関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Acetic Acid | HCID 176 | — |
| 反応物 | (1-Ethoxycyclopropoxy)trimethylsilane | HCID 2734686 | — |
| 反応物 | Sodium cyanoborohydride | HCID 5003444 | — |
| 反応物 | (4-Morpholin-4-ylmethyl-phenyl)piperazin-1-yl-methanone | HCID 59218186 | — |
| 溶媒 | Methanol | HCID 887 | — |
| 生成物 | Bavisant | HCID 16061509 | — |
反応手順
A solution of (4-morpholin-4-ylmethyl-phenyl)-piperazin-1-yl-methanone (0.128 g) in methanol (7.5 mL) was treated with (1-ethoxy-cyclopropoxy)-trimethyl-silane (1.5 mL), acetic acid (0.2 mL), and NaBH3CN (˜400 mg). The mixture was heated at 60° C. for 18 h, and then was cooled to room temperature and concentrated. The residue was diluted with 1 N NaOH and extracted with CH2Cl2. The organic layer was dried (Na2SO4) and concentrated. The residue was purified by column chromatography (SiO2) to yield the title compound.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US07728129B2 |
|---|
| 出典データセット | uspto-grants-2010_06 |
|---|
| ORD ID | ord-7ed386d7e56a467c9382415fc0799b9b |
|---|
| 出典メモ | uspto-grants-2010_06 |
|---|
