Month: October 2022

The author of 《Novel practical deprotection of N-Boc compounds using fluorinated alcohols》 were Choy, Jason; Jaime-Figueroa, Saul; Jiang, Laurence; Wagner, Paul. And the article was published in Synthetic Communications in 2008. Recommanded Product: 4-(Piperazin-1-yl)-1H-indole The author mentioned the following in the article:

The thermolytic deprotection of N-Boc compounds was accomplished using F3CCH2OH or (F3C)2CHOH as solvents. Even though the cleavage of the tert-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodol. was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. In the experiment, the researchers used many compounds, for example, 4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0Recommanded Product: 4-(Piperazin-1-yl)-1H-indole)

4-(Piperazin-1-yl)-1H-indole(cas: 84807-09-0) belongs to piperazines. Two common salts in the form of which piperazine is usually prepared for pharmaceutical or veterinary purposes are the citrate, 3C4H10N2.2C6H8O7 (i.e. containing 3 molecules of piperazine to 2 molecules of citric acid), and the adipate, C4H10N2.C6H10O4 (containing 1 molecule each of piperazine and adipic acid).Recommanded Product: 4-(Piperazin-1-yl)-1H-indole

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

HPLC of Formula: 109-01-3In 2020 ,《Metal-Free Synthesis of Thermally Stable Fluorescent p-Terphenyls by Ring Transformation of 2H-Pyran-2-ones》 was published in ChemistrySelect. The article was written by Chandrasekar, Subashini; Singh, Fateh V.. The article contains the following contents:

A metal-free approach for the synthesis of p-terphenyls I (Y = piperidin-1-yl, N,N-dimethylamin-1-yl, 4-methylpiperidin-1-yl, etc.) and cyclic p-terphenyls II and III is described via carbanion induced ring transformation reaction of 6-biphenyl-2H-pyran-2-ones IV with malononitrile, cyclohexanone and 1,4-dioxaspiro[4.5]decan-8-one resp. Addnl., the base-mediated ring transformation reactions were working smoothly under mild reaction conditions and ring transformation products I, II and III were isolated in good to excellent yields. The synthetic approach provides the flexibility of introducing of both electron-withdrawing and -donating functionalities in p-terphenyl architecture. Moreover, the photo phys. properties of compounds I, II and III were analyzed using UV-visible and Fluorescence Spectroscopy. The p-Terphenyls I (Y = 4-phenylpiperazin-1-yl) showed cyan fluorescence in chloroform (λmax (em): 508 nm) and acetonitrile (λmax (em): 420 nm) while cyclic p-terphenyl II (Y = 4-phenylpiperazin-1-yl) showed blue fluorescence in chloroform and 1,4-dioxane (λmax (em): 470 nm). Similarly, compound III (Y = 4-phenylpiperazin-1-yl) showed blue fluorescence in chloroform (λmax (em): 468 nm) and 1,4-dioxane (λmax (em): 473 nm). Addnl., the thermal stability of synthesized cyclic p-terphenyls III (Y = 4-methylpiperidin-1-yl, N,N-dipropylamin-1-yl, piperidin-1-yl) were also studied using TG and DTA techniques. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3HPLC of Formula: 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..HPLC of Formula: 109-01-3

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

Quality Control of 4-Methyl-1-piperazinesulfonyl ChlorideOn November 1, 2019 ,《Photoredox-Catalyzed Generation of Sulfamyl Radicals: Sulfonamidation of Enol Silyl Ether with Chlorosulfonamide》 appeared in Journal of Organic Chemistry. The author of the article were Luo, Qiyu; Mao, Runyu; Zhu, Yan; Wang, Yonghui. The article conveys some information:

A novel and practical photoredox-catalyzed generation of sulfamyl radicals followed by radical sulfonamidation of enol silyl ether has been described. Diverse functionalized β-ketosulfonamides ArCOCH2SO2NRR1 (Ar = 4-MeC6H4, 4-BrC6H4, 2-FC6H4, etc.; R = H, Me, Et, etc.; R1 = H, Me, Et, etc.) were prepared in modest to excellent yields under mild and economic reaction conditions through the present catalytic protocol. Furthermore, the methodol. developed provides an efficient and convenient approach to the synthesis of the antiseizure drug Zonisamide. In the experiment, the researchers used 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride)

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.Quality Control of 4-Methyl-1-piperazinesulfonyl Chloride

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

《Microwave-Assisted Cu(I)-Catalyzed Synthesis of Unsymmetrical 1,4-Diamino-2-butynes via Cross-A3-Coupling/Decarboxylative A3-Coupling》 was written by Xu, Xianjun; Feng, Huangdi; Van der Eycken, Erik V.. Safety of 1-MethylpiperazineThis research focused onunsym diamino butyne preparation chemoselective microwave irradiation; amine formaldehyde propiolic acid decarboxylative cross coupling copper. The article conveys some information:

1,4-Diamino-2-butynes display both chem. and physiol. properties. Here a highly efficient synthesis avenue to generate unsym. 1,4-diamino-2-butynes has been developed by microwave-assisted Cu(I)-catalyzed cross-A3-coupling/decarboxylative coupling of two different amines, formaldehyde, and propiolic acid through a domino process. This multicomponent reaction provides a series of target products in moderate to good yields with high chemoselectivity. In the experiment, the researchers used many compounds, for example, 1-Methylpiperazine(cas: 109-01-3Safety of 1-Methylpiperazine)

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..Safety of 1-Methylpiperazine

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

In 2019,Organic Chemistry Frontiers included an article by Zhang, Fei-Yi; Lan, Xiao-Bing; Xu, Chang; Yao, Hua-Gang; Li, Tian; Liu, Feng-Shou. Formula: C5H12N2. The article was titled 《Rigid hindered N-heterocyclic carbene palladium precatalysts: synthesis, characterization and catalytic amination》. The information in the text is summarized as follows:

To explore the high efficiency of the Buchwald-Hartwig amination with a wide substrate scope, easily prepared and air stable palladium precatalysts bearing rigid hindered N-heterocyclic carbenes (NHCs) were synthesized and characterized. A simple and efficient protocol for the amination of (hetero)aryl chlorides with amines is described, which revealed that sterically encumbered NHC ligands are crucial to promote the transformation. It is highlighted that the most challenging reactions could be performed between less reactive five-membered heteroaryl chlorides and heteroanilines. This methodol. provides a rapid and straightforward access to a wide range of arylated amines with excellent functional group tolerance. Remarkably, the powerful synthetic utility of palladium precatalysts was further extended to the synthesis of pharmaceuticals. After reading the article, we found that the author used 1-Methylpiperazine(cas: 109-01-3Formula: 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..Formula: C5H12N2

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

《Optimization of phthalazin-based aryl/heteroarylhydrazones to design new promising antileishmanicidal agents: synthesis and biological evaluation of 3-aryl-6-piperazin-1,2,4-triazolo[3,4-a]phthalazines》 was written by Romero, Angel H.; Rodriguez, Noris; Ramirez, Oscar G.. Computed Properties of C5H12N2 And the article was included in New Journal of Chemistry in 2020. The article conveys some information:

1-Monosubstituted and 1,4-substituted phthalazins based on aryl/heteroarylhydrazinyl have demonstrated attractive antileishmanial profiles against amastigote forms of the Leishmania braziliensis parasite. Further optimization of the mentioned acyclic scaffold motivated us to design a series of 3-aryl-1,2,4-triazolo[3,4-a]phthalazines, cyclic versions of the phthalazins based on aryl/heteroarylhydrazinyl, which have not been evaluated against Leishmania parasites yet. In order to compare to phthalazine-based aryl/heteroarylhydrazones, five essential 3-aryl-6-piperazin-1,2,4-triazolo[3,4-a]phthalazines were efficiently prepared in excellent yields (73-83%) through a facile one-pot procedure from 4-chloro-1-phthalazinyl-arylhydrazones via C-H dehydrogenative cyclization using silver(I) salt. From in vitro antileismanial evaluation, compound 2d, a nitro derivative, was identified as the most promising agent with a good anti-amastigote response (IC50 = 9.37 μM) and low relative toxicity against peritoneal macrophages (LD50 = 123.93 μM). A moderate response was found against clin. amastigote isolates of L. braziliensis, although superior compared to the reference glucantime. A comparison with their phthalazin analogs based on aryl/heteroarylhydrazinyl gave evidence that the efficacy of each chem. system is determined by the nature of the functionalization next to the aryl moiety, which suggests that different mechanisms of action are involved for each chem. system. The cyclized form led to an enhancement of the antileismanial activity compared to the acyclic form, but the nitroderivatives seemed to be highly more toxic than the parent non-cyclized compounds From the three compared phthalazine groups, 4-chloro-1-phthalazine-(5-nitrofuryl)hydrazinil with a nanomolar antileishmanial response was identified as a promising lead for further optimization, whereas compound 2d emerges as a prominent hit platform to prepare a group of derivatives based on phthalazine-1,2,4-triazolo bearing 3-nitro-Ph at the 3-position. The results came from multiple reactions, including the reaction of 1-Methylpiperazine(cas: 109-01-3Computed Properties 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..Computed Properties of C5H12N2

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

Computed Properties of C5H11ClN2O2SOn October 12, 2017 ,《Discovery of Novel Macrocyclic Hedgehog Pathway Inhibitors Acting by Suppressing the Gli-Mediated Transcription》 was published in Journal of Medicinal Chemistry. The article was written by Liu, Gang; Huang, Wenjing; Wang, Juan; Liu, Xiaohua; Yang, Jun; Zhang, Yu; Geng, Yong; Tan, Wenfu; Zhang, Ao. The article contains the following contents:

A systemic medicinal chem. campaign was conducted based on a literature hit compound I bearing the 4,5-dihydro-2H-benzo[b][1,5]oxazocin-6(3H)-one core through cyclization of two side substituents of the bicyclic skeleton combined with N-atom walking or ring walking and the central ring expansion or extraction approaches, leading to several series of structurally unique tricyclic compounds Among these, compound II was identified as the most potent against the Hedgehog (Hh) signaling pathway showing an IC50 value of 23 nM. Mechanism studies indicated that compound II inhibited the Hh signaling pathway by suppressing the expression of the transcriptional factors Gli rather than by interrupting the binding of Gli with DNA. We further observed that II was equally potent against both Smo wild type and the two major resistant mutants (Smo D473H and Smo W535L). It potently inhibited the proliferation of medulloblastoma cells and showed significant tumor growth inhibition in the ptch± ;p53-/- medulloblastoma allograft mice model. Though more studies are needed to clarify the precise interaction pattern of II with Gli, its promising in vitro and in vivo properties encourage further profiling as a new-generation Hh signaling inhibitor to treat tumors primarily or secondarily resistant to current Smo inhibitors. In the experimental materials used by the author, we found 4-Methyl-1-piperazinesulfonyl Chloride(cas: 1688-95-5Computed Properties of C5H11ClN2O2S)

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.Computed Properties of C5H11ClN2O2S

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