참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Methanesulfonic Acid | HCID 6395 | — |
| 반응물 | Eprosartan | HCID 5281037 | — |
| 용매 | Acetone | HCID 180 | — |
| 생성물 | Eprosartan Mesylate | HCID 5282474 | 91.7% |
반응 단계
Eprosartan free base (8 gm, obtained in example 3) is suspended in acetone (120 ml) at 25-30° C., the suspension is cooled to 0-5° C., methanesulfonic acid (5.4 gm) is added drop wise while maintaining the temperature at 0-5° C. The temperature of the mass is raised to 25-30° C. and stirred for 5 hours. The mass is cooled to 0-5° C., stirred for 1 hour, the material is filtered and then suck dried. To the resulting wet cake is added acetone (16 ml) and stirred for 15 minutes at 25-30° C. The material is filtered, washed with acetone (8 ml) and then dried to give 9 gm of pure eprosartan mesylate [HPLC Purity: 99.96%; Specific Surface Area: 1.11 m2/g; Mean particle size (D50): 11.23 μm and 90 volume-% of the particles (D90): 30.42 μm].
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08361507B2 |
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| 출처 데이터셋 | uspto-grants-2013_01 |
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| ORD ID | ord-a1e9f9db88014c8d80d9196bfae79ba5 |
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| 출처 메모 | uspto-grants-2013_01 |
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