Tianjin University

Asymchem Laboratories (tianjin) Co., Ltd.

Feng Zhang

Jiangping Lu

Hao Hong

Baohong Hou

Ying Bao

Chuang Xie

Xichun Feng

Ting Zhang

Xingfang Sun

Yinghui Chai

Peihua Liang

The present disclosure discloses a method and a device for continuously synthesizing cyclopropane compounds. The method includes the following steps: continuously performing a synthetic reaction of a diazomethane precursor in a first reactor, the reaction product of the first reactor flowing into a separator for stratification, the organic phase obtained by stratification overflowing into a second reactor, continuously consuming the diazomethane precursor in a second reactor to prepare diazomethane and performing an electron-rich monoolefin cyclopropanation reaction in situ so as to obtain the cyclopropane compound.

Method and device for continuously synthesizing cyclopropane compounds

The disclosure relates to etoricoxib solvates and a preparation method thereof. A solvent is a hydrogen bond donor solvent with a polarity value &#x3c0;* ranging from 60 to 100 or a hydrogen bond acceptor solvent with a polarity value &#x3c0;* ranging from 92 to 100. Solvents with a polarity value &#x3c0;* within the above range all can form corresponding etoricoxib solvates with etoricoxib. The etoricoxib solvate can be prepared by cooling crystallization or suspension crystallization. A 1,2-propanediol solvate of etoricoxib and a dimethyl sulfoxide (DMSO) solvate of etoricoxib provided in the present disclosure have high thermal stability, unique crystal form, large size, concentrated distribution, and prominent flowability and is safe, pharmaceutically acceptable, and not easy to agglomerate. Compared with etoricoxib, the etoricoxib solvates exhibit significantly improved solubility. Moreover, preparation of the solvates requires low consumption in time, energy, and solvent, and has high efficiency, with a molar yield higher than 90%.

Etoricoxib solvates and preparation method thereof

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Tianjin, China

Feng Zhang