Zhejiang Huahai Pharmaceutical Co., Ltd.

Shanghai Syncores Technologies Inc. Ltd.

Shanghai Aobo Pharmtech, Inc., Ltd.

Jicheng Zhang

Luning Huang

Anping Tao

Hong Gu

Zeng Li

Siyuan Li

Shaoxiao Gui

Chen Liu

Jianguo An

Eric Gu

Qian Chen

Xing Li

Wenjing Liao

Huaxiang Ye

Jianfeng Ge

Genliang Wang

Xianliang He

Xiaosong Cheng

The present application relates to a method for citalopram intermediate citalopram diol. The method comprises: first mixing two Grignard reagents required for a reaction; then mixing the mixed Grignard reagents with a raw material 5-cyanophthalide in a temperature-controllable micromixer to obtain a reaction solution; then subjecting the reaction solution to the reaction by means of a reactor to obtain a citalopram diol reaction solution; and then performing operations such as quenching, concentration, extraction, acidification, and crystallization to obtain a qualified product. The citalopram diol provided in the present invention has good selectivity, high yield, high safety, safety and reliability, and little sewage discharge, and is suitable for industrial production.

Method for continuously preparing citalopram diol

The present application relates to a synthesis method for cariprazine, comprising performing an acylation reaction between a compound represented by formula (I) and dimethylcarbamoyl chloride in a reaction solvent in the presence of an aqueous solution of an inorganic base, so as to obtain the cariprazine compound represented by formula (II). The synthesis method overcomes defects in the prior art such as a long reaction time, large size impurities and the difficulty of purification, and provides a new method suitable for commercial production wherein the reaction is fast, impurity sizes are small, the product is easily purified, the purity of the product can reach 99.0% or more, and the yield is high. 

Synthesis method for cariprazine

Provided are a fosaprepitant phosphate intermediate (IV) preparation method, a fosaprepitant phosphate intermediate (IV-A) and a method of (AA) for preparing fosaprepitant dimeglumine by using the intermediate (IV-A). IV: Rand Rare independently selected from C1-C7 alkyl groups or benzyl groups; IV-A: Rand Rare independently selected from C1-C7 alkyl groups, and Rand Rare not both benzyl groups.

Fosaprepitant phosphate intermediate and preparation method therefor

The present application provides a method for preparing nintedanib. The method of the present application is carried out by using 4-halo-3-nitro-benzoic acid methyl ester (compound II) and 3-oxo-3-phenylpropionate (compound III) as raw materials, and preparing nintedanib via intermediates of methyl 4-(1-alkoxy-1,3-dioxo-3-phenyl propan-2-yl)-3-nitrobenzoate (compound IV) and methyl 3-benzoyl-2-oxoindoline-6-formate (compound V). The method for preparing nintedanib (I) provided by the present application has the advantages of using easily obtained raw materials, having a simple process, being cost effective and environmentally friendly, and is suitable for industrial-scale production.

Methods for preparing Nintedanib and intermediates thereof

The invention relates to a method for preparing an oxazolidinone intermediate. Specifically, a synthesis procedure for the intermediate comprises: directly performing a 'one-pot' reaction on a compound I, compound J or compound L without performing isolation, wherein a salt of a compound K is selected from a hydrochloride, sulfate, malate, tartrate, p-toluenesulfonate, or lactate, and wherein the symbol * in a compound indicates an atom of an R-type chirality or an S-type chirality or a racemate thereof. 

Method for preparing oxazolidinone intermediate

The present invention relates to a preparation method for a tedizolid compound in Formula I. In Formula I, R is selected from hydrogen, formula A, formula B, benzyl or benzyl substituted by a substituent, the substituent is selected from a group consisting of halogen, nitryl, C-Calkyl, and C-Calkoxy, and Ris C-Calkyl or C-Calkyl substituted by halogen. The method comprises: generating a compound having a structure as shown in Formula C and a compound having a structure as shown in Formula D by a coupled reaction under the catalysis of a metal catalyst, a substituent of R being defined as above, where X is a leaving group, the leaving group comprising chlorine, bromine, iodine, and sulfonyl oxy such as trifluoromethane sulfonic oxy, methylsulfonyl oxy and benzenesulfonyl oxy, or benzenesulfonyl oxy substituted by one or more substituents, the substituent being selected from a group consisting of halogen, C-Calkyl, and C-Calkoxy. 

Preparation method for tedizolid, tedizolid intermediate, and preparation method therefor

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Shanghai, China

Jicheng Zhang