184177-81-9Relevant articles and documents
Preparation method of 4-[4-[4-(4-hydroxyphenyl) piperazine-1-yl] phenyl] phenyl carbamate
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, (2022/04/08)
The invention discloses a preparation method of 4-[4-[4-(4-hydroxyphenyl) piperazine-1-yl] phenyl] phenyl carbamate, which comprises the following steps: by taking 4-hydroxyaniline as a raw material, carrying out ring closing on the 4-hydroxyaniline and dichloroethylamine hydrochloride to synthesize 1-(4-hydroxyphenyl) piperazine with the purity of 95A% and the correction yield of 80%; 4-nitrochlorobenzene and the prepared 1-(4-hydroxyphenyl) piperazine are coupled to synthesize 4-(4-(4-nitrophenyl)-1-piperazinyl) phenol, the purity is 93 A%, and the correction yield is 88%; then carrying out nitro reduction to synthesize 1-(4-aminophenyl)-4-(4-hydroxyphenyl) piperazine with the purity of 98A% and the correction yield of 77%; and finally, synthesizing 4-[4-[4-(4-hydroxyphenyl) piperazine-1-yl] phenyl] phenyl carbamate with the purity of 98.7%, the content of 98.5 wt% and the correction yield of 83% by using phenyl chloroformate to protect phenolic hydroxyl groups. According to the invention, the high-purity target product 4-[4-[4-(4-hydroxyphenyl) piperazine-1-yl] phenyl] phenyl carbamate can be obtained through easily available raw materials and simple process steps.
Antifungal water-soluble compound as well as preparation method and application thereof (by machine translation)
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Paragraph 0095; 0107-0108, (2020/06/02)
The invention provides an antifungal water-soluble compound, a preparation method thereof and application, of the compound as I shown in formula. The compound has good antifungal effect and water solubility, can be used for treating and preventing,configuration optical isomers of the optical isomer SRSS obtained by chiral synthesis. (by machine translation)
Synthesis, Crystal Structure, Anti-Bone Cancer Activity and Molecular Docking Investigations of the Heterocyclic Compound 1-((2S,3S)-2-(Benzyloxy)Pentan-3-yl) -4-(4-(4-(4-Hydroxyphenyl)Piperazin-1-yl) Phenyl)-1H-1,2,4-Triazol-5(4H)-One
Lv,Zhang,Wang,Pan,Liu
, p. 1173 - 1179 (2019/08/12)
Heterocyclic compound 1-((2S,3S)-2-(benzyloxy)pentan-3-yl)-4-(4-(4-(4-hydroxyphenyl)piperazin-1-yl)phenyl)-1H-1,2,4-triazol-5(4H)-one (1) designed using 4-(4-(4-aminophenyl)piperazin-1-yl)phenol (2) and (S)-N′-(2-(benzyloxy)propylidene)formohydrazide (3) as start materials is successfully obtained via a multistep synthesis and finally characterized by IR, 1H NMR, and single crystal X-ray diffraction. In addition, the in vitro anticancer activities of newly synthesized compound 1 are evaluated against three human bone cancer cell lines U2OS, Saos-2, and GC9811. In addition, the molecular docking is used to study the potential antiviral activity of 1 by calculating the binding sites for the 1AS0 protein.
Preparation method of posaconazole
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Paragraph 0028; 0029; 0030; 0031, (2017/08/29)
The invention discloses a preparation method of posaconazole. The preparation method of the posaconazole provided by the invention comprises the following steps: in the presence of inorganic protonic acid, performing hydrolysis reaction on a compound II to obtain posaconazole I. The preparation method provided by the invention is easy and safe to operate, does not need any special equipment, is free from heavy metal residues, produces less reaction side products, and has high yield; a prepared product has high purity (chiral purity is larger than 99.90 percent, related substance purity is larger than 99.50 percent, all impurities are less than 0.1 percent, and raw materials meet the standard), is low in production cost, is environmentally friendly, and is suitable for industrial production. The formula of the posaconazole is shown in the description.
Process for the Preparation of Triazole Antifungal Drug, Its Intermediates and Polymorphs Thereof
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Paragraph 0325, (2014/12/09)
A process for the preparation of 4-[4-[4-[4-[[(3R,5R)-5-(2,4-difluorophenyl)tetrahydro-5-(1H-1,2,4-triazol-1-ylmethyl)-3-furanyl]methoxy]phenyl]-1-piperazinyl]phenyl]-2-[(1S,2S)-1-ethyl-2-hydroxypropyl]-2,4-dihydro-3H-1,2,4-triazol-3-one compound of formula-1, its intermediates and polymorphs thereof. (I)