Category: 214834-18-1

Ding, Lu et al. published their research in Zhongguo Yaowu Huaxue Zazhi in 2012 | CAS: 214834-18-1

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Synthetic Route of C11H20N2O2S

Synthesis of G protein-coupled receptor 119 agonist MBX-2982 was written by Ding, Lu;Luo, Tang;Song, Kai-zhen;Gong, Ping;Han, Jing. And the article was included in Zhongguo Yaowu Huaxue Zazhi in 2012.Synthetic Route of C11H20N2O2S This article mentions the following:

Type 2 diabetes is emerging as a disease of staggering proportions in twenty-first century. MBX-2982, discovered by Metabolex company, is a potential oral first-in-class treatment for type 2 diabetes that targets G protein-coupled receptor 119. According to the synthetic methods of MBX-2982 in literature, a new route was developed. The target compound was prepared from 4-cyanopiperidine-1-carboxylic tert-Bu ester via five steps including sulfidation, condensation, etherification, deprotection and substitution. The overall yield was 42.8% (based on 4-cyanopiperidine-1-carboxylic tert-Bu ester), which was 12% higher than that reported in the literature. The synthetic methods of intermediate 2, 6 and MBX-2982 were improved. The final structure and some intermediates were confirmed by 1H-NMR and MS. Compared with the synthetic process in literature, this route has an economic advantage in view of application to in-depth study. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1Synthetic Route of C11H20N2O2S).

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine’s the lone pair does not contribute to the aromatic system but importantly influences the chemical properties of pyridine, as it easily supports bond formation via an electrophilic attack. Several pyridine derivatives play important roles in biological systems. While its biosynthesis is not fully understood, nicotinic acid (vitamin B3) occurs in some bacteria, fungi, and mammals.Synthetic Route of C11H20N2O2S

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Li, Gang et al. published their research in European Journal of Medicinal Chemistry in 2020 | CAS: 214834-18-1

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of −48.7 × 10−6 cm3·mol−1.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·mol−1 in the liquid phase and 140.4 kJ·mol−1 in the gas phase. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Category: pyridine-derivatives

The optimization of xanthine derivatives leading to HBK001 hydrochloride as a potent dual ligand targeting DPP-IV and GPR119 was written by Li, Gang;Meng, Bingxu;Yuan, Baokun;Huan, Yi;Zhou, Tian;Jiang, Qian;Lei, Lei;Sheng, Li;Wang, Weiping;Gong, Ningbo;Lu, Yang;Ma, Chen;Li, Yan;Shen, Zhufang;Huang, Haihong. And the article was included in European Journal of Medicinal Chemistry in 2020.Category: pyridine-derivatives This article mentions the following:

A series of xanthine compounds derived from the previous hit I with modification on the terminal side chain was discovered through ring formation strategy. Systematic optimization of the compounds with rigid heterocycles in the hydrophobic side chain led to the new lead compound HBK001 (II) with the improved DPP-IV inhibition and moderate GPR119 agonism activity in vitro. As a continuing work to further study the PK and PD profiles, II and its hydrochloride (22) were synthesized on grams scale and evaluated on the ADME/T and oral glucose tolerance test (OGTT) in ICR mice. Compound 22 showed the improved bioavailability and blood glucose-lowering effect in vivo compared to its free base 21h probably attributed to its improved solubility and permeability. The preliminary toxicity studies on compound 22 exhibited that the result of mini-Ames was neg. and the preliminary acute toxicity LD50 in mice was above 1.5 g/kg, while it showed moderate inhibition on hERG channel with IC50 4.9μM maybe due to its high lipophilicity. These findings will be useful for the future drug design for more potent and safer dual ligand targeting DPP-IV and GPR119 for the treatment of diabetes. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1Category: pyridine-derivatives).

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine is diamagnetic and has a diamagnetic susceptibility of −48.7 × 10−6 cm3·mol−1.The molecular electric dipole moment is 2.2 debyes. The standard enthalpy of formation is 100.2 kJ·mol−1 in the liquid phase and 140.4 kJ·mol−1 in the gas phase. Reduced pyridines, namely tetrahydropyridines, dihydropyridines and piperidines, are found in numerous natural and synthetic compounds. The synthesis and reactivity of these compounds have often been driven by the fact many of these compounds have interesting and unique pharmacological properties. Category: pyridine-derivatives

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem

Ding, Chengrong et al. published their research in Youji Huaxue in 2020 | CAS: 214834-18-1

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Recommanded Product: tert-Butyl 4-carbamothioylpiperidine-1-carboxylate

Synthesis and biological activity of aryl thiazole piperidine amide compounds was written by Ding, Chengrong;Pan, Yayun;Tan, Chengxia. And the article was included in Youji Huaxue in 2020.Recommanded Product: tert-Butyl 4-carbamothioylpiperidine-1-carboxylate This article mentions the following:

In order to find a novel biol. active compound containing aromatic thiazole piperidine structure, 15 novel aryl thiazole piperidine amide derivatives were designed and synthesized. The structures of the target compounds were fully characterized by 1H NMR, 13C NMR and HRMS spectra. The bioactivity test showed that some target compounds had good fungicidal and insecticidal activity. For example, the inhibition rate of 5-(3-bromophenyl)-4-methyl-2-(1-((4-nitrophenyl) sulfonyl) piperidin-4-yl) thiazole (6b) shown in I against Pseudoperonospora cubensis was 100% better than azoxystrobin, and the inhibition rate of 5-(4-bromophenyl)-2-(1-((4-chlorophenyl) sulfonyl) piperidin-4-yl)-4-methylthiazole (6c) shown in II against Rhizoctonia solani was 58.86% comparable to azoxystrobin at 200μg/mL. The lethal rate of (4-(5-(3-bromophenyl)-4-methylthiazol-2-yl) piperidin-1-yl) (m-tolyl) methanone (6h) shown in III against Mythimna separata was 100% at 500μg/mL. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1Recommanded Product: tert-Butyl 4-carbamothioylpiperidine-1-carboxylate).

tert-Butyl 4-carbamothioylpiperidine-1-carboxylate (cas: 214834-18-1) belongs to pyridine derivatives. Pyridine has a dipole moment and a weaker resonant stabilization than benzene (resonance energy 117 kJ·mol−1 in pyridine vs. 150 kJ·mol−1 in benzene). Pyridine derivatives are also useful as small-molecule α-helix mimetics that inhibit protein-protein interactions, as well as functionally selective GABA ligands.Recommanded Product: tert-Butyl 4-carbamothioylpiperidine-1-carboxylate

Referemce:
Pyridine – Wikipedia,
Pyridine | C5H5N – PubChem