Tag: 100-200

《A Cu (I) catalyzed large scale synthesis of an antipsychotic drug substance Clozapine with new precursor 2-chloro benzoic acid》 was published in Arabian Journal of Chemistry in 2020. These research results belong to Venkat Rao, S.. Category: piperazines The article mentions the following:

Development of an economic and com. manufacturing process for an anti-psychotic drug substance clozapine I with an alternative key starting material (2-chloro benzoic acid) in the place of literature reported key starting material Anthranilic acid. To avoid narcotic key starting materials usage in drug substances the author invented a com. available raw material 2-chlorobenzoic acid, which reacts with another key starting material 4-chloro-1,2-diamino benzene. This reaction proceeded through Ullman reaction to produce multi scale level Clozapine which quality meets the ICH requirements.1-Methylpiperazine(cas: 109-01-3Category: piperazines) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Category: piperazines

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

The author of 《Volume changes in the proton ionization of amines in water. 1. Morpholines and piperazines》 were Cabani, S.; Mollica, V.; Lepori, L.; Lobo, S. T.. And the article was published in Journal of Physical Chemistry in 1977. Electric Literature of C5H14Cl2N2 The author mentioned the following in the article:

Apparent molar volumes, Φv, at various concentrations in water at 25° of some cyclic bifunctional amines [morpholine, 4-methylmorpholine, piperazine, 1-methyl- and 1,4-dimethylpiperazine, 1,4-diazabicyclo[2.2.2]octane (triethylenediamine)] and their mono- and dihydrochlorides were determined The volume changes ΔV1° and ΔV2°, involved in the 1st and 2nd proton ionizations from the protonated amines, were calculated from the limiting partial molar volumes V̅2°. The volumes of ionization for the bifunctional cyclic amines were compared with those for the monofunctional amines ad the relationship between entropies and volumes of ionization was examined In the experiment, the researchers used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Electric Literature of C5H14Cl2N2)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Electric Literature of C5H14Cl2N2

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

《One-pot multicomponent synthesis of novel 3, 4-dihydro-3-methyl-2(1H)-quinazolinone derivatives and their biological evaluation as potential antioxidants, enzyme inhibitors, antimicrobials, cytotoxic and anti-inflammatory agents》 was written by Farooq, Samra; Mazhar, Aqsa; Ihsan-Ul-Haq; Ullah, Naseem. Electric Literature of C5H12N2 And the article was included in Arabian Journal of Chemistry in 2020. The article conveys some information:

A series of 3,4-dihydro-3-methyl-2(1H)-quinazolinones I [R = pyrrolidin-1-yl, 1-piperidyl, morpholino, etc.] with amines and formaldehyde were designed and synthesized by a reflux condensation reaction in the presence of an acid catalyst resulted in N-Mannich bases. Mannich bases I were evaluated pharmacol. for their antioxidant, α-amylase enzyme inhibition, antimicrobial, cell cytotoxicity and anti-inflammatory activities. Most of the compounds I exhibited potent activities against these bioassays. Among them, compounds I [R = 1-piperidyl, N-acetyl-4-hydroxyanilino] showed potent antioxidant activity against DPPH free radical at IC50 of 9.94 ± 0.16μg/mL and 11.68 ± 0.32μg/mL, resp. Compounds I [R = N-phenylanilino, N-acetylanilino, N-acetyl-4-hydroxyanilino] showed significant resulted in TAC and TRP antioxidant assays, comparable to that of ascorbic acid. Compounds I [R = morpholino, pyrrolidin-1-yl] showed potent activity in inhibiting α-amylase enzyme at IC50 of 10.17 ± 0.23μg/mL and 9.48 ± 0.17μg/mL, resp., when compared with acarbose (13.52 ± 0.19μg/mL). Compound I [R = N-phenylanilino] was the most active against Gram-pos. and Gram-neg. bacterial strains, compound I [R = N-acetyl-4-hydroxyanilino] was the most potent against P. aeruginosa inhibited its growth up to 80% (MIC = 11.11μg/mL). Compounds I [R = dipropylamino, 4-methylpiperazin-1-yl, piperazin-1-yl] exhibited significant activity against some fungal strains. Among the thirteen N-Mannich bases I, four were screened out based on the results of brine shrimp lethality assay (LD50) and cell cytotoxicity assay (IC50),determine their anti-cancer potential against Hep-G2 cells. The study was conducted for 24, 48, and 72 h. Compound I [R = diethylamino] showed potent results at IC50 of 6.48μM at 72 h when compared with cisplatin (2.56μM). An in-vitro nitric oxide (NO) assay was performed to shortlist compounds for in-vivo anti-inflammatory assay. Among shortlisted compounds, I [R = N-acetyl-4-hydroxyanilino] exhibited potent anti-inflammatory activity by decreasing the paw thickness to the maximum compared to the standard, acetylsalicylic acid (ASA). The experimental process involved the reaction of 1-Methylpiperazine(cas: 109-01-3Electric Literature of C5H12N2)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Electric Literature of C5H12N2

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

The author of 《Synthesis of dithioacetylenic piperazine derivatives》 were Mukanova, M. S.; Sycheva, Ye. S.; Seilkhanov, T. M.; Yu, V. K.. And the article was published in Khimicheskii Zhurnal Kazakhstana in 2019. COA of Formula: C5H12N2 The author mentioned the following in the article:

The conditions for the three-component one-pot synthesis of dithioacetylenic piperazine derivatives was developed. As a result prop-2-yn-1-yl-4-methylpiperazine-1-carbodithioate (73.4%) and prop-2-yn-1-yl-4-diphenylmethylpiperazine-1-carbodithioate (93.6%) were synthesized. Structure of dithioacetylenic piperazine derivatives were established based on IR and NMR(1H and 13C) spectroscopic data. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3COA of Formula: C5H12N2) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..COA of Formula: C5H12N2

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

Muraglia, Ester; Kinzel, Olaf; Gardelli, Cristina; Crescenzi, Benedetta; Donghi, Monica; Ferrara, Marco; Nizi, Emanuela; Orvieto, Federica; Pescatore, Giovanna; Laufer, Ralph; Gonzalez-Paz, Odalys; Di Marco, Annalise; Fiore, Fabrizio; Monteagudo, Edith; Fonsi, Massimiliano; Felock, Peter J.; Rowley, Michael; Summa, Vincenzo published an article on February 28 ,2008. The article was titled 《Design and Synthesis of Bicyclic Pyrimidinones as Potent and Orally Bioavailable HIV-1 Integrase Inhibitors》, and you may find the article in Journal of Medicinal Chemistry.SDS of cas: 1688-95-5 The information in the text is summarized as follows:

HIV integrase is one of the three enzymes encoded by HIV genome and is essential for viral replication, but integrase inhibitors as marketed drugs have just very recently started to emerge. In this study, the evolution from the N-methylpyrimidinone structure to bicyclic pyrimidinones, e.g., I and II, is shown. Introduction of a suitably substituted amino moiety modulated the phys.-chem. properties of the mols. and conferred nanomolar activity in the inhibition of spread of HIV-1 infection in cell culture. An extensive SAR study led to sulfamide I, which inhibited the strand transfer with an IC50 of 7 nM and HIV infection in MT4 cells with a CIC95 of 44 nM, and ketoamide II that inhibited strand transfer with an IC50 of 12 nM and the HIV infection in MT4 cells with a CIC95 of 13 nM and exhibited a good pharmacokinetic profile when dosed orally to preclin. species. The experimental process involved the reaction of 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5SDS of cas: 1688-95-5)

4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5) is a member of sulfamide. Sulfamide was used in the synthesis of: Schiff bases of the type ArCH=NSO2NH2; 1H,3H-2,1,3-benzothiadiazin-4-one-2,2-dioxide (BTDD); sulfamide analogs of oleoylethanolamide analogs in a study of PPARα activation.SDS of cas: 1688-95-5

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

《Thiazolothiazepine Inhibitors of HIV-1 Integrase》 was written by Neamati, Nouri; Turpin, Jim A.; Winslow, Heather E.; Christensen, John L.; Williamson, Karen; Orr, Ann; Rice, William G.; Pommier, Yves; Garofalo, Antonio; Brizzi, Antonella; Campiani, Giuseppe; Fiorini, Isabella; Nacci, Vito. Recommanded Product: 1-Methylpiperazine dihydrochloride And the article was included in Journal of Medicinal Chemistry on August 26 ,1999. The article conveys some information:

A series of thiazolothiazepines were prepared and tested against purified human immunodeficiency virus type-1 integrase (HIV-1 IN) and viral replication. Structure-activity studies reveal that the compounds possessing the pentat. moiety SC(O)CNC(O) with two carbonyl groups are in general more potent against purified IN than those containing only one carbonyl group. Substitution with electron-donating or -withdrawing groups did not enhance nor abolish potency against purified IN. By contrast, compounds with a naphthalene ring system showed enhanced potency, suggesting that a hydrophobic pocket in the IN active site might accommodate an aromatic system rather than a halogen. The position of sulfur in the thiazole ring appears important for potency against IN, as its replacement with an oxygen or carbon abolished activity. Further extension of the thiazole ring diminished potency. I [R, R1 = H, X = S, Y = CH2; RR1 = CH:CHCH:CH; X = S, Y = CH2; X = CH2, Y = S] showed antiviral activity and inhibited IN within similar concentrations These compounds inhibited IN when Mn2+ or Mg2+ was used as cofactor. None of these compounds showed detectable activities against HIV-1 reverse transcriptase, protease, virus attachment, or nucleocapsid protein zinc fingers. Therefore, thiazolothiazepines are potentially important lead compounds for development as inhibitors of IN and HIV replication. In the part of experimental materials, we found many familiar compounds, such as 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Recommanded Product: 1-Methylpiperazine dihydrochloride)

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Recommanded Product: 1-Methylpiperazine dihydrochloride

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

Recommanded Product: 109-01-3In 2020 ,《Efficient Synthesis of Sulfenamides through Mitsunobu-type Coupling Reaction of Thiols with Amines using Dibenzyl Azodicarboxylate》 was published in Asian Journal of Organic Chemistry. The article was written by Ryu, Se Hwan; Ra, Jongmin; Ko, Haye Min. The article contains the following contents:

S-H activation reaction of thiols employing dibenzyl azodicarboxylate (DBAD) had been developed for the preparation of sulfenamides I [R = H; R1 = Et, Bn, cyclopropyl, cyclopentyl, cyclohexyl; RR1 = (CH2)4, (CH2)6, (CH2)2O(CH2)2, etc.; X = O, S]. The dehydrogenation of thiols and amines under these reaction conditions involved the formation of dibenzyl hydrazine-1,2-dicarboxylate, which led to the S-N bond formation reaction. The reaction proceeded efficiently with release of dibenzyl hydrazine-1,2-dicarboxylate and afforded various sulfenamides I in good to excellent yields. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Recommanded Product: 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Recommanded Product: 109-01-3

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

In 2022,Yamaguchi, Nobuharu; Biniecki, Kristof; Jankowski, Christopher K.; Ciszewski, Lech published an article in Acta Poloniae Pharmaceutica. The title of the article was 《Cardiovascular evaluation of the chemical structure of N-methylpiperazinyl phthalazine analogs》.Product Details of 109-01-3 The author mentioned the following in the article:

The chem. structure of N-methylpiperazinyl phthalazine analogs – KB compounds, having potential cardiovascular effects, were synthesized and its detailed spectral identification is reported. For KB-1, moiety structure, five physiol. cardiovascular tests were performed and the results were discussed. This mol. showed long-lasting antihypertensive properties with similarly long-lasting bradycardia. However, a slight modification of the mol. structure might minimize the cardiac depressant phenomenon, which is a common undesired effect of various antihypertensive drugs on the market. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Product Details of 109-01-3)

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Product Details of 109-01-3

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

In 2022,Venkatesh, Rapelly; Shankar, Gauri; Narayanan, Aswathi C.; Modi, Gyan; Sabiah, Shahulhameed; Kandasamy, Jeyakumar published an article in Journal of Organic Chemistry. The title of the article was 《Multicomponent Synthesis of S-Benzyl Dithiocarbamates from para-Quinone Methides and Their Biological Evaluation for the Treatment of Alzheimer’s Disease》.Product Details of 109-01-3 The author mentioned the following in the article:

Multicomponent synthesis of biol. relevant S-benzyl dithiocarbamates I [Ar = Ph, 2-thienyl, 2-naphthyl, etc.; R = methylamino, 1-pyrrolidinyl, benzylamino, etc.] from para-quinone methides, amines and carbon disulfide were described under catalyst and additive-free conditions. The reactions proceeded at room temperature in a short span of time with excellent yields. One of the synthesized compounds, compound I [Ar = Ph, R = isopropylamino] showed considerable acetylcholinesterase (AChE) inhibitory (51.70 + 5.63% at 20μm) and antioxidant (63.52 ± 1.15 at 20μm) activities. In addition to this study using 1-Methylpiperazine, there are many other studies that have used 1-Methylpiperazine(cas: 109-01-3Product Details of 109-01-3) was used in this study.

1-Methylpiperazine(cas: 109-01-3) can be used as mimic template in the preparation of molecularly imprinted microspheres (MIMs). It was also used to prepare the difunctional strong anion-exchange stationary phase from a 1,4-diazacyclohexane derivative..Product Details of 109-01-3

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

Obniska, Jolanta; Kulig, Katarzyna; Zejc, Alfred published an article in Acta Poloniae Pharmaceutica. The title of the article was 《Synthesis and anticonvulsant properties of new N-piperazinylalkyl imides of succinic acid》.Name: 1-Methylpiperazine dihydrochloride The author mentioned the following in the article:

A number of N-[((4-aryl)- or (4-methyl)-1-piperazinyl)alkyl]imides of 3-aryl- or 3,3-pentamethylenesuccinic acid, I [R1 = 3-ClC6H4, 4-ClC6H4, R2 = H, R1R2 = (CH2)5, R3 = Ph, CH2Ph, Me.2HCl, 2-MeOC6H4, 3-ClC6H4, n = 1; R1 = Ph, R2 = Ph, Me, R1R2 = (CH2)5, R3 = H.2HCl, Me.2HBr, Me.2HCl, n = 2, 3; R1 = Ph, R2 = Me, R3 = Ph, n = 3], were synthesized and tested for anticonvulsant activity in the maximum electroshock seizure (MES) and pentylenetetrazole seizure threshold (scMet) tests. Structures of the novel compounds were confirmed by elemental and spectral analyses. In addition to this study using 1-Methylpiperazine dihydrochloride, there are many other studies that have used 1-Methylpiperazine dihydrochloride(cas: 34352-59-5Name: 1-Methylpiperazine dihydrochloride) was used in this study.

1-Methylpiperazine dihydrochloride(cas: 34352-59-5) is used in the preparation of 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), 1-methylpiperazine-1,4-diium tetrachloridozincate hemihydrate, 2-(4-Methyl-1-piperazinylmethyl)acrylophenone(MPMAP), an antimicrotubular drug..Name: 1-Methylpiperazine dihydrochloride

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