Category: 109384-19-2

Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylateIn 2020 ,《Structure-Activity Relationship for the Oxadiazole Class of Antibacterials》 was published in ACS Medicinal Chemistry Letters. The article was written by Boudreau, Marc A.; Ding, Derong; Meisel, Jayda E.; Janardhanan, Jeshina; Spink, Edward; Peng, Zhihong; Qian, Yuanyuan; Yamaguchi, Takao; Testero, Sebastian A.; O’Daniel, Peter I.; Leemans, Erika; Lastochkin, Elena; Song, Wei; Schroeder, Valerie A.; Wolter, William R.; Suckow, Mark A.; Mobashery, Shahriar; Chang, Mayland. The article contains the following contents:

A structure-activity relationship (SAR) for the oxadiazole class of antibacterials was evaluated by syntheses of 72 analogs and determination of the minimal-inhibitory concentrations (MICs) against the ESKAPE panel of bacteria. Selected compounds were further evaluated for in vitro toxicity, plasma protein binding, pharmacokinetics (PK), and a mouse model of methicillin-resistant Staphylococcus aureus (MRSA) infection. Oxadiazole 72c shows potent in vitro antibacterial activity, exhibits low clearance, a high volume of distribution, and 41% oral bioavailability, and shows efficacy in mouse models of MRSA infection. In the experiment, the researchers used tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Quality Control 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.Quality Control of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Zha, Liang; Xie, Yunfeng; Wu, Chengyao; Lei, Ming; Lu, Xueer; Tang, Wenjian; Zhang, Jing published an article in European Journal of Medicinal Chemistry. The title of the article was 《Novel benzothiazole-urea hybrids: Design, synthesis and biological activity as potent anti-bacterial agents against MRSA》.Category: piperidines The author mentioned the following in the article:

Novel benzothiazole-urea hybrids were designed, synthesized and evaluated for their anti-bacterial activity. They only exhibited anti-bacterial activity against Gram-pos. bacteria, including clin. methicillin-resistant S. aureus (MRSA), compounds I (R = 4-CF3C6H4NH, 2,4-F2C6H3NH), II (R1 = H, R2 = 4-CF3C6H4NH), II (R1 = Cl, R2 = 4-CF3C6H4NH), and II (R1 = Cl, R2 = 2,4-F2C6H3NH) exhibited potent activity (MIC = 0.39 and 0.39/0.78μM against SA and MRSA, resp.). Crystal violet assay showed that compounds I (R = 4-CF3C6H4NH) II (R1 = H, R2 = 4-CF3C6H4NH), and II (R1 = Cl, R2 = 2,4-F2C6H3NH) not only inhibited the formation of biofilms but also eradicated preformed biofilms. Compound II (R1 = Cl, R2 = 2,4-F2C6H3NH) had membrane disruption, little propensity to induce resistance, benign safety and in vivo anti-MRSA efficacy in a mouse model of abdominal infection. Therefore, authors data demonstrated the potential to advance benzothiazole-urea hybrids as a new class of antibiotics. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Category: piperidines)

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.Category: piperidines

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

《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

Formula: C10H19NO3In 2019 ,《Discovery of (R)-5-((5-(1-methyl-1H-pyrazol-4-yl)-4-(methylamino)pyrimidin-2-yl)amino)-3-(piperidin-3-yloxy)picolinonitrile, a novel CHK1 inhibitor for hematologic malignancies》 appeared in European Journal of Medicinal Chemistry. The author of the article were Tong, Lexian; Song, Pinrao; Jiang, Kailong; Xu, Lei; Jin, Tingting; Wang, Peipei; Hu, Xiaobei; Fang, Sui; Gao, Anhui; Zhou, Yubo; Liu, Tao; Li, Jia; Hu, Yongzhou. The article conveys some information:

Through virtual screening, we identified the lead compound MCL1020, which exhibited modest CHK1 inhibitory activity. Then a series of 5-(pyrimidin-2-ylamino)picolinonitrile derivatives as CHK1 inhibitors were discovered by further rational optimization. One promising mol., I, whose potency was one of the best, had an IC50 of 0.4 nM with remarkable selectivity (>4300-fold CHK1 vs. CHK2). Compound I effectively inhibited the growth of malignant hematopathy cell lines especially Z-138 (IC50: 0.013 μM) and displayed low affinity for hERG (IC50 > 40 μM). Moreover, I significantly suppressed the tumor growth in Z-138 cell inoculated xenograft model (20 mg/kg I.V., TGI = 90.29%) as a single agent with body weight unaffected. Taken together, our data demonstrated compound I could be a promising drug candidate for the treatment of hematol. malignancies. The results came from multiple reactions, including the reaction of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Formula: C10H19NO3)

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.Formula: C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Angewandte Chemie, International Edition included an article by Wu, Jingjing; Baer, Robin M.; Guo, Lin; Noble, Adam; Aggarwal, Varinder K.. Related Products of 109384-19-2. The article was titled 《Photoinduced Deoxygenative Borylations of Aliphatic Alcohols》. The information in the text is summarized as follows:

A photochem. method for converting aliphatic alcs. into boronic esters is described. Preactivation of the alc. as a 2-iodophenyl-thionocarbonate enables a novel Barton-McCombie-type radical deoxygenation that proceeds efficiently with visible light irradiation and without the requirement for a photocatalyst, a radical initiator, or Sn or Si hydrides. The resultant alkyl radical is intercepted by bis(catecholato)diboron, furnishing boronic esters from a diverse range of structurally complex alcs. In the part of experimental materials, we found many familiar compounds, such as tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Related Products of 109384-19-2)

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.Related Products of 109384-19-2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2019,Bioorganic & Medicinal Chemistry Letters included an article by Wang, Jiming; Zhang, Xiangyu; Yan, Jiangkun; Li, Wei; Jiang, Qinwen; Wang, Xinran; Zhao, Dongmei; Cheng, Maosheng. Electric Literature of C10H19NO3. The article was titled 《Design, synthesis and biological evaluation of curcumin analogues as novel LSD1 inhibitors》. The information in the text is summarized as follows:

Histone lysine-specific demethylase 1 (LSD1) was the first discovered histone demethylase. Inactivating LSD1 or downregulating its expression inhibits cancer-cell development, and thus, it is an attractive mol. target for the development of novel cancer therapeutics. In this study, we worked on the structural optimization of natural products and identified 30 novel LSD1 inhibitors. Utilizing a structure-based drug design strategy, we designed and synthesized a series of curcumin analogs that were shown to be potent LSD1 inhibitors in the enzyme assay. Compound WB07 (I) displayed the most potent LSD1 inhibitory activity, with an IC50 value of 0.8μM. Moreover, WA20 (II) showed an anticlonogenic effect on A549 cells with an IC50 value of 4.4μM. Mol. docking simulations were also carried out, and the results indicated that the inhibitors bound to the protein active site located around the key residues of Asp555 and Asp556. These findings suggested that compounds II and I are the first curcumin analog-based LSD1 inhibitors with remarkable A549 suppressive activity, providing a novel scaffold for the development of LSD1 inhibitors. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Electric Literature of C10H19NO3)

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.Electric Literature of C10H19NO3

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Efficacy and Tolerability of Pyrazolo[1,5-a]pyrimidine RET Kinase Inhibitors for the Treatment of Lung Adenocarcinoma》 was written by Mathison, Casey J. N.; Chianelli, Donatella; Rucker, Paul V.; Nelson, John; Roland, Jason; Huang, Zhihong; Yang, Yang; Jiang, Jiqing; Xie, Yun Feng; Epple, Robert; Bursulaya, Badry; Lee, Christian; Gao, Mu-Yun; Shaffer, Jennifer; Briones, Sergio; Sarkisova, Yelena; Galkin, Anna; Li, Lintong; Li, Nanxin; Li, Chun; Hua, Su; Kasibhatla, Shailaja; Kinyamu-Akunda, Jacqueline; Kikkawa, Rie; Molteni, Valentina; Tellew, John E.. Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate And the article was included in ACS Medicinal Chemistry Letters in 2020. The article conveys some information:

RET (REarranged during Transfection) kinase gain-of-function aberrancies have been identified as potential oncogenic drivers in lung adenocarcinoma, along with several other cancer types, prompting the discovery and assessment of selective inhibitors. Internal mining and anal. of relevant kinase data informed the decision to investigate a pyrazolo[1,5-a]pyrimidine scaffold, where subsequent optimization led to the identification of compound WF-47-JS03 (1), a potent RET kinase inhibitor with >500-fold selectivity against KDR (Kinase insert Domain Receptor) in cellular assays. In subsequent mouse in vivo studies, compound 1 demonstrated effective brain penetration and was found to induce strong regression of RET-driven tumor xenografts at a well-tolerated dose (10 mg/kg, po, qd). Higher doses of 1, however, were poorly tolerated in mice, similar to other pyrazolo[1,5-a]pyrimidine compounds at or near the efficacious dose, and indicative of the narrow therapeutic windows seen with this scaffold. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-hydroxypiperidine-1-carboxylate(cas: 109384-19-2Safety 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.Safety of tert-Butyl 4-hydroxypiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem