105685-06-1Relevant articles and documents
SALT OF CYCLOHEXANE DERIVATIVE
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Paragraph 0117-0119, (2021/10/11)
The present invention provides a maleate, phosphate, sulfate, hydrochloride of a cyclohexane derivative, N′-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl]ethyl]cyclohexyl]-N,N-dimethylurea, as shown in Formula I and crystal forms thereof. The crystal forms have low hygroscopicity and good stability and are convenient for long-term storage and transportation; or the crystal forms have a long half-life in vivo, high bioavailability and small individual difference, and thus have obvious clinical application advantages.
Benzothiophene derivative and preparation method thereof
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, (2020/05/14)
The invention discloses a benzothiophene derivative and a preparation method thereof. The structural formula of the benzothiophene derivative is shown as the following formula 2 or formula 3, and R1 is halogen, benzenesulfonyloxy, p-toluenesulfonyloxy, trifluoromethanesulfonyloxy or methanesulfonyloxy. The benzothiophene derivative disclosed by the invention can be used for further preparing 7-piperazinyl benzothiophene, a compound I, salt of the compound I and other substances. The preparation method disclosed by the invention has advantages of simple reaction, mild condition and relatively high total reaction yield.
Crystal form of cyclohexane derivative
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Paragraph 0045; 0047-0049, (2020/03/02)
The invention relates to a crystal form of a compound, namely a cyclohexane derivative N'-[trans-4-[2-[7-(benzo[b]thiophene)-7-piperazinyl] ethyl] cyclohexyl]-N,N-dimethyl urea of a formula I shown inthe description, and a preparation method of the compound. An XRPD (X-ray powder diffraction) spectrum which has CuKalpha radiation and is presented by 2theta angles, of the crystal form, has diffraction peaks at 9.151+/-0.2 degrees, 13.856+/-0.2 degrees, 16.219+/-0.2 degrees and 18.585+/-0.2 degrees at least. The crystal form is low in dehumidification, good in stability and convenient for long-term storage and transportation.
Preparation method of cyclohexane derivative maleate crystal form
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Paragraph 0048-0052, (2020/06/09)
The invention relates to a preparation method of a maleate crystal form of a compound cyclohexane derivative N'-[trans-4-[2-[7-(benzo[b]thiophene)-4-yl-1-piperazine]ethyl]cyclohexyl]-N,N-dimethylurearepresented by a formula I. The crystal form is an anhydrous crystal form and is generated under the condition that the water activity is less than or equal to 0.6 solvent.
Preparation method of benzothiophene derivative
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, (2020/07/02)
The invention provides a preparation method of a benzothiophene derivative, which comprises the following steps: reacting a compound shown as a formula 2 with dimethylamine under the conditions of anorganic solvent, an acid-binding agent and an additive to obtain a compound shown as a formula 1, namely the benzothiophene derivative. The preparation method provided by the invention is a benzothiophene derivative which is simple in reaction, mild in condition, few in reaction steps, few in reaction byproducts, simple in aftertreatment, high in yield, high in purity and easy for industrial production.
Method for preparing benzothiophene derivative
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Paragraph 0060-0062, (2020/05/14)
The invention relates to a method for preparing a benzothiophene derivative. The method comprises the following steps: taking 7-nitrothiophene as a raw material, and forming a thiophene derivative through nucleophilic substitution. The method provided by the invention has the advantages of mild reaction conditions, simple operation, controllable post-treatment and convenient quality control, and is beneficial to large-scale industrial production.
Preparation method of 7-piperazinyl benzothiophene or salt thereof
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, (2020/05/14)
The invention discloses a preparation method of 7-piperazinyl benzothiophene or salt thereof, comprising the following steps: (1) carrying out substitution ring closing reaction on a compound 3 and acompound 4 to obtain a compound 5; (2) carrying out hydr
