Tag: 100-200

《Stereoselective assembly of 3,4-epoxypyrrolines via nucleophilic addition induced domino cyclization of 6-halo-1-oxa-4-azahexatrienes》 was published in Organic Chemistry Frontiers in 2020. These research results belong to Smetanin, Ilia A.; Agafonova, Anastasiya V.; Rostovskii, Nikolai V.; Khlebnikov, Alexander F.; Yufit, Dmitry S.; Novikov, Mikhail S.. Application of 39546-32-2 The article mentions the following:

A two-step method for the preparation of 3,4-epoxypyrroline derivatives (6-oxa-3-azabicyclo[3.1.0]hex-2-enes) from 2-halo-2H-azirine-2-carboxylates, diazo keto esters and amines was developed. 6-Halo-1-oxa-4-azahexa-1,3,5-trienes, prepared in the first step from the azirines and diazo compounds under Rh(II) catalysis were subjected to nucleophile-induced tandem cyclization to afford highly functionalized rac-(1R,4R,5S)-6-oxa-3-azabicyclo[3.1.0]hex-2-enes in good yields. The stereochem. outcome of the tandem cyclization induced by the secondary amines was rationalized in terms of the structural rigidity of the betaine-type precursor due to the hydrogen bonding between the ammonium group and ester group adjacent to the halogen atom. Post-modification of the 3,4-epoxypyrrolines by the Stille cross-coupling, reduction, and UV-irradiation was also demonstrated.Piperidine-4-carboxamide(cas: 39546-32-2Application of 39546-32-2) was used in this study.

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Examples of direct uses of amines and their salts are as corrosion inhibitors in boilers and in lubricating oils (morpholine), as antioxidants for rubber and roofing asphalt (diarylamines), as stabilizers for cellulose nitrate explosives (diphenylamine), as protectants against damage from gamma radiation (diarylamines), as developers in photography (aromatic diamines), as flotation agents in mining, as anticling and waterproofing agents for textiles, as fabric softeners, in paper coating, and for solubilizing herbicides.Application of 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Solid phase syntheses of peptoid like arylureido compounds and sequencing of isobars without molecular encoding》 was published in Organic & Biomolecular Chemistry in 2019. These research results belong to Asif, Kanwal; O’Brien, Gregory L.; Goodman, Scott M.; Suwal, Sujit. Reference of Piperidine-4-carboxamide The article mentions the following:

Arylureido-backbone containing peptoid-like trimers were prepared using the one-bead-one-compound approach. Isobaric mols. were synthesized from isocyanate precursors that contain alkyl halide handles at the ortho and para-positions in the Ph ring. After chain extension with a primary amine, the piperazine-capped mols. were sequenced using tandem mass spectrometry and successfully identified based on their fragmentation pattern without a need for internal mol. encoding. In addition to this study using Piperidine-4-carboxamide, there are many other studies that have used Piperidine-4-carboxamide(cas: 39546-32-2Reference of Piperidine-4-carboxamide) was used in this study.

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Amines can be classified according to the nature and number of substituents on nitrogen. Aliphatic amines contain only H and alkyl substituents. Aromatic amines have the nitrogen atom connected to an aromatic ring.Important amines include amino acids, biogenic amines, trimethylamine, and aniline. Inorganic derivatives of ammonia are also called amines, such as monochloramine (NClH2).Reference of Piperidine-4-carboxamide

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of V-0219: A Small-Molecule Positive Allosteric Modulator of the Glucagon-Like Peptide-1 Receptor toward Oral Treatment for “”Diabesity””》 was written by Decara, Juan M.; Vazquez-Villa, Henar; Brea, Jose; Alonso, Monica; Srivastava, Raj Kamal; Orio, Laura; Alen, Francisco; Suarez, Juan; Baixeras, Elena; Garcia-Carceles, Javier; Escobar-Pena, Andrea; Lutz, Beat; Rodriguez, Ramon; Codesido, Eva; Garcia-Ladona, F. Javier; Bennett, Teresa A.; Ballesteros, Juan A.; Cruces, Jacobo; Loza, Maria I.; Benhamu, Bellinda; Rodriguez de Fonseca, Fernando; Lopez-Rodriguez, Maria L.. Recommanded Product: 39546-32-2 And the article was included in Journal of Medicinal Chemistry on April 14 ,2022. The article conveys some information:

Peptidic agonists of the glucagon-like peptide-1 receptor (GLP-1R) have gained a prominent role in the therapy of type-2 diabetes and are being considered for reducing food intake in obesity. Potential advantages of small mols. acting as pos. allosteric modulators (PAMs) of GLP-1R, including oral administration and reduced unwanted effects, could improve the utility of this class of drugs. Here, we describe the discovery of compound 9 (4-{[1-({3-[4-(trifluoromethyl)phenyl]-1,2,4-oxadiazol-5-yl}methyl)piperidin-3-yl]methyl}morpholine, V-0219) that exhibits enhanced efficacy of GLP-1R stimulation, subnanomolar potency in the potentiation of insulin secretion, and no significant off-target activities. The identified GLP-1R PAM shows a remarkable in vivo activity, reducing food intake and improving glucose handling in normal and diabetic rodents. Enantioselective synthesis revealed oral efficacy for (S)-9 in animal models. Compound 9 behavior bolsters the interest of a small-mol. PAM of GLP-1R as a promising therapeutic approach for the increasingly prevalent obesity-associated diabetes. The results came from multiple reactions, including the reaction of Piperidine-4-carboxamide(cas: 39546-32-2Recommanded Product: 39546-32-2)

Piperidine-4-carboxamide(cas: 39546-32-2) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Recommanded Product: 39546-32-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Discovery of novel xanthine compounds targeting DPP-IV and GPR119 as anti-diabetic agents》 was written by Li, Gang; Huan, Yi; Yuan, Baokun; Wang, Jin; Jiang, Qian; Lin, Ziyun; Shen, Zhufang; Huang, Haihong. Computed Properties of C7H15NOThis research focused onxanthine derivative preparation GPR119 DPPIV targeting diabetes; DPP-IV; Dual ligands; GPR119; Merged pharmacophores; Xanthine derivatives. The article conveys some information:

A series of xanthine derivatives as potent dual ligands targeting DPP-IV and GPR119 was discovered through an approach of the merged pharmacophores of GPR119 agonists and DPP-IV inhibitor linagliptin. Systematic optimization of general structure 5 led to the identification of compound 20i with selective DPP-IV inhibition, good GPR119 agonism activity and favorable metabolic stability. Docking study was performed to elucidate the potent DPP-IV inhibition of 20i. Compound 20i may serve as a tool compound for further design of anti-diabetic drugs targeting both DPP-IV and GPR119. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Computed Properties of C7H15NO)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKComputed Properties of C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Correlation Study Between Biochemical and Molecular Pathways of Trichoderma harzianum Recombinant Strains on Plant Growth and Health》 was written by Eslahi, Negin; Kowsari, Mojegan; Zamani, Mohammad Reza; Motallebi, Mostafa. Application In Synthesis of Triacetonamine And the article was included in Journal of Plant Growth Regulation on April 30 ,2022. The article conveys some information:

The genus of Trichoderma are mostly found in soil. Trichoderma species are known as probiotic with biocontrol and biofertilizer activity. They are producers of secondary metabolites like volatile organic compounds (VOCs) with antifungal, antibacterial, and growth promoter properties. Trichoderma VOCs can induce resistance to plant pathogens leading to improved plant growth and health. In this study, we compared the performance of Trichoderma harzianum recombinant strains (T13 and T15), containing chimeric chit42 with Chitin Binding Domain (ChBD) and wild-type (Tw) strain on plant growth promotion. To achieve this goal, the ability of strains in plant growth-promoting (production of IAA and siderophore) and fungal gene expression involved in biocontrol and biofertilizer activity, as well as, VOCs from T. harzianum strains (wild-type and recombinants) by headspace gas chromatog.-mass spectrometry (GC-SPME) have been investigated. In addition, bean seeds were exposed to the T. harzianum strains in a shared atm. In addition to growth indexes (root fresh and dry weight, root length, and lateral root number), expression of root growth-related genes was measured by qTR-PCR. The results showed that recombinant strains had increased ability to produce IAA and siderophore. In addition, T. harzianum genes expression anal. demonstrated an upregulation in biocontrol and biofertilizer-associated genes in T13 and T15 strains. VOCs profile of strains revealed a total of 11, 57, and 29 metabolites from the Tw, T15, and T13, resp. Most of the VOCs produced from T13 and T15 had growth enhancement and biocontrol activity, resp., on the plant. The diversity of VOCs from T. harzianum recombinant strains (T13 and T15) involved in growth-promoting and biocontrol activity, was higher than the Tw strain. These compounds might work synergistically to promote growth, and enhance biocontrol and antifungal activity, and thus, recombinant strains with higher diversity of VOCs might be more effective than Tw. Plant phenotypic characterization and root genes expression showed that the recombinant strains, T13 particularly, were effective in growth-promoting compared to the Tw strain. In this study, we observed a pos. correlation among the production of secondary metabolite and mol. pathways of recombinant strains on plant growth activity. This finding can create a link between basic and applied studies in agriculture. The experimental process involved the reaction of Triacetonamine(cas: 826-36-8Application In Synthesis of Triacetonamine)

Triacetonamine(cas: 826-36-8) is a member of piperidine. Piperidine is a key saturated heterocyclic scaffold found in several of the top-selling small molecule pharmaceuticals and natural alkaloids, with a diverse range of biological activities. Hence, continuous efforts have been made to develop convenient methods to prepare piperidine derivatives.Application In Synthesis of Triacetonamine

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C6H11NOIn 2021 ,《In Situ-Doped Superacid in the Covalent Triazine Framework Membrane for Anhydrous Proton Conduction in a Wide Temperature Range from Subzero to Elevated Temperature》 was published in ACS Applied Materials & Interfaces. The article was written by Huang, Wenbo; Li, Bin; Wu, Yue; Zhang, Ying; Zhang, Wenxiang; Chen, Shuhui; Fu, Yu; Yan, Tong; Ma, Heping. The article contains the following contents:

Synthesis of solid-state proton-conducting membranes with low activation energy and high proton conductivity under anhydrous conditions is a great challenge. Here, we show a simple and convenient way to prepare covalent triazine framework membranes (CTF-Mx) with acid in situ doping for anhydrous proton conduction in a wide temperature range from subzero to elevated temperature (160 °C). The low proton dissociation energy and continuous hydrogen bond network in CTF-Mx make the membrane achieve high proton conductivity from 1.21×10-3 S cm-1 (-40 °C) to 2.08×10-2 S cm-1 (160 °C) under anhydrous conditions. Mol. dynamics and proton relaxation time analyses reveal proton hopping at low activation energies with greatly enhanced mobility in the CTF membranes. After reading the article, we found that the author used 1-Methyl-4-piperidone(cas: 1445-73-4Electric Literature of C6H11NO)

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.Electric Literature of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

HPLC of Formula: 1445-73-4In 2020 ,《Propargylated monocarbonyl curcumin analogues: synthesis, bioevaluation and molecular docking study》 appeared in Medicinal Chemistry Research. The author of the article were Nagargoje, Amol A.; Akolkar, Satish V.; Subhedar, Dnyaneshwar D.; Shaikh, Mubarak H.; Sangshetti, Jaiprakash N.; Khedkar, Vijay M.; Shingate, Bapurao B.. The article conveys some information:

Abstract: In the current exptl. study, we have synthesized new monocarbonyl curcumin analogs bearing propargyl ether moiety in their structure and evaluated for in vitro antifungal and radical scavenging activity. The antifungal activity was carried out against five human pathogenic fungal strains such as Candida albicans, Fusarium oxysporum, Aspergillus flavus, Aspergillus niger and Cryptococcus neoformans. Most of the curcumin analogs displayed excellent to moderate fungicidal activity when compared with standard drug Miconazole. Also, synthesized analogs exhibited potential radical scavenging activity as compared with standard antioxidant Butylated hydroxyl toluene (BHT). Based on biol. data, structure-activity relationship (SAR) were also discussed. Furthermore, in silico computational study was carried out to know binding interactions of synthesized analogs in the active sites of enzyme sterol 14α-demethylase (CYP51). [graphic not available: see fulltext] In addition to this study using 1-Methyl-4-piperidone, there are many other studies that have used 1-Methyl-4-piperidone(cas: 1445-73-4HPLC of Formula: 1445-73-4) was used in this study.

1-Methyl-4-piperidone(cas: 1445-73-4) is a member of piperidine. Piperidine-containing compounds are also frequently employed in synthesis as ligands or auxiliaries. Accordingly, many efforts have been devoted to the development of novel methods for the synthesis of these compounds over the years.HPLC of Formula: 1445-73-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Continuous-Flow Synthesis of Phenothiazine Antipsychotics: A Feasibility Study》 were Movsisyan, Marine; De Coen, Laurens M.; Heugebaert, Thomas S. A.; Verlee, Arno; Roman, Bart I.; Stevens, Christian V.. And the article was published in European Journal of Organic Chemistry in 2019. Safety of 2-(Piperidin-4-yl)ethanol The author mentioned the following in the article:

The continuous flow synthesis of a model phenothiazine I antipsychotic was reported, using 3-chloropropionyl chloride as a central building block. The basic phenothiazine-derived scaffold was (atom)-efficiently and mildly synthesized with the aim to present continuous flow technol. as a contributor to fast and efficient synthesis of challenging APIs, which were experiencing supply disruptions and global shortages. The experimental process involved the reaction of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Safety of 2-(Piperidin-4-yl)ethanol)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKSafety of 2-(Piperidin-4-yl)ethanol

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2016,Park, Jung Sang; Im, Weonbin; Choi, Sunghak; Park, Sook Jin; Jung, Jun Min; Baek, Ki Seon; Son, Han Pyo; Sharma, Satyasheel; Kim, In Su; Jung, Young Hoon published 《Discovery and SAR of N-(1-((substituted piperidin-4-yl)methyl)-3-methoxypiperidin-4-yl)-2-methoxybenzamide derivatives: 5-Hydroxytryptamine receptor 4 agonist as a potent prokinetic agent》.European Journal of Medicinal Chemistry published the findings.Formula: C7H15NO The information in the text is summarized as follows:

A series of novel benzamide derivatives altering the 4-fluorophenylalkyl moiety in cisapride, was synthesized as 5-HT4 receptor agonists; and SAR of these analogs was examined on in vitro and in vivo prokinetic activities. These compounds were synthesized for high 5-HT4 receptor binding affinities and low hERG affinities. Several types of analogs were obtained and screened for 5-HT4 binding, hERG blocking, agonism and gastric emptying assessment. Among the analogs, compound I showed promising results compared with the other analogs with respect to gastric emptying rates in rats and can be a clin. candidate for the development of a potent prokinetic agent to treat GI disorders. In the experiment, the researchers used many compounds, for example, 2-(Piperidin-4-yl)ethanol(cas: 622-26-4Formula: C7H15NO)

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) have been used as an intermediate in the synthetic preparation of cellular-active allosteric inhibitors of FAKFormula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2014,Gao, Mingzhang; Wang, Min; Zheng, Qi-Huang published 《Concise and high-yield synthesis of T808 and T808P for radiosynthesis of [18F]-T808, a PET tau tracer for Alzheimer’s disease》.Bioorganic & Medicinal Chemistry Letters published the findings.COA of Formula: C7H15NO The information in the text is summarized as follows:

The authentic standard T808 and its corresponding mesylate precursor T808P were synthesized in six steps using Et vinyl ether and trichloroacetyl chloride as starting materials. The overall chem. yields of T808 and T808P were 35% and 52%, resp. [18F]-T808 was synthesized from T808P by the nucleophilic substitution with K[18F]F/Kryptofix 2.2.2 and isolated by HPLC combined with solid-phase extraction (SPE) purification in 35-45% radiochem. yield with 37-370 GBq/μmol specific activity at end of bombardment (EOB). In addition to this study using 2-(Piperidin-4-yl)ethanol, there are many other studies that have used 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: C7H15NO) was used in this study.

2-(Piperidin-4-yl)ethanol(cas: 622-26-4) can be used to synthese ursolic acid derivatives, spiroimidazolidinone NPC1L1 inhibitors, neurokinin-2 receptor antagonists, antagonists for inhibition of platelet aggregation.COA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem