-
公开(公告)号:US10550109B2
公开(公告)日:2020-02-04
申请号:US16300301
申请日:2017-05-12
发明人: Yinglu Jiao , Handa Li , Boyu Wang , Luning Huang , Xi Chen , Hong Gu
IPC分类号: C07D409/14
摘要: Disclosed are a crystal form of brexpiprazole and a preparation method therefor. The X-ray powder diffraction pattern, which is detected with Cu—Kα radiation, of the crystal form of brexpiprazole has characteristic peaks at the positions where 2θ is about 9.1±0.2, 15.2±0.2, 15.7±0.2, 17.6±0.2, 18.1±0.2, 24.4±0.2. The crystal form I of brexpiprazole has a high purity, good stability and good reproducibility, and is suitable for industrial production.
-
公开(公告)号:US11845710B2
公开(公告)日:2023-12-19
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
CPC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.
-
公开(公告)号:US12084425B2
公开(公告)日:2024-09-10
申请号:US17295843
申请日:2019-10-12
IPC分类号: C07D307/87
CPC分类号: C07D307/87 , C07B2200/13
摘要: Provided herein is a method for preparing an Escitalopram bis-hydroxynaphtoate ((S)-(+)-1-(3-(-(dimethylamino)propyl)-1-(4-fluorophenyl)-1,3-dihydro-5-cyanisob enzofuranone) crystal form A. Said method is ecofriendly and non pollutive, and the obtained Escitalopram bis-hydroxynaphtoate crystal form A is highly pure and easy to reproduce.
-
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.
-
公开(公告)号:US11014885B2
公开(公告)日:2021-05-25
申请号:US16618896
申请日:2018-06-05
IPC分类号: C07D211/32 , C07C63/46
摘要: Disclosed is a new method for preparing a donepezil pamoate (1-benzyl-4-[(5,6-dimethoxyindan-2-one)methyl]piperidine pamoate). The donepezil pamoate prepared by using the method has a high purity and a good flowability.
-
公开(公告)号:US10590154B2
公开(公告)日:2020-03-17
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: C07D401/04 , C07D263/24 , C07F9/6558 , C07D413/14 , C07C213/00 , C07C217/48 , C07C231/10 , C07C235/78 , C07D263/20 , C07C217/40 , B01J27/055 , B01J27/122 , B01J31/02 , B01J31/22 , B01J31/28 , B01J31/30
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.
-
公开(公告)号:US20200087273A1
公开(公告)日:2020-03-19
申请号:US16618898
申请日:2018-06-05
IPC分类号: C07D307/87
摘要: The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability.
-
公开(公告)号:US20190040052A1
公开(公告)日:2019-02-07
申请号:US16073929
申请日:2017-01-25
发明人: Jianping Lin , Xiaowen Guo , Xiaofei Gao , Chao Huang , Yuanbing Guo , Anping Tao , Luning Huang , Hong Gu
IPC分类号: C07D413/14 , C07D413/04
摘要: The present invention relates to a synthesis process of suvorexant, novel compounds represented by formulas II, III, IV or V, or salts thereof for preparing suvorexant, and a method for preparing the intermediates. The preparation method uses a chiral starting material to synthesize chiral compounds represented by formulas II, III, IV or V, the compounds obtained being used for synthesizing the suvorexant. The preparation method has the advantages of simple operation, low cost, mild reaction conditions, simple post-treatment, easy to purify, high yield, high ee value for the product, and easy to industrialize. In the reaction route shown, R represents benzyl, allyl or 1-phenethyl, or optionally substituted benzyl at the 2 position to 6 position, such as 4-methoxybenzyl, 4-nitrobenzyl, 2-methylbenzyl, 4-chlorobenzyl or 3-fluorobenzyl.
-
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.
-
公开(公告)号:US11168063B2
公开(公告)日:2021-11-09
申请号:US16618898
申请日:2018-06-05
IPC分类号: C07D307/87
摘要: The present invention relates to a new preparation method for escitalopram pamoate ((S)-(+)-1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)-1,3-dihydro-5-cyanoisob enzofuran pamoate), wherein the method is environmentally friendly and pollution-free, and the escitalopram pamoate prepared by means of the method has a high purity and a good repeatability.
-
-
-
-
-
-
-
-
-