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New Rosuvastatine intermediate, the preparation method thereof and the preparation method of Rosuvastatine hemicalcium salt using the same
专利权人:
发明人:
황성관,박장하,양준하
申请号:
KR1020110074429
公开号:
KR1013689740000B1
申请日:
2011.07.27
申请国别(地区):
KR
年份:
2014
代理人:
摘要:
PURPOSE: A novel intermediate of rosuvastatin hemicalcium salts is provided to easily prepare a crystalline intermediate with a high purity and a high yield without complex purification. CONSTITUTION: A novel rosuvastain intermediate is denoted by chemical formula 1. The DSC(Differential Scanning Calorimetry) value of a compound is 128 deg. C. at a heating rate of 5 deg. C./min. In an X-ray powder diffraction spectrum, a peak of diffraction angle(2theta =/- 0.2 deg.) is 5.6, 9.4, 13.5, 17.4, 18.8, 19.7, 20.5, 21.6, 22.3, and 22.9 when the wavelength of a light source is Cu-Kalpha 1.5406 angstrom. A method for preparing the compound of chemical formula 1 comprises a step of reacting a compound of chemical formula 2 with a compound of chemical formula 3 at 20-120 deg. C. under the presence of a base. The method further comprises a step of crystallizing the result using a crystallizing solvent of C1-C6 alcohol.본 발명은 로수바스타틴 헤미칼슘염의 신규한 중간체인 결정형 메틸 6-[(1E)-2-[4-(4-플루오로페닐)-6-(1-메틸에틸)-2-[메틸(메틸설포닐)아미노]-5-피리미딘일]에테닐]-2,2-디메틸-1,3-디옥산-4-아세테이트를 제공하며, 이의 제조방법 및 이를 이용한 로수바스타틴 헤미칼슘염을 제조하는 방법을 제공한다. 본 발명의 신규한 중간체는 결정형이며, 컬럼크로마토 그래피와 같은 복잡한 정제 공정 없이 결정화 용매로 용이하게 고순도 및 고수율로 제조가능케 하는 효과가 있다.
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