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公开(公告)号：US20210300883A1
公开(公告)日：2021-09-30
申请号：US17266955
申请日：2019-08-06
发明人： Wenjing LIAO , Jianfeng GE , Jicheng ZHANG , Luning HUANG , Anping TAO , Eric GU
IPC分类号： C07D295/135
摘要： 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.
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公开(公告)号：US20180312476A1
公开(公告)日：2018-11-01
申请号：US15771449
申请日：2016-11-02
发明人： Siyuan LI , Shaoxiao GUI , Genliang WANG , Jicheng ZHANG , Luning HUANG , Anping TAO , Hong GU
IPC分类号： C07D263/24 , C07C217/40
摘要： 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.
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公开(公告)号：US20220024860A1
公开(公告)日：2022-01-27
申请号：US17312635
申请日：2019-12-02
发明人： Chen LIU , Xing LI , Huaxiang YE , Jicheng ZHANG , Luning HUANG , Anping TAO , Jianguo AN , Hong GU
IPC分类号： C07C253/30
摘要： 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.
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