Day: October 18, 2022

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

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

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

《Amine-Responsive Disassembly of AuI-CuI Double Salts for Oxidative Carbonylation》 was published in Angewandte Chemie, International Edition in 2020. These research results belong to Cao, Yanwei; Yang, Jian-Gong; Deng, Yi; Wang, Shengchun; Liu, Qi; Shen, Chaoren; Lu, Wei; Che, Chi-Ming; Chen, Yong; He, Lin. Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate The article mentions the following:

A sensitive amine-responsive disassembly of self-assembled AuI-CuI double salts was observed and its use for the synergistic catalysis was enlightened. Study of the disassembly of [Au(NHC)2][CuI2] revealed the contribution of Cu-assisted ligand exchange of N-heterocyclic carbene (NHC) by amine in [Au(NHC)2]+ and the capacity of [CuI2]- on the oxidative step. By integrating the implicative information coded in the responsive behavior and inherent catalytic functions of d10 metal complexes, a catalyst for the oxidative carbonylation of amines was developed. The advantages of this method were clearly reflected on mild reaction conditions and the significantly expanded scope (51 examples); both primary and steric secondary amines can be employed as substrates. The cooperative reactivity from Au and Cu centers, as an indispensable prerequisite for the excellent catalytic performance, was validated in the synthesis of (un)sym. ureas and carbamates. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Application In Synthesis of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Luo, Guoshun; Lin, Xin; Li, Zhenbang; Xiao, Maoxu; Li, Xinyu; Zhang, Dayong; Xiang, Hua published an article in 2021. The article was titled 《Structure-guided modification of isoxazole-type FXR agonists: Identification of a potent and orally bioavailable FXR modulator》, and you may find the article in European Journal of Medicinal Chemistry.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate The information in the text is summarized as follows:

Farnesoid X receptor (FXR) agonists are emerging as potential therapeutics for the treatment of various metabolic diseases, as they display multiple effects on bile acid, lipid, and glucose homeostasis. Although the steroidal obeticholic acid, a full FXR agonist, was recently approved, several side effects probably due to insufficient pharmacol. selectivity impede its further clin. application. Activating FXR in a partial manner is therefore crucial in the development of novel FXR modulators. Our efforts focusing on isoxazole-type FXR agonists, common nonsteroidal agonists for FXR, led to the discovery a series of novel FXR agonists bearing aryl urea moieties through structural simplification of LJN452 (phase 2). Encouragingly, compound I was discovered as a potent FXR agonist which exhibited similar FXR agonism potency but lower maximum efficacy compared to full agonists GW4064 and LJN452 in cell-based FXR transactivation assay. Extensive in vitro evaluation further confirmed partial efficacy of I in cellular FXR-dependent gene modulation, and revealed its lipid-reducing activity. More importantly, orally administration of I in mice exhibited desirable pharmacokinetic characters resulting in promising in vivo FXR agonistic activity. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate)

tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas:109384-19-2) is a 4-hydroxypyridine with a boc protecting group used in the preparation of neurologically active agents and other pharmaceutical compounds.Name: tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Thu, Zaw Min; Sun, Jian; Ji, Jingwen; He, Lili; Ji, Jinbo; Iqbal, Zafar; Myo, Ko Ko; Gao, Yuanyu; Zhai, Lijuan; Mu, Yangxiu; Tang, Dong; Vidari, Giovanni; Yang, Haikang; Yang, Zhixiang published an article in 2021. The article was titled 《Synthesis and antibacterial evaluation of new monobactams》, and you may find the article in Bioorganic & Medicinal Chemistry Letters.Application of 87120-72-7 The information in the text is summarized as follows:

Monobactams play an important role in antibiotic drug discovery. Based on the structural characteristics of aztreonam and its biol. targets, six new monobactam derivatives were synthesized and their in vitro antibacterial activities were investigated. Some compounds showed higher activities against tested gram-neg. bacteria than that of parent aztreonam. Monobactam I exhibited the most potent activities, with MIC ranging from 0.25 to 2μg/mL against most bacteria. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Application of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Many important products require amines as part of their syntheses. Methylamine is utilized in the production of the analgesic meperidine (trade name Demerol) and the photographic developer Metol (trademark), and dimethylamine is used in the synthesis of the antihistamine diphenhydramine (trade name Benadryl), the solvent dimethylformamide (DMF), and the rocket propellant 1,1-dimethylhydrazine. The synthesis of the insect repellent N,N-diethyl-m-toluamide (DEET) incorporates diethylamine while that of the synthetic fibre Kevlar requires aromatic amines.Application of 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Chen, Nanjun; Hu, Chuan; Wang, Ho Hyun; Kim, Sun Pyo; Kim, Hae Min; Lee, Won Hee; Bae, Joon Yong; Park, Jong Hyeong; Lee, Young Moo published an article in 2021. The article was titled 《Poly(Alkyl-Terphenyl Piperidinium) Ionomers and Membranes with an Outstanding Alkaline-Membrane Fuel-Cell Performance of 2.58 W cm-2》, and you may find the article in Angewandte Chemie, International Edition.Recommanded Product: 1-Methyl-4-piperidone The information in the text is summarized as follows:

Aryl-ether-free anion-exchange ionomers (AEIs) and membranes (AEMs) have become an important benchmark to address the insufficient durability and power-d. issues associated with AEM fuel cells (AEMFCs). Here, we present aliphatic chain-containing poly(diphenyl-terphenyl piperidinium) (PDTP) copolymers to reduce the Ph content and adsorption of AEIs and to increase the mech. properties of AEMs. Specifically, PDTP AEMs possess excellent mech. properties (storage modulus>1800 MPa, tensile strength>70 MPa), H2 fuel-barrier properties (<10 Barrer), good ion conductivity, and ex-situ stability. Meanwhile, PDTP AEIs with low Ph content and high-water permeability display excellent peak power densities (PPDs). The present AEMFCs reach outstanding PPDs of 2.58 W cm-2(>7.6 A cm-2c.d.) and 1.38 W cm-2 at 80°C in H2/O2 and H2/air, resp., along with a specific power (PPD/catalyst loading) over 8 W mg-1, which is the highest record for Pt-based AEMFCs so far. In addition to this study using 1-Methyl-4-piperidone, there are many other studies that have used 1-Methyl-4-piperidone(cas: 1445-73-4Recommanded Product: 1-Methyl-4-piperidone) 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.Recommanded Product: 1-Methyl-4-piperidone

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Lu, Shaoyong; Fu, Zhong; Li, Fu; Weng, Kangkang; Zhou, Likuan; Zhang, Lipeng; Yang, Yuchen; Qiu, Hengwei; Liu, Dan; Qing, Wenyue; Ding, He; Sheng, Xing; Chen, Menglu; Tang, Xin; Duan, Lian; Liu, Wenyong; Wu, Longjia; Yang, Yixing; Zhang, Hao; Li, Jinghong published an article in Angewandte Chemie, International Edition. The title of the article was 《Beyond a Linker: The Role of Photochemistry of Crosslinkers in the Direct Optical Patterning of Colloidal Nanocrystals》.Electric Literature of C6H11NO The author mentioned the following in the article:

Surface chem. mediated direct optical patterning represents an emerging strategy for incorporating colloidal nanocrystals (NCs) in integrated optoelectronic platforms including displays and image sensors. However, the role of photochem. of crosslinkers and other photoactive species in patterning remains elusive. Here we show the design of nitrene- and carbene-based photocrosslinkers can strongly affect the patterning capabilities and photophys. properties of NCs, especially quantum dots (QDs). Their role beyond phys. linkers stems from structure-dictated electronic configuration, energy alignment and associated reaction kinetics and thermodn. Patterned QD layers with designed carbene-based crosslinkers fully preserve their photoluminescent and electroluminescent properties. Patterned light emitting diodes (QLEDs) show a maximum external quantum efficiency of ∼12 % and lifetime over 4800 h, among the highest for reported patterned QLEDs. These results would guide the rational design of photoactive species in NC patterning and create new possibilities in the monolithic integration of NCs in high-performance device platforms. The experimental part of the paper was very detailed, including the reaction process of 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 is ubiquitous structural motif widely occurred in diverse synthetically and naturally occurring bioactive molecules. Piperidines are an immensely important class of compounds medicinally: the piperidine ring is the most common heterocyclic subunit among FDA approved drugs.Electric Literature of C6H11NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

COA of Formula: C7H15NOIn 2013 ,《Structure-based discovery of cellular-active allosteric inhibitors of FAK》 appeared in Bioorganic & Medicinal Chemistry Letters. The author of the article were Tomita, Naoki; Hayashi, Yoko; Suzuki, Shinkichi; Oomori, Yoshimasa; Aramaki, Yoshio; Matsushita, Yoshihiro; Iwatani, Misa; Iwata, Hidehisa; Okabe, Atsutoshi; Awazu, Yoshiko; Isono, Osamu; Skene, Robert J.; Hosfield, David J.; Miki, Hiroshi; Kawamoto, Tomohiro; Hori, Akira; Baba, Atsuo. The article conveys some information:

In order to develop potent and selective focal adhesion kinase (FAK) inhibitors, synthetic studies on pyrazolo[4,3-c][2,1]benzothiazines targeted for the FAK allosteric site were carried out. Based on the X-ray structural anal. of the co-crystal of the lead compound, 8-(4-ethylphenyl)-5-methyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazine 4,4-dioxide 1 with FAK, we designed and prepared 1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin derivatives which selectively inhibited kinase activity of FAK without affecting seven other kinases. The optimized compound, N-(4-tert-butylbenzyl)-1,5-dimethyl-1,5-dihydropyrazolo[4,3-c][2,1]benzothiazin-8-amine 4,4-dioxide 30 possessed significant FAK kinase inhibitory activities both in cell-free (IC50 = 0.64 μM) and in cellular assays (IC50 = 7.1 μM). These results clearly demonstrated a potential of FAK allosteric inhibitors as antitumor agents. The experimental part of the paper was very detailed, including the reaction process of 2-(Piperidin-4-yl)ethanol(cas: 622-26-4COA of Formula: 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 FAKCOA of Formula: C7H15NO

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem