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N-methyl-2-pyrrolidone → Hydrochloric Acid
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | N-methyl-2-pyrrolidone | HCID 13387 | — |
| 反応物 | 6-Morpholinonicotinoyl Chloride | HCID 2776461 | — |
| 反応物 | N-((1S,2R,3S,4R)-4-{2-((R)-3-Amino-pyrrolidin-1-yl)-6-[2,2-bis-(4-hydroxy-phenyl)-ethylamino]-purin-9-yl}-2,3-dihydroxy-cyclopentyl)-propionamide | HCID 66630815 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | Hydrochloric Acid | HCID 313 | — |
| 生成物 | N-{(R)-1-[6-[2,2-Bis-(4-hydroxy-phenyl)-ethylamino]-9-((1R,2S,3R,4S)-2,3-dihydroxy-4-propionylamino-cyclopentyl)-9H-purin-2-yl]-pyrrolidin-3-yl}-6-morpholin-4-yl-nicotinamide hydrochloride | HCID 66630618 | — |
反応手順
A suspension of N-((1S,2R,3S,4R)-4-{2-((R)-3-amino-pyrrolidin-1-yl)-6-[2,2-bis-(4-hydroxy-phenyl)-ethylamino]-purin-9-yl}-2,3-dihydroxy-cyclopentyl)-propionamide (20 mg, 33 μmol) in dry THF is treated with NMP (0.5 ml) followed by TEA (13.4 mg, 0.13 mmol) and 6-morpholinonicotinoyl chloride (8.3 mg, 37 μmol). The reaction mixture is stirred at room temperature for 30 minutes and then the solvent is removed in vacuo. Purification by C-18 reverse phase column chromatography eluting with acetonitrile:water:HCl (0.1%) (gradient of 0 to 100% acetonitrile) yields the title compound. (MH+ 793.4)
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08318750B2 |
| 出典データセット | uspto-grants-2012_11 |
| ORD ID | ord-655f74af66734bccbf3efd6e022678c2 |
| 出典メモ | uspto-grants-2012_11 |