참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Dimethylformamide | HCID 6228 | — |
| 반응물 | Potassium Carbonate | HCID 11430 | — |
| 반응물 | 4-(3-Chloropropoxy)-3-methoxyacetophenone | HCID 7314264 | — |
| 반응물 | R-56109 hydrochloride | HCID 11334359 | — |
| 용매 | Water | HCID 962 | — |
| 생성물 | Iloperidone | HCID 71360 | 58.6% |
반응 단계
A stirred mixture of 6-fluoro-3-(4-piperidinyl)-1,2 benzisoxazole hydrochloride (5.1 g, 20 mmol), K2CO3 (5.2 g, 40 mmol), 1-[4-(3-chloropropoxy)-3-methoxyphenyl]-ethanone (5.3 g, 22 mmol), and dimethylformamide (60 ml) was heated at 90° C. for 16 hours. The reaction was poured into water, and the aqueous mixture was extracted with ethyl acetate. The ethyl acetate was washed (water), dried (MgSO4) and concentrated to afford a moist solid. Recrystallization (twice) from ethyl alcohol afforded 5.0 g (58%) of 1-[4-[3-[4-(6-fluoro-1,2-benzisoxazol-3-yl)-1-piperidinyl]-propoxy]-3-methoxyphenyl]-ethanone as a beige solid, m.p.=118°-120° C.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 특허 번호 | US05624927 |
|---|
| 출처 데이터셋 | uspto-grants-1997_04 |
|---|
| ORD ID | ord-5b85e800ef074400805726359dcfd768 |
|---|
| 출처 메모 | uspto-grants-1997_04 |
|---|
