Tag: M.W=200-250

Liang, Shuang published the artcileSynthesis and antifungal activity of 1-(1H-1,2,4-triazol-1-yl)-2-(2,4-difluorophenyl)-3-[(4-substituted)-1-piperazinyl]-2-propanols, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2004), 14(2), 71-75, database is CAplus.

The effect of the side chain in (4-substituted)-1-piperazinyl on the antifungal activity of fluconazole compounds was studied. Thirteen title compounds were synthesized and confirmed by the elementary anal., ¹H-NMR and IR spectra. The MICs of all the title compounds were determined by the method recommended by the National Committee for Clin. Laboratory Standards (NCCLS) using the RPMI1640 test medium. The results of the preliminary antifungal test showed that all the title compounds exhibited potent antifungal activities. The activities of the eight compounds thus prepared were more than 4 times as high as that of fluconazole and equal to that of ketoconazole against Candida albicans in vitro. The lipid/water distribution coefficient and stereochem. have important influence on the antifungal activities of the title compounds

Zhongguo Yaowu Huaxue Zazhi published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Zhao, Lihua published the artcileDesign, synthesis and antitumor activity of thalidomide derivatives, Category: piperazines, the publication is Zhongguo Yaowu Huaxue Zazhi (2008), 18(1), 16-22, database is CAplus.

The antitumor activity of thalidomide derivatives [i.e., 2-(2,6-dioxo-3-piperidinyl)-1H-isoindole-1,3(2H)-dione derivatives] was studied. A method for the synthesis of the title compounds is reported here. According to the structure of thalidomide, starting from ¦Â-D-glucosamine hydrochloride, twenty compounds were designed and synthesized. Product structures were determined by NMR, IR, MS. The target compounds were evaluated for their anticancer activity. The survival of 4T1 cells was determined Compounds substituted by a 3,4,6-tri-O-acetyl glucopyranoside have better antitumor activity than thalidomide dose.

Zhongguo Yaowu Huaxue Zazhi published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C2H4ClNO, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Huang, Jian-Dong published the artcileTetra-(acetyl piperazine phenoxy) phthalocyaninato zinc complexes and their proteins conjugates: synthesis, characterisation and photodynamic activities, Computed Properties of 67914-60-7, the publication is Wuji Huaxue Xuebao (2006), 22(3), 435-442, database is CAplus.

Two zinc phthalocyanines, tetra-¦Á-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn) and tetra-¦Â-[4-(4-acetyl piperazine) phenoxy] phthalocyaninato zinc (C₈₀H₇₂N₁₆O₈Zn), have been synthesized and characterized with ¹H NMR, MS, IR and elemental anal. The electronic absorption spectra of two complexes in common organic solvents (N,N-DMF, THF, n-octanol) were typical for nonaggregated phthalocyanines, showing a Q band at 693?698 nm for 1 and 681 ? 682 nm for 2. This indicates that the Q band of zinc phthalocyanine with the substituted groups located in the ¦Á position is largely red shifted than that in the ¦Â position. The spectral features of complexes 1 and 2 in aqueous media suggest the ¦Á-substituted groups are more effective than ¦Â-substituted groups to hinder the aggregation of phthalocyanine mol. The interactions between two complexes with serum albumin and transferrin (BSA, HSA and apoTf) were investigated by absorption and fluorescence spectroscopy. The binding constants were found to be (1 ? 20) ¡Á 10⁵ mol^-1¡¤L. By comparison, ¦Â-substituted 2 had stronger combining ability with albumin than that of ¦Á-substituted 1. The non-covalent conjugates (1-BSA, 2-BSA, 1-HSA, 1-apoTf and 1-FeTf) with the molar ratio of about 1 : 1 have also been prepared The photodynamic activities of two complexes and their bioconjugates against MCF-7 mammary tumor cells were examined The result shows that the photocytotoxicities of conjugates are higher than that of complexes 1 ? 2 and follows the order 1-BSA > 1-FeTf > 1-HSA, 1-apoTf > 2-BSA > 1>2.

Wuji Huaxue Xuebao published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Computed Properties of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Yang, Jiqiu published the artcileSynthesis of an antifungal drug ketoconazole, Application In Synthesis of 67914-60-7, the publication is Yiyao Gongye (1984), 1-4, database is CAplus.

The title compound [I, R = p-(4-acetylpiperazin-1-yl)phenyl] was prepared by condensation of I (R = MeSO₂) with piperazine II which was prepared starting from piperazine.

Yiyao Gongye published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C24H12, Application In Synthesis of 67914-60-7.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Cheng, Xian-Chao published the artcileDesign, synthesis, and biological activities of novel Ligustrazine derivatives, Related Products of piperazines, the publication is Bioorganic & Medicinal Chemistry (2007), 15(10), 3315-3320, database is CAplus and MEDLINE.

A series of novel Ligustrazine derivatives was designed, synthesized, and assayed for their protective effects on damaged ECV-304 cells and antiplatelet aggregation activities. The results showed that most Ligustrazine derivatives exhibited lower EC₅₀ values for protective effects on the ECV-304 cells damaged by hydrogen peroxide in comparison with Ligustrazine. And some Ligustrazine derivatives presented better antiplatelet aggregation activities than Ligustrazine. The derivatives containing the bisphenylmethyl pharmacophore (7a-c) exhibited highest potency. Compound 7a displayed most potential protective effects on the ECV-304 cells damaged by hydrogen peroxide, and compound 7c was found to be the most active antiplatelet aggregation agent. Structure-activity relationships were briefly discussed.

Bioorganic & Medicinal Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Related Products of piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Chen, Yonghao published the artcileSynthesis of ketoconazole by phase-transfer catalysis, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, the publication is Zhongguo Yiyao Gongye Zazhi (2008), 39(8), 564-566, database is CAplus.

Antifungal drug ketoconazole was synthesized by utilization of phase-transfer catalysis from [2-bromomethyl-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl]methanol via acylation, N-alkylation with imidazole and hydrolysis, formation the active ester with methanesulfonyl chloride, and then condensation with the side chain 1-acetyl-4-(4-hydroxyphenyl)piperazine. The overall yield was about 30%.

Zhongguo Yiyao Gongye Zazhi published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Recommanded Product: 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Heinz, Christoph published the artcileNi-Catalyzed Carbon-Carbon Bond-Forming Reductive Amination, Formula: C13H18N2, the publication is Journal of the American Chemical Society (2018), 140(6), 2292-2300, database is CAplus and MEDLINE.

This report describes a three-component, Ni-catalyzed reductive coupling that enables the convergent synthesis of tertiary benzhydryl amines (e.g. I), which are challenging to access by traditional reductive amination methodologies. The reaction makes use of iminium ions generated in situ from the condensation of secondary N-trimethylsilyl amines with benzaldehydes, and these species undergo reaction with several distinct classes of organic electrophiles. The synthetic value of this process is demonstrated by a single-step synthesis of antimigraine drug flunarizine (Sibelium) and high yielding derivatization of paroxetine (Paxil) and metoprolol (Lopressor). Mechanistic investigations support a sequential oxidative addition mechanism rather than a pathway proceeding via ¦Á-amino radical formation. Accordingly, application of catalytic conditions to an intramol. reductive coupling is demonstrated for the synthesis of endo- and exocyclic benzhydryl amines.

Journal of the American Chemical Society published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Formula: C13H18N2.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Schiaffella, Fausto published the artcileNovel ketoconazole analogues based on the replacement of 2,4-dichlorophenyl group with 1,4-benzothiazine moiety: Design, synthesis, and microbiological evaluation, Category: piperazines, the publication is Bioorganic & Medicinal Chemistry (2006), 14(15), 5196-5203, database is CAplus and MEDLINE.

As a part of a program to develop novel antifungal agents, new compounds which incorporate the 1,4-benzothiazine moiety into the structure of ketoconazole (KTZ) were prepared These compounds were computationally investigated to assess whether the 1,4-benzothiazine moiety was a suitable bioisosteric replacement for the 2,4-dichlorophenyl group of KTZ in order to obtain a more potent inhibition of CYP51 enzyme of Candida albicans. Results of preliminary microbiol. studies show that the racemic cis-7 analog has a good in vivo activity, comparable to that of KTZ, but the best activity was observed in the racemic trans-7 analog.

Bioorganic & Medicinal Chemistry published new progress about 67914-60-7. 67914-60-7 belongs to piperazines, auxiliary class Piperazine,Benzene,Phenol,Amide, name is 1-(4-(4-Hydroxyphenyl)piperazin-1-yl)ethanone, and the molecular formula is C12H16N2O2, Category: piperazines.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Zhang, Yun published the artcileDicationic Electrophiles from Olefinic Amines in Superacid, Synthetic Route of 87179-40-6, the publication is Journal of Organic Chemistry (2003), 68(13), 5119-5122, database is CAplus and MEDLINE.

Olefins containing amine moieties undergo Friedel-Crafts alkylations with benzene and substituted benzenes in the presence of triflic acid to yield arenes in 49-99% yields. Suspension of the amine-containing olefins in triflic acid and an arene yields the product arenes. This method is used in brief syntheses of the anti-spasmodic agents fenpiprane and prozapine from 1-(trans-cinnamyl)piperidine and 1-(trans-cinnamyl)hexahydroazepine, resp. Alkenes can be immobilized on polystyrene beads with triflic acid to yield resin-bound amines and piperazines; beads crosslinked with 2% divinylbenzene are stable to the reaction conditions while macroporous beads are damaged under the reaction conditions. The alkylation reactions are proposed to occur via dicationic carbocation intermediates containing protonated amine salts; the ¹³C NMR spectra of a dication generated in situ from (4,4-diphenyl-3-butenyl)piperidine under superacidic conditions is obtained as evidence for the proposed intermediates.

Journal of Organic Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C19H14O2, Synthetic Route of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics

Liu, Hangyu published the artcileSynthesis of formamides containing unsaturated groups by N-formylation of amines using CO₂ with H₂, Quality Control of 87179-40-6, the publication is Green Chemistry (2017), 19(1), 196-201, database is CAplus.

The selective and efficient N-formylation of amines containing unsaturated groups using CO₂ and H₂ with a Cu(OAc)₂-4-dimethylaminopyridine (DMAP) catalytic system was described. The substrates were converted to the desired formamides, while the unsaturated groups, such as the carbonyl group, the C=C bond, CN bond and the ester group remained. The main reason for the excellent selectivity of the Cu(OAc)₂-DMAP catalytic system was that it was very active for the N-formylation reaction, but was not active for the hydrogenation of the unsaturated groups.

Green Chemistry published new progress about 87179-40-6. 87179-40-6 belongs to piperazines, auxiliary class Benzenes, name is (E)-1-Cinnamylpiperazine, and the molecular formula is C13H18N2, Quality Control of 87179-40-6.

Referemce:
https://en.wikipedia.org/wiki/Piperazine,
Piperazines – an overview | ScienceDirect Topics