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(3-Amino-5-(methoxycarbonyl)phenyl)boronic acid → methyl 3-(2-(1H-indazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-5-aminobenzoate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | (3-Amino-5-(methoxycarbonyl)phenyl)boronic acid | HCID 2737799 | — |
| 反応物 | 4-(4,4,5,5-Tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazole | HCID 45480186 | — |
| 反応物 | 4-(2-Chloro-6-iodothieno[3,2-d]pyrimidin-4-yl)morpholine | HCID 59593061 | — |
| 生成物 | methyl 3-(2-(1H-indazol-4-yl)-4-morpholinothieno[3,2-d]pyrimidin-6-yl)-5-aminobenzoate | HCID 59592844 | — |
反応手順
2-Chloro-6-iodo-4-morpholinothieno[3,2-d]pyrimidine 19 (50 mg) was coupled to 3-amino-5-methoxycarbonylphenyl boronic acid, and then reacted with 4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-indazole via General Procedure F. The product was purified by reverse phase HPLC to yield 5.2 mg of 300. MS. (Q1) 487.1 (M)+
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08450315B2 |
| 出典データセット | uspto-grants-2013_05 |
| ORD ID | ord-64270aa4cfd64d6d9da16249e4316e77 |
| 出典メモ | uspto-grants-2013_05 |