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Acetone → 8-{3-[4-(bis(4-fluorophenyl)hydroxymethyl)-1-piperidinyl]propoxy}-2,3-dihydro-7-methoxy-cyclopenta[c][1]benzopyran-4(1H)-one
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Acetone | HCID 180 | — |
| 反応物 | Fumarate | HCID 5460307 | — |
| 反応物 | Bis(4-fluorophenyl)(piperidin-4-yl)methanol | HCID 11208889 | — |
| 反応物 | 8-(3-chloropropoxy)-2,3-dihydro-7-methoxycyclopenta[c][1]benzopyran-4(1H)-one | HCID 19927690 | — |
| 溶媒 | Water | HCID 962 | — |
| 溶媒 | tert-Butyl methyl ether | HCID 15413 | — |
| 生成物 | 8-{3-[4-(bis(4-fluorophenyl)hydroxymethyl)-1-piperidinyl]propoxy}-2,3-dihydro-7-methoxy-cyclopenta[c][1]benzopyran-4(1H)-one | HCID 19927669 | 67% |
反応手順
Method B (38 h at 60° C.); starting materials: 8-(3-chloropropoxy)-2,3-dihydro-7-methoxy-cyclopenta[c][1]benzopyran-4(1H)-one (example 83) and 4-[bis(4-fluorophenyl)hydroxy-methyl]piperidine; yield 67%; fusion point 91° C. (decomposes; from acetone and TBME). Fumarate (×0.5 C4H4O4): method E; yield 70%; fusion point 191° C. (decomposes; from water).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US05428038 |
| 出典データセット | uspto-grants-1995_06 |
| ORD ID | ord-bb603f9d9f244b9cb7303716b685f5eb |
| 出典メモ | uspto-grants-1995_06 |