 μmol) in dry dioxane (10 mL) was added Cs2CO3 (607 mg, 1.86 mmol). The mixture was heated for 12 h at 85° C., cooled and evaporated. The residue was purified by chromatography (CH2Cl2, 0-10% MeOH) to give the desired product (178 mg, 34% yield).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07977342B2 |
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| 出典データセット | uspto-grants-2011_07 |
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| ORD ID | ord-040016ec6429455caa5df4c81638b485 |
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| 出典メモ | uspto-grants-2011_07 |
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