IMPROVED PROCESS OF SILODOSIN
The present invention relates to an improved method for manufacturing silodosin and, more specifically, to an improved manufacturing method for performing an N-alkylation reaction using oxetan under Lewis acid catalysts in a step of inducing a 3-hydroxypropyl group on an N1 position of indolin. Ther...
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| Format: | Patent |
| Sprache: | eng ; kor |
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| Zusammenfassung: | The present invention relates to an improved method for manufacturing silodosin and, more specifically, to an improved manufacturing method for performing an N-alkylation reaction using oxetan under Lewis acid catalysts in a step of inducing a 3-hydroxypropyl group on an N1 position of indolin. Therefore, the method is capable of obtaining high purity and high yield silodosin by maintaining a reduced manufacturing process and a mild reaction condition. In addition, the present invention relates to a method for easily obtaining a beta-type crystal of silodosin, by selectively using a good solvent and an anti-solvent suitable for amorphous silodosin.
본 발명은 실로도신의 개선된 제조방법에 관한 것으로서, 더욱 상세하게는 인돌린의 N1 위치에 3-하이드록시프로필기를 도입하는 단계에서 루이스산 촉매 하에서 옥세탄을 이용한-알킬화 반응을 수행함으로써, 단축된 제조공정과 온화한 반응조건을 유지하는 것이 가능하여 고순도 및 고수율로 실로도신을 수득할 수 있는 개선된 제조방법에 관한 것이다. 또한, 본 발명은 무정형 실로도신을 적절한 양용매(good solvent) 및 반용매(anti-solvent)를 선택 사용함으로써, 실로도신의 베타형 결정을 용이하게 수득하는 방법에 관한 것이다. |
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