Month: October 2022

In 2018,Sturgess, Dayna; Chen, Zongjia; White, Jonathan M.; Rizzacasa, Mark A. published 《Enantiospecific total synthesis of the squalene synthase inhibitors (-)-CJ-13,982 and its enantiomer from a common intermediate》.Journal of Antibiotics published the findings.Recommanded Product: tert-Butyl N,N’-diisopropylcarbamimidate The information in the text is summarized as follows:

The total syntheses of both the natural and unnatural enantiomers of the alkyl citrate natural product CJ-13,982 from the common D-ribose-derived acid 6 are described. In addition to this study using tert-Butyl N,N’-diisopropylcarbamimidate, there are many other studies that have used tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Recommanded Product: tert-Butyl N,N’-diisopropylcarbamimidate) was used in this study.

tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8) belongs to anime. To avoid the problem of multiple alkylation, methods have been devised for “blocking” substitution so that only one alkyl group is introduced. The Gabriel synthesis is one such method; it utilizes phthalimide, C6H4(CO)2NH, whose one acidic hydrogen atom has been removed upon the addition of a base such as KOH to form a salt.Recommanded Product: tert-Butyl N,N’-diisopropylcarbamimidate

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2019,Dalton Transactions included an article by Pradhan, Rabindra N.; Chakraborty, Subhayan; Bharti, Pratibha; Kumar, Janesh; Ghosh, Arindam; Singh, Akhilesh K.. SDS of cas: 683-57-8. The article was titled 《Seven coordinate Co(II) and six coordinate Ni(II) complexes of an aromatic macrocyclic triamide ligand as paraCEST agents for MRI》. The information in the text is summarized as follows:

We are reporting Co(II) and Ni(II) complexes of a pyridine containing aromatic macrocyclic triamide ligand, 3,6,9,15-tetraazabicyclo(9.3.1)pentadeca-1(15),11,13-triene-3,6,9-triacetamide (TPTA), as paramagnetic chem. exchange saturation transfer (paraCEST) MRI contrast agents. The synthesis and characterization of TPTA and its complexes are reported. The solution chem. and solid-state structure of Co(II) and Ni(II) complexes are studied. Crystallog. data show that the [Co(TPTA)]·Cl2·2H2O complex (seven-coordinate, all four N atoms of ring and three amide O atoms) has a distorted pentagonal bipyramidal geometry, however the [Ni(TPTA)Cl]·Cl·0.25H2O complex (six-coordinate, all four N atoms of the ring, one amide O and one chloride ion) adopts a distorted octahedral geometry. Notably the two pendent amide arms are not coordinated in the [Ni(TPTA)Cl]+ complex and one chloride ion fulfils its sixth coordination. The CEST effect of [Co(TPTA)]2+ and [Ni(TPTA)Cl]+ amide protons is observed at 57 ppm and 78 ppm downfield of the bulk water proton resp. in a buffer solution containing 20 mM N-(2-hydroxyethyl)piperazine-N’-ethanesulfonic acid and 100 mM NaCl at pH 7.4 at 37 °C on a 9.4 T NMR spectrometer. The effects of CEST intensity and exchange rate constant with variation of pH of the solution were studied. The CEST effect and exchange rate constant for the amide protons of the [Co(TPTA)]2+ complex have been monitored in HEPES buffer, fetal bovine serum (FBS), rabbit serum and 4% agarose gel (weight/weight). The stability of the [Co(TPTA)]2+ complex in aqueous solution towards oxidation was verified by cyclic voltammetry measurement. The stability of [Co(TPTA)]2+ has further been monitored in the presence of biol. relevant ions including HPO42-, CO32-, and Zn2+ and under acidic conditions. The experimental process involved the reaction of 2-Bromoacetamide(cas: 683-57-8SDS of cas: 683-57-8)

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Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2019,Inorganic Chemistry included an article by Bond, Christopher J.; Sokolow, Gregory E.; Crawley, Matthew R.; Burns, Patrick J.; Cox, Jordan M.; Mayilmurugan, Ramasamy; Morrow, Janet R.. Safety of 2-Bromoacetamide. The article was titled 《Exploring Inner-Sphere Water Interactions of Fe(II) and Co(II) Complexes of 12-Membered Macrocycles To Develop CEST MRI Probes》. The information in the text is summarized as follows:

Several paramagnetic Co(II) and Fe(II) macrocyclic complexes were prepared with the goal of introducing a bound H2O ligand to produce paramagnetically shifted H2O 1H resonances and for paramagnetic chem. exchange saturation transfer (paraCEST) applications. Three 12-membered macrocycles with amide pendent groups including 1,7-bis(carbamoylmethyl)-1,4,7,10-tetraazacyclodocane (DCMC), 4,7,10-tris(carbamoylmethyl)-,4,7,10-triaza-12-crown-ether (N3OA), and 4,10-bis(carbamoylmethyl)-4,10-diaza-12-crown-ether (NODA) were prepared and their Co(II) complexes were characterized in the solid state and in solution The crystal structure of [Co(DCMC)]Br2 featured a six-coordinated Co(II) center with distorted octahedral geometry, while [Co(NODA)(OH2)]Cl2 and [Co(N3OA)](NO3)2 were seven-coordinated. The analogous Fe(II) complexes of NODA and NO3A were successfully prepared, but the complex of DCMC oxidized rapidly to the Fe(III) form. Similarly, [Fe(NODA)]2+ oxidized over several days, forming crystals of the Fe(III) complex isolated as the μ-O bridged dimer. Magnetic susceptibility values and paramagnetic NMR spectra of the Fe(II) complexes of NODA and N3OA, as well as Co(II) complexes of DCMC, NODA, and N3OA, were consistent with high spin complexes. CEST peaks ranging from 60 ppm to 70 ppm, attributed to NH groups of the amide pendents, were identified. Variable-temperature 17O NMR spectra of Co(II) and Fe(II) NODA complexes were consistent with rapid exchange of the H2O ligand with bulk H2O. Notably, the Co(II) and Fe(II) complexes presented here produced substantial paramagnetic shifts of bulk H2O 1H resonances, independent of having an inner-sphere H2O. In addition to this study using 2-Bromoacetamide, there are many other studies that have used 2-Bromoacetamide(cas: 683-57-8Safety of 2-Bromoacetamide) was used in this study.

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Safety of 2-Bromoacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Discovery and Optimization of Small Molecules Targeting the Protein-Protein Interaction of Heat Shock Protein 90 (Hsp90) and Cell Division Cycle 37 as Orally Active Inhibitors for the Treatment of Colorectal Cancer》 was published in Journal of Medicinal Chemistry in 2020. These research results belong to Wang, Lei; Jiang, Jingsheng; Zhang, Lixiao; Zhang, Qiuyue; Zhou, Jianrui; Li, Li; Xu, Xiaoli; You, Qidong. Reference of 2-Bromoacetamide The article mentions the following:

Cell division cycle 37 (Cdc37) is known to work as a kinase-specific cochaperone, which selectively regulates the maturation of kinases through protein-protein interaction (PPI) with Hsp90. Directly disrupting the Hsp90-Cdc37 PPI is emerging as an alternative strategy to develop anticancer agents through a specific inhibition manner of kinase clients of Hsp90. Based on a first specific small-mol. inhibitor targeting Hsp90-Cdc37 PPI (DDO-5936), which was previously reported by our group, we conducted a preliminary investigation of the structure-activity relationships and pharmacodynamic evaluations to improve the potency and drug-like properties. Here, our efforts resulted in the currently best inhibitor 18h with improved binding affinity (Kd = 0.5μM) and cellular inhibitory activity (IC50 = 1.73μM). Both in vitro and in vivo assays revealed that 18h could efficiently block the Hsp90-Cdc37 interaction to specifically inhibit kinase clients of Hsp90. Furthermore, 18h showed ideal physiochem. properties with favorable stability, leading to an oral efficacy in vivo. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Reference of 2-Bromoacetamide)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Reference of 2-Bromoacetamide

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Garcia-Vazquez, Victor; Hoteite, Larry; Lakeland, Christopher P.; Watson, David W.; Harrity, Joseph P. A. published an article in 2021. The article was titled 《A Pd-Catalyzed [4 + 2] Annulation Approach to Fluorinated N-Heterocycles》, and you may find the article in Organic Letters.Recommanded Product: 78191-00-1 The information in the text is summarized as follows:

3-Fluoro- and trifluoromethylthio-piperidines represent important building blocks for discovery chem. We report a simple and efficient method to access analogs of these compounds that are armed with rich functionality allowing them to be chemoselectively derivatized with high diastereocontrol.N-Methoxy-N-methylacetamide(cas: 78191-00-1Recommanded Product: 78191-00-1) was used in this study.

N-Methoxy-N-methylacetamide(cas: 78191-00-1) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Recommanded Product: 78191-00-1

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Han, Lu; Zhang, Xue-Ting; Xie, Dong; Tian, Shi-Kai published an article in 2021. The article was titled 《Aryne-mediated [2,3]-sigmatropic rearrangement of tertiary 2,3-allenylamines bearing an electron-withdrawing group at the α-position》, and you may find the article in Organic & Biomolecular Chemistry.Product Details of 683-57-8 The information in the text is summarized as follows:

An unprecedented [2,3]-sigmatropic rearrangement reaction of quaternary 2,3-allenylammonium ylides, generated in-situ from tertiary 2,3-allenylamines and arynes, was established. With 2-(trimethylsilyl)aryl triflates as aryne precursors, a range of tertiary 2,3-allenylamines bearing an electron-withdrawing group at the α-position smoothly participated in the aryne-mediated [2,3]-sigmatropic rearrangement at room temperature, delivering structurally diverse 2-vinylallyamines or 1-amino-1,3-dienes in moderate to excellent yields. The reaction proceeded in the absence of strong bases and transition metals, was compatible with moisture and air and tolerated a wide variety of functional groups. In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Product Details of 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Product Details of 683-57-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

In 2022,Perez-Lourido, Paulo; Madarasi, Eniko; Antal, Fanni; Esteban-Gomez, David; Wang, Gaoji; Angelovski, Goran; Platas-Iglesias, Carlos; Tircso, Gyula; Valencia, Laura published an article in Dalton Transactions. The title of the article was 《Stable and inert macrocyclic cobalt(II) and nickel(II) complexes with paraCEST response》.Category: amides-buliding-blocks The author mentioned the following in the article:

We report the synthesis of the macrocyclic ligands 3,9-PC2AMH (2,2′-(3,6,9-triaza-1(2,6)-pyridinacyclodecaphane-3,9-diyl)diacetamide) and 3,9-PC2AMtBu (2,2′-(3,6,9-triaza-1(2,6)-pyridinacyclodecaphane-3,9-diyl)bis(N-tert-butyl)acetamide) which contain a pyclen platform functionalized with acetamide or tert-butylacetamide pendant arms at positions 3 and 9 of the macrocyclic unit. The corresponding Co(II) and Ni(II) complexes were prepared, isolated and characterized as potential paramagnetic chem. exchange saturation transfer (paraCEST) agents. The X-ray structures of the Ni(II) complexes reveal six-coordination of the ligands to the metal ion. The Co(II) complex with 3,9-PC2AMtBu shows a similar six-coordinate structure in the solid state, while the Co(II) complex with 3,9-PC2AMH contains a seven-coordinate metal ion, seventh coordination being completed by the presence of an inner-sphere water mol. The structure of the Co(II) complexes was investigated using 1H NMR spectroscopy and computational methods. The complexes present a seven-coordinate structure in solution, as demonstrated by the anal. of the paramagnetic shifts using d. functional theory. Ligand protonation constants and stability constants of the complexes with 3,9-PC2AMH were determined using potentiometric titrations (I = 0,15 M NaCl). The Co(II) complex was found to be more stable than the Ni(II) analog (log KCoL = 14.46(5) and log KNiL = 13.15(3)). However, the Ni(II) and Co(II) complexes display similar rate constants characterizing the proton-assisted dissociation mechanism. The presence of highly shifted 1H NMR signals due to the amide protons in slow exchange with bulk water results in sizeable CEST signals, which are observed at +67 and +15 ppm for the Co(II) complex with 3,9-PC2AMH and +42 and +7 ppm for the Ni(II) analog at 25°C. In the experiment, the researchers used many compounds, for example, 2-Bromoacetamide(cas: 683-57-8Category: amides-buliding-blocks)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Category: amides-buliding-blocks

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Related Products of 71432-55-8In 2018 ,《Coordination-Mediated Synthesis of Purification-Free Bivalent 99mTc-Labeled Probes for in Vivo Imaging of Saturable System》 was published in Bioconjugate Chemistry. The article was written by Taira, Yuichiro; Uehara, Tomoya; Tsuchiya, Masao; Takemori, Hideaki; Mizuno, Yuki; Takahashi, Shiori; Suzuki, Hiroyuki; Hanaoka, Hirofumi; Akizawa, Hiromichi; Arano, Yasushi. The article contains the following contents:

In the synthesis of technetium-99m (99mTc) labeled target-specific ligands, the presence of a large excess of unlabeled ligands over 99mTc in the injectate hinders target accumulation of 99mTc-labeled ligands by competing for target mols. To circumvent the problem, we recently developed a concept of the metal coordination-mediated multivalency, and proved the concept with a 99mTc-labeled trivalent compound [99mTc(CO)3(CN-RGD)3]+. In this study, D-penicillamine (Pen) was selected as a chelating mol. and a cyclic RGDfK peptide was conjugated to Pen via a hexanoic linkage (Pen-Ahx-c(RGDfK)). 99mTc complexation reaction, and the stability, integrin αvβ3 binding affinity, and biodistribution of the 99mTc-labeled probe were investigated to evaluate the applicability of the concept to bivalent probes. 99mTc-[Pen-Ahx-c(RGDfK)]2 was obtained over 95% radiochem. yields under low Pen-Ahx-c(RGDfK) concentration (50 μM). 99mTc-[Pen-Ahx-c(RGDfK)]2 showed approx. 10-times higher integrin αvβ3 binding affinity than the monovalent compounds, Pen-Ahx-c(RGDfK) and c(RGDyV). In biodistribution studies, the tumor accumulation of 99mTc-[Pen-Ahx-c(RGDfK)]2 was decreased to 77% and 43% of HPLC-purified (Pen-Ahx-c(RGDfK)-free) 99mTc-[Pen-Ahx-c(RGDfK)]2 by the presence of 5 nmol of unlabeled Pen-Ahx-c(RGDfK) and Re-[Pen-Ahx-c(RGDfK)]2, resp. 99mTc-[Pen-Ahx-c(RGDfK)]2 provided tumor image without removing unlabeled ligand, while a 99mTc-labeled monovalent probe prepared from a monovalent ligand could not. These findings indicate the availability of the design concept to prepare 99mTc-labeled bivalent probes with a variety of 99mTc core and other metallic radionuclides of clin. relevance. In the experiment, the researchers used tert-Butyl N,N’-diisopropylcarbamimidate(cas: 71432-55-8Related Products of 71432-55-8)

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Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

Recommanded Product: 683-57-8In 2021 ,《Allosteric binding properties of a 1,3-alternate thiacalix[4]arene-based receptor having phenylthiourea and 2-pyridylmethyl moieties on opposite faces》 was published in New Journal of Chemistry. The article was written by Rahman, Shofiur; Tomiyasu, Hirotsugu; Wang, Chuan-Zeng; Georghiou, Paris E.; Alodhayb, Abdullah; Carpenter-Warren, Cameron L.; Elsegood, Mark R. J.; Teat, Simon J.; Redshaw, Carl; Yamato, Takehiko. The article contains the following contents:

The synthesis of three new heteroditopic receptors (5a-c) which are based on thiacalix[4]arenes in the 1,3-alternate conformation is reported herein. These new receptors each have two thiourea moieties linking Ph groups, two of which are substituted with electron-withdrawing groups at their para-positions, and at the opposite side of the thiacalix[4]arene cavity, with two 2-pyridylmethyl groups. One example (5a) was also characterized by X-ray crystallog. A limited 1H-NMR and UV-vis anion complexation study was conducted. DFT computational determinations indicated that 5c, which has strongly electron-withdrawing NO2 groups, had the most effective recognition ability towards the selected anions. The binding of Ag+ at the 2-pyridyl moieties, and the binding of the anions at the two thiourea NH groups of the p-substituted phenylthioureido moieties, resp., was also investigated. The appearance of a pos. allosteric effect with receptor 5b was also found using 1H-NMR titration experiments In the part of experimental materials, we found many familiar compounds, such as 2-Bromoacetamide(cas: 683-57-8Recommanded Product: 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Recommanded Product: 683-57-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics

《Design, synthesis, and insecticidal and fungicidal activities of quaternary ammonium salt derivatives of a triazolyphenyl isoxazoline insecticide》 was written by Huang, Shi-sheng; Zhu, Bin-bing; Wang, Kai-hua; Yu, Mo; Wang, Zi-wen; Li, Yongqiang; Liu, Yu-xiu; Zhang, Peng-li; Li, Shou-jun; Li, Ya-ling; Liu, Ai-ling; Wang, Qing-min. Recommanded Product: 683-57-8This research focused ontriazolyphenyl isooxazoline ammonium salt derivative insecticidal fungicidal activity; DP-9; fungicidal activity; insecticidal activity; isoxazoline; quaternary ammonium; structure optimization. The article conveys some information:

Insect pests seriously decrease the yield and quality of agricultural crops. Resistance to commonly used insecticides is increasingly undermining their effectiveness, and therefore the development of agents with novel modes of action is desirable. Isoxazolines are a new class of insecticides that act on γ-aminobutyric acid (GABA) gated chloride channels. In this work, we used the highly active 4-triazolyphenyl isoxazoline DP-9 as a parent structure to design and synthesize a series of quaternary ammonium salt (QAS) derivatives, and we systematically evaluated their insecticidal and antifungal activities. RESULTS : Many of the synthesized QASs exhibit insecticidal activities equivalent to or higher than that of DP-9. In particular, compounds I-31 (93%, 0.00005 mg/L) and I-34 (80%, 0.00001 mg/L) showed insecticidal activities against diamondback moth larvae that were 2-10 times higher than those of fluralaner (70%, 0.0001 mg/L) and DP-9 (80%, 0.0001 mg/L), in addition to showing excellent activities against oriental armyworm, fall armyworm, cotton bollworm, corn borer, and mosquito larvae. Furthermore, all of the synthesized compounds also showed broad-spectrum fungicidal activities. The insecticidal activities of QAS derivatives of DP-9 were the same as or better than the activity of DP-9. Compounds I-31 and I-34 showed better insecticidal activities against diamondback moth larvae than fluralaner and DP-9, and thus are promising new candidates for insecticide research. In the experimental materials used by the author, we found 2-Bromoacetamide(cas: 683-57-8Recommanded Product: 683-57-8)

2-Bromoacetamide(cas: 683-57-8) can be used in preparation of (2-carbamoylmethoxy-5-chloro-benzyl)-carbamic acid tert-butyl ester. It was aslo used as precursor to dehydropeptidase I inactivator.Recommanded Product: 683-57-8

Referemce:
Amide – Wikipedia,
Amide – an overview | ScienceDirect Topics