Zhejiang Hisun Pharmaceutical Co., Ltd.

Shanghai Institute of Pharmaceutical Industry

Hairong Luo

Jian Chai

Liang Zhang

Hua Bai

Fuli Zhang

Zhiqing Yang

Xuyang Zhao

Xiaoyu Liu

Xiaohe Zheng

Jiang Li

Qifeng Zhu

Yuncai Zhang

Xiaojie Xu

Bin Liang

Xiangyang Zhang

Maojian Gu

Yong Zhang

Hongying Luo

Qingfeng Cai

Chunbo Yang

Pengcheng Qiu

Jinyi Xu

Dejin Fu

Zhenjuan Shi

Zhi Chen

Ying Chen

Zhaozhao Zhang

Chuan Liu

Di Su

The present invention relates to novel crystal forms M and N of dabigatran etexilate mesylate and preparation method and uses thereof, wherein the X-Ray powder diffractogram of the crystal form M has characteristic peaks at the following 2&#x3b8; diffraction angles: 5.7&#xb1;0.2&#xb0;, 6.2&#xb1;0.2&#xb0;, 11.2&#xb1;0.2&#xb0;, 12.4&#xb1;0.2&#xb0;, 18.2&#xb1;0.2&#xb0;, 21.4&#xb1;0.2&#xb0;, 21.8&#xb1;0.2&#xb0; and 23.6&#xb1;0.2&#xb0;; and the X-Ray powder diffractogram of the crystal form N has characteristic peaks at the following 2&#x3b8; diffraction angles: 6.0&#xb1;0.2&#xb0;, 11.8&#xb1;0.2&#xb0;, 18.2&#xb1;0.2&#xb0;, 21.6&#xb1;0.2&#xb0;, 24.4&#xb1;0.2&#xb0;, 27.7&#xb1;0.2&#xb0; and 29.7&#xb1;0.2&#xb0;. The crystal forms of the present invention have excellent properties in the aspects of leaching time, biological release, chemical stability and processing adaptability.

Crystal form of dabigatran etexilate mesylate and preparation method and use thereof

Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) (I), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production. 

Method for preparing linezolid intermediate

Preparation of azetidinone compounds and medical use thereof are provided by the present invention. More particularly, azetidionne compounds, shown as formula (I), wherein R, R, R, R, Rand Rare defined in description, and preparation methods thereof are provided by the present invention. The compounds of the present invention can reduce the levels of total cholesterol (TC) and low density lipoprotein cholesterol (LDL-C) in plasma, and can be used as medicaments for reducing cholesterol in blood. Therefore the compounds of the present invention can be used to treat or prevent diseases of atherosclerosis, cacergasia of blood vessel, cardiac failure, coronary artery disease, angiocardiopathy, myocardial, angina, hyperlipoidemia and hypercholesteremia and the like. Preparation method of compounds of formula (I) and intermediate compounds are also provided by the present invention. 

Azetidinone compounds and medical use thereof

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Zhejiang, China

Hairong Luo