Category: piperazines

On November 30, 2013, Kavitha, Channappa N.; Jasinski, Jerry P.; Anderson, Brian J.; Yathirajan, H. S.; Kaur, Manpreet published an article.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was 1-[4-(4-Hydroxyphenyl)piperazin-1-yl]ethanone. And the article contained the following:

In the title compound, C12H16N2O2, the piperazine ring has a chair conformation. The dihedral angle between the mean planes of the benzene ring and the acetyl group is 48.7 (1)°. In the crystal, mols. are linked via O-H···O hydrogen bonds, forming chains propagating along [010]. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to hydroxyphenylpiperazinylethanone crystal structure, Crystallography and Liquid Crystals: Polytypism, Polymorphism, Crystal Phase Transitions, Ordering, Amorphization and other aspects.Safety of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On August 1, 2012, Li, Qingeng; Wang, Tao; Xia, Biao; Guo, Bin published a patent.Category: piperazines The title of the patent was Novel 7,10-O,O-dimethyldocetaxel derivative, its preparation process and application for treating cancers. And the patent contained the following:

The invention disclosed a kind of 7,10-O,O-dimethyldocetaxel derivatives and their salts, preparation method and medical application as antitumor agents. The claimed title compounds are shown in structure I (R = H, Me, Et, Pr, iso-Pr, Bu, iso-Bu, or CH2-Ph; HB = inorganic or organic acid from HCl, HBr, HNO3, acetic acid, lactic acid, or tartaric acid etc.). The claimed compounds are prepared with II via esterification etc. multiple steps (procedure given). The obtained compounds and pharmaceutically acceptable salts can be used for preparing water-soluble medicals for treating cancers such as breast cancer, lung cancer and ovarian cancer without side effect, high safety and controlled quality (no data provided). The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).Category: piperazines

The Article related to dimethyldocetaxel derivative salt synthesis esterification antitumor agent, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.Category: piperazines

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On January 22, 1998, Shimizu, Hideaki; Abe, Atsuhiro; Yaegashi, Takashi; Sawada, Seigo; Nagata, Hiroshi published a patent.HPLC of Formula: 53788-12-8 The title of the patent was Preparation of taxane derivatives as antitumors and pharmaceuticals containing them. And the patent contained the following:

The title compounds [I; X, Y = CO-A-B; A = bond, -R-CO-, -R-OCO-, -R-NHCO-; R = alkylene, phenylene; B = (un)substituted heterocyclyl, e.g., piperazin-1-yl; Z = H, trialkylsilyl, trihaloalkoxycarbonyl; Bz = benzoyl], II [R7 = H, alkoxycarbonyl, aralkyloxycarbonyl; R8, R9 = H, alkyl, haloalkyl, etc.] or their salts are prepared Thus, 7-O-triethylsilyl-10-deacetylbaccatin III was reacted with 4-(dimethylamino)piperidinocarbonyl chloride (also prepared) in THF-hexane containing BuLi at -40° to room temperature to give 90% 10-O-(4-dimethylaminopiperidinocarbonyl)-7-O-triethylsilyl-10-deacetylbaccatin III. This was reacted with (4S,5R)-3-(benzyloxycarbonyl)-2,2-dimethyl-4-phenyl-5-oxazolidinecarboxylic acid to give the title compound III. These compounds exhibit a high solubility in water and showed excellent antitumor activity. In an ELISA screening using human oral cancer KB cells, the GI50 for 13-O-[3-(tert-butoxycarbonylamino)-2-hydroxy-3-phenylpropionyl]-10-O-(4-dipropylaminopiperidinocarbonyl)-10-deacetylbaccatin III (also prepared) was 0.78 ng/mL vs. 2.0 ng/mL for taxol. The solubility of 13-O-[3-(tert-butoxycarbonylamino)-2-hydroxy-3-phenylpropionyl]-10-O-(4-dimethylaminopiperidinocarbonyl)-10-O-deacetylbaccatin III (also prepared) in water was 1260 μg/mL vs. 0.4 μg/mL for taxol. The experimental process involved the reaction of 4-Ethyl-piperazine-1-carbonyl chloride(cas: 53788-12-8).HPLC of Formula: 53788-12-8

The Article related to taxane derivative preparation antitumor solubility, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.HPLC of Formula: 53788-12-8

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 14, 1994, Bourzat, Jean Dominique; Commercon, Alain published a patent.Formula: C8H18Cl2N2O2 The title of the patent was Preparation of taxol analogs as antiproliferatives. And the patent contained the following:

Title compounds [I; R1 = (cyclo)alkyl, aryl, heterocyclyl, etc.; R2 = aminohydroxypropionyl group Q; R = Ph, OR6; R3 = aryl; R6 = (cyclo)alk(en)yl, Ph, N-containing heterocyclyl, etc.] were prepared as antiproliferatives (no data). Thus, 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1,13α,10β-trihydroxy-9-oxo-7β-triethylsilyloxy-11-taxene was acylated by 3-morpholinopropionic acid and the product acylated by (4S,5R)-3-tert-butoxycarbonyl-2,2-dimethyl-4-phenyloxazolidine-5-carboxylic acid to give, in 2 addnl. steps, 4-acetoxy-2α-benzoyloxy-5β,20-epoxy-1,7β-dihydroxy-10β-(3-morpholinopropionyloxy)-9-oxo-11-taxen-13α-yl (2R,3S)-3-tert-butyloxy-2-hydroxy-3-phenylpropionate. The experimental process involved the reaction of 3-(4-Methylpiperazin-1-yl)propanoic acid dihydrochloride(cas: 59695-29-3).Formula: C8H18Cl2N2O2

The Article related to taxol analog preparation antiproliferative, Terpenes and Terpenoids: Diterpenes (C20), Including Gibberellins, Retinoids, Quassinoids, and Tocopherols and other aspects.Formula: C8H18Cl2N2O2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On May 31, 2018, Komami, Narumi; Matsuoka, Keitaro; Yoshino, Tatsuhiko; Matsunaga, Shigeki published an article.Related Products of 67914-60-7 The title of the article was Palladium-Catalyzed Germylation of Aryl Bromides and Aryl Triflates Using Hexamethyldigermane. And the article contained the following:

Pd-catalyzed germylation of aryl bromides and aryl triflates using com. available hexamethyldigermane is described. Optimized reaction conditions afforded various functionalized aryltrimethylgermanes, including drug-like mols., in moderate to good yields, demonstrating the versatility of the presented protocols. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Related Products of 67914-60-7

The Article related to palladium catalyst aryl bromide triflate germylation hexamethyldigermane aryltrimethylgermane preparation, Organometallic and Organometalloidal Compounds: Groups Iva, Va, Via – Ge, Sn, Pb, As, Sb, Bi, Se, Te, Po and other aspects.Related Products of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 2005, Liu, Yong; Wang, Jingkang; Yin, Qiuxiang published an article.Electric Literature of 86393-32-0 The title of the article was Determination of the space group for ciprofloxacin hydrochloride monohydrate crystals. And the article contained the following:

Ciprofloxacin hydrochloride monohydrate (CPFX) crystals were obtained exptl. The deaquation, melting, decomposing apex temperatures and water content of ciprofloxacin hydrochloride monohydrate crystals were measured by DSC and TG techniques resp. The data of X-ray powder diffraction (XRPD) of these crystals were collected exptl. The indexing results by the software Cerius2 were obtained. The results showed that the crystal of ciprofloxacin hydrochloride monohydrate belonged to monoclinic, and the unit cell parameters a, b, c and β were 12.93×10-10 m, 19.56×10-10 m, 7.07×10-10 m, and 91.10° resp. Based on the indexing results and the extinction principle, the space group for ciprofloxacin hydrochloride monohydrate crystals produced in crystallization experiment was P21/c. The experimental process involved the reaction of 1-Cyclopropyl-6-fluoro-4-oxo-7-(piperazin-1-yl)-1,4-dihydroquinoline-3-carboxylic acid hydrochloride hydrate(cas: 86393-32-0).Electric Literature of 86393-32-0

The Article related to ciprofloxacin hydrochloride monohydrate x ray powder diffraction space group, unit cell parameter, Crystallography and Liquid Crystals: Crystallographic Methods and Apparatus For Structure Determination and other aspects.Electric Literature of 86393-32-0

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On December 31, 1990, Chapman, David R.; Bauer, Ludwig; Waller, Donald P.; Zaneveld, Lourens J. D. published an article.Recommanded Product: 67914-60-7 The title of the article was Synthesis of diastereomeric ketoconazole analogs. And the article contained the following:

Syntheses of trans-isomers of ketoconazole (I) and the corresponding des-acetyl, 1-Me, 1-formyl and 1-methanesulfonyl analogs were investigated. These isomers, along with the corresponding cis-diastereomers were characterized by their carbon-13 NMR spectra. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Recommanded Product: 67914-60-7

The Article related to ketoconazole diastereomer, imidazolylmethyldioxolanylmethoxyphenylpiperazine, piperazinophenol imidazolylmethyldioxolanylmethanesulfonate reaction, nmr ketoconazole, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Recommanded Product: 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On September 17, 1998, Tanoury, Gerald J.; Senanayake, Chris H.; Hett, Robert; Kuhn, Amy M.; Kessler, Donald W.; Wald, Stephen A. published an article.Electric Literature of 67914-60-7 The title of the article was Pd-catalyzed aminations of aryltriazolones: effective synthesis of hydroxyitraconazole enantiomers. And the article contained the following:

A palladium-catalyzed amination of triazolone I by piperazine II was used as the key step in an efficient synthesis of highly enantiomerically pure hydroxyitraconazole (III). II (>99% ee) was prepared by reaction of an achiral phenol precursor with the corresponding dioxolyl tosylate (>99% ee). The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Electric Literature of 67914-60-7

The Article related to hydroxyitraconazole asym preparation, amination aryltriazolone palladium, triazolone aryl amination palladium, heck coupling vs palladium catalyzed amination, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Electric Literature of 67914-60-7

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On June 30, 2007, He, Qiu Qin; Li, Ke; Cao, Yong Bing; Dong, Huan Wen; Zhao, Li Hua; Liu, Chao Mei; Sheng, Chun Quan published an article.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone The title of the article was Design, synthesis and molecular docking studies of novel triazole antifungal compounds. And the article contained the following:

Based on the active site of Candida albicans lanosterol 14α-demethylase (CACYP51), novel triazole compounds structurally different from the current triazole drugs were designed and synthesized. In vitro antifungal activities showed that compounds I (R = R1 = Me; R = CMe3, CN, NO2, R1 = H) exhibited strong activities. In addition, the first three also displayed certain activities against fluconazole-resistant fungi. The experimental process involved the reaction of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone(cas: 67914-60-7).Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

The Article related to triazolylpropanol benzylpiperazinylphenoxy derivative preparation antifungal activity, mol docking triazolylpropanol derivative lanosterol demethylase, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Quality Control of 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics

On April 30, 2009, Barlaam, Bernard Christophe; Bower, Justin Fairfield; Delouvrie, Benedicte; Fairley, Gary; Harris, Craig Steven; Lambert, Christine; Ouvry, Gilles; Winter, Jon James Gordon published a patent.Related Products of 1211568-27-2 The title of the patent was Pyridine and pyrazine derivatives as Axl and/or c-Met receptor enzyme inhibitors and their preparation, pharmaceutical compositions and use in the treatment of tumors. And the patent contained the following:

The invention concerns pyridine a nd pyrazine derivatives of formula I or a pharmaceutically-acceptable salt thereof, processes for their preparation, pharmaceutical compositions containing them and their use in the manufacture of a medicament for use in the treatment of tumors. Compounds of formula I wherein W is CH and N; J is O and S; each G1, G2, G3 and G4 is CH and N, proved that no more than two of G1,G2, G3 and R4 is N; A is (un)substituted Ph, (un)substituted 5- to 6-membered monocyclic heteroaryl; and (un)substituted 8- to 10-membered bicyclic ring; each R3 is independently H, halo, CN, amino, sulfamoyl, CF3, C1-8 alkyl, etc.; n is 0, 1, 2, and 3; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by cyclization of 2-aminophenol with 2-amino-5-bromopyridine-3-carboxylic acid; the resulting 3-(benzoxazol-2-yl)-5-bromopyridin-2-amine underwent cross-coupling with 4-(dimethylaminomethyl)phenylboronic acid to give compound II. All the invention compounds were evaluated for their Axl and c-Met receptor tyrosine kinase inhibitory activity. From the Axl tyrosine kinase assay, it was determined that compound II exhibited 99.8 % inhibition at 1 μM concentration The experimental process involved the reaction of tert-Butyl 4-(piperidin-4-ylmethyl)piperazine-1-carboxylate(cas: 1211568-27-2).Related Products of 1211568-27-2

The Article related to pyridine preparation axl cmet tyrosine kinase inhibitor treatment tumor, pyrazine preparation axl cmet tyrosine kinase inhibitor treatment tumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Related Products of 1211568-27-2

Referemce:
Piperazine – Wikipedia,
Piperazines – an overview | ScienceDirect Topics