Category: 87120-72-7

The author of 《Identification of dihydrofuro[3,4-d]pyrimidine derivatives as novel HIV-1 non-nucleoside reverse transcriptase inhibitors with promising antiviral activities and desirable physicochemical properties》 were Kang, Dongwei; Zhang, Heng; Wang, Zhao; Zhao, Tong; Ginex, Tiziana; Luque, Francisco Javier; Yang, Yang; Wu, Gaochan; Feng, Da; Wei, Fenju; Zhang, Jian; De Clercq, Erik; Pannecouque, Christophe; Chen, Chin Ho; Lee, Kuo-Hsiung; Murugan, N. Arul; Steitz, Thomas A.; Zhan, Peng; Liu, Xinyong. And the article was published in Journal of Medicinal Chemistry in 2019. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate The author mentioned the following in the article:

To address drug resistance to HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs), a series of novel diarylpyrimidine (DAPY) derivatives targeting “”tolerant region I”” and “”tolerant region II”” of the NNRTIs binding pocket (NNIBP) were designed utilizing a structure-guided scaffold-hopping strategy. The dihydrofuro[3,4-d]pyrimidine derivatives I and II proved to be exceptionally potent against a wide range of HIV-1 strains carrying single NNRTI-resistant mutations (EC50 = 0.9-8.4 nM), which were remarkably superior to that of etravirine III. Meanwhile, both compounds exhibited comparable activities with III toward the virus with double mutations F227L+V106A and K103N+Y181C. Furthermore, the most active compound I showed favorable pharmacokinetic properties with an oral bioavailability of 30.96% and a half-life of 11.1 h, which suggested that I is worth further investigation as a novel NNRTI to circumvent drug resistance. In the experiment, the researchers used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Jin, Tingting; Xu, Lei; Wang, Peipei; Hu, Xiaobei; Zhang, Runyuan; Wu, Zhiqi; Du, Wenxin; Kan, Weijuan; Li, Kun; Wang, Chang; Zhou, Yubo; Li, Jia; Liu, Tao published an article in 2021. The article was titled 《Discovery and Development of a Potent, Selective, and Orally Bioavailable CHK1 Inhibitor Candidate: 5-((4-((3-Amino-3-methylbutyl)amino)-5-(trifluoromethyl)pyrimidin-2-yl)amino)picolinonitrile》, and you may find the article in Journal of Medicinal Chemistry.Electric Literature of C10H20N2O2 The information in the text is summarized as follows:

Checkpoint kinase 1 (CHK1) plays an important role in the DNA damage response pathway, being a potential anti-cancer drug target. In this study, we used a strategy for trifluoromethyl substitution to obtain orally bioavailable CHK1 inhibitors to overcome the limitations of lead compound 1, which can only be administered i.v. After detailed investigation, we identified compound 6c as an oral CHK1 inhibitor, which demonstrated a considerably higher plasma exposure in mice. Compound 6c also showed good kinase selectivity. Moreover, it exhibited a significant antiproliferative effect in MV-4-11 cells singly and a synergistic effect in combination with gemcitabine in HT-29, A549, and RPMI-8226 cells. Addnl., compound 6c could inhibit tumor growth in the MV-4-11 xenograft mouse model. The combination of 6c and gemcitabine exhibited synergistic effect in the HT-29 xenograft mouse model. Thus, compound 6c was found to be a selective and oral potential anticancer CHK1 inhibitor. After reading the article, we found that the author used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Electric Literature of C10H20N2O2)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Electric Literature of C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Kang, Dongwei; Sun, Yanying; Feng, Da; Gao, Shenghua; Wang, Zhao; Jing, Lanlan; Zhang, Tao; Jiang, Xiangyi; Lin, Hao; De Clercq, Erik; Pannecouque, Christophe; Zhan, Peng; Liu, Xinyong published an article in Journal of Medicinal Chemistry. The title of the article was 《Development of Novel Dihydrofuro[3,4-d]pyrimidine Derivatives as HIV-1 NNRTIs to Overcome the Highly Resistant Mutant Strains F227L/V106A and K103N/Y181C》.Product Details of 87120-72-7 The author mentioned the following in the article:

Here, we report the design, synthesis, structure-activity relationship studies, antiviral activity, enzyme inhibition, and druggability evaluation of dihydrofuro[3,4-d]pyrimidine derivatives as a potent class of HIV-1 non-nucleoside reverse transcriptase inhibitors (NNRTIs). Compounds 14b (I) (EC50 = 5.79-28.3 nM) and 16c (II) (EC50 = 2.85-18.0 nM) exhibited superior potency against a panel of HIV-1-resistant strains. Especially, for the changeling mutations F227L/V106A and K103N/Y181C, both compounds exhibited remarkably improved activity compared to those of etravirine and rilpivirine. Moreover, 14b and 16c showed moderate RT enzyme inhibition (IC50 = 0.14-0.15 μM), which demonstrated that they acted as HIV-1 NNRTIs. Furthermore, 14b and 16c exhibited favorable pharmacokinetic and safety properties, making them excellent leads for further development. After reading the article, we found that the author used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Product Details of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Milder oxidation, using reagents such as NaOCl, can remove four hydrogen atoms from primary amines of the type RCH2NH2 to form nitriles (R―C≡N), and oxidation with reagents such as MnO2 can remove two hydrogen atoms from secondary amines (R2CH―NHR′) to form imines (R2C=NR′). Tertiary amines can be oxidized to enamines (R2C=CHNR2) by a variety of reagents.Product Details of 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Recommanded Product: 87120-72-7In 2021 ,《2,4,5-Trisubstituted Pyrimidines as Potent HIV-1 NNRTIs: Rational Design, Synthesis, Activity Evaluation, and Crystallographic Studies》 appeared in Journal of Medicinal Chemistry. The author of the article were Kang, Dongwei; Ruiz, Francesc X.; Sun, Yanying; Feng, Da; Jing, Lanlan; Wang, Zhao; Zhang, Tao; Gao, Shenghua; Sun, Lin; De Clercq, Erik; Pannecouque, Christophe; Arnold, Eddy; Zhan, Peng; Liu, Xinyong. The article conveys some information:

There is an urgent unmet medical need for novel human immunodeficiency virus type 1 (HIV-1) inhibitors that are effective against a variety of NNRTI-resistance mutations. We report our research efforts aimed at discovering a novel chemotype of anti-HIV-1 agents with improved potency against a variety of NNRTI-resistance mutations in this paper. Structural modifications of the lead K-5a2 led to the identification of a potent inhibitor 16c. 16c yielded highly potent anti-HIV-1 activities and improved resistance profiles compared with the approved drug etravirine. The co-crystal structure revealed the key role of the water networks surrounding the NNIBP for binding and for resilience against resistance mutations, while suggesting further extension of 16c toward the NNRTI-adjacent site as a lead development strategy. Furthermore, 16c demonstrated favorable pharmacokinetic and safety properties, suggesting the potential of 16c as a promising anti-HIV-1 drug candidate. The experimental process involved the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Recommanded Product: 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Recommanded Product: 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Electric Literature of C10H20N2O2In 2022 ,《Exploratory studies on soluble small molecule CD4 mimics as HIV entry inhibitors》 appeared in Bioorganic & Medicinal Chemistry. The author of the article were Tsuji, Kohei; Kobayakawa, Takuya; Konno, Kiju; Masuda, Ami; Takahashi, Kohei; Ohashi, Nami; Yoshimura, Kazuhisa; Kuwata, Takeo; Matsushita, Shuzo; Harada, Shigeyoshi; Tamamura, Hirokazu. The article conveys some information:

Several small mol. CD4 mimics, which inhibit the interaction of gp120 with CD4, have been developed. Original CD4 mimics such as NBD-556, which has an aromatic ring, an oxalamide linker and a piperidine moiety, possess significant anti-HIV activity but with their hydrophobic aromatic ring-containing structures are poorly soluble in water. We have developed derivatives with a halopyridinyl group in place of the Ph group, such as KKN-134, and found them to have excellent aqueous solubility Other leads that were examined are YIR-821, a compound with a cyclohexane group in a spiro attachment to a piperidine ring and a guanidino group on the piperidine nitrogen atom, and its PEGylated derivative, TKB-002. YIR-821 and TKB-002 retain potent anti-HIV activity. Here, new CD4 mimics, in which the Ph group was replaced by a halopyridinyl group with the halogen atoms in different positions, their derivatives without a cyclohexane group on the piperidine ring and their hybrid mols. with PEG units were designed and synthesized. Some of these compounds show significantly higher aqueous solubility with maintenance of certain levels of anti-HIV activity. The present data should be useful in the future design of CD4 mimic mols. The experimental process involved the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Electric Literature of C10H20N2O2)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Electric Literature of C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

《Structure-Based Bioisosterism Yields HIV-1 NNRTIs with Improved Drug-Resistance Profiles and Favorable Pharmacokinetic Properties》 was written by Kang, Dongwei; Feng, Da; Sun, Yanying; Fang, Zengjun; Wei, Fenju; De Clercq, Erik; Pannecouque, Christophe; Liu, Xinyong; Zhan, Peng. Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylateThis research focused onthiophenepyrimidine piperidine substituted preparation antiHIV activity. The article conveys some information:

The development of efficacious NNRTIs for AIDS therapy commonly encountered the rapid generation of drug-resistant mutations, which becomes a major impediment to effective anti-HIV treatment. Using a structure-based bioisosterism strategy, a series of piperidine-substituted thiophene[2,3-d]pyrimidine derivatives were designed and synthesized. Compound I yielded the greatest potency, exhibiting significantly better anti-HIV-1 activity than ETR against all of the tested NNRTI-resistant HIV-1 strains. In addition, the phenotypic (cross)resistance of I and other NRTIs to the different selected HIV-1 strains was evaluated. As expected, no phenotypic cross-resistance against the NRTIs (AZT and PMPA) was observed with the mutant Ires strain. Furthermore, I was identified with improved solubility, lower CYP liability, and hERG inhibition. Remarkably, I exhibited optimal pharmacokinetic properties in rats (F = 37.06%) and safety in mice (LD50 > 2000 mg/kg), which highlights I as a promising anti-HIV-1 drug candidate. After reading the article, we found that the author used tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Quality Control of tert-Butyl 4-aminopiperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

The author of 《Structure overhaul affords a potent purine PI3Kδ inhibitor with improved tolerability》 were Methot, Joey L.; Zhou, Hua; Kattar, Sam D.; McGowan, Meredeth A.; Wilson, Kevin; Garcia, Yudith; Deng, Yongi; Altman, Michael; Fradera, Xavier; Lesburg, Charles; Fischmann, Thierry; Li, Chaomin; Alves, Steve; Shah, Sanjiv; Fernandez, Rafael; Goldenblatt, Peter; Hill, Armetta; Shaffer, Lynsey; Chen, Dapeng; Tong, Vince; McLeod, Robbie L.; Yu, Hongshi; Bass, Alan; Kemper, Ray; Gatto, Nicholas T.; LaFranco-Scheuch, Lisa; Trotter, Benjamin Wesley; Guzi, Timothy; Katz, Jason D.. And the article was published in Journal of Medicinal Chemistry in 2019. Product Details of 87120-72-7 The author mentioned the following in the article:

PI3Kδ catalytic activity is required for immune cell activation, and has been implicated in inflammatory diseases as well as hematol. malignancies in which the AKT pathway is overactive. A purine PI3Kδ inhibitor bearing a benzimidazolone-piperidine motif was found to be poorly tolerated in dog, which was attributed to diffuse vascular injury. Several strategies were implemented to mitigate this finding, including reconstruction of the benzimidazolone-piperidine selectivity motif. Structure-based design led to the identification of O- and N-linked heterocycloalkyls, with pyrrolidines being particularly ligand efficient and kinome selective, and having an improved safety pharmacol. profile. A representative was advanced into a dog tolerability study where it was found to be well tolerated, with no histopathol. evidence of vascular injury. In the experiment, the researchers used many compounds, for example, tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Product Details of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Large quantities of aliphatic amines are made synthetically. The most widely used industrial method is the reaction of alcohols with ammonia at a high temperature, catalyzed by metals or metal oxide catalysts (e.g., nickel or copper). Mixtures of primary, secondary, and tertiary amines are thereby produced.Product Details of 87120-72-7

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Nguyen, Huy H.; Tahirovic, Yesim A.; Truax, Valarie M.; Wilson, Robert J.; Jecs, Edgars; Miller, Eric J.; Kim, Michelle B.; Akins, Nicholas S.; Xu, Lingjie; Jiang, Yi; Wang, Tao; Sum, Chi S.; Cvijic, Mary E.; Schroeder, Gretchen M.; Wilson, Lawrence J.; Liotta, Dennis C. published an article in 2021. The article was titled 《Amino-Heterocycle Tetrahydroisoquinoline CXCR4 Antagonists with Improved ADME Profiles via Late-Stage Buchwald Couplings》, and you may find the article in ACS Medicinal Chemistry Letters.COA of Formula: C10H20N2O2 The information in the text is summarized as follows:

This work surveys a variety of diamino-heterocycles as an isosteric replacement for the piperazine substructure of our previously disclosed piperarinyl-tetrahydroisoquinoline containing CXCR4 antagonists. A late-stage Buchwald coupling route was developed for rapid access to final compounds from com. building blocks. Among 13 analogs in this study, compound 31 (I) embodying an aza-piperazine linkage was found to have the best overall profile with potent CXCR4 inhibitory activity and favorable in vitro absorption, distribution, metabolism, and excretion (ADME) properties. An anal. of the calculated physiochem. parameters (ROF, cLogD) and the exptl. ADME attributes of the analogs lead to the selection of 31 for pharmacokinetic studies in mice. Compared with the clin. compound AMD11070, compound 31 has no CYP450 3A4 or 2D6 inhibition, higher metabolic stability and PAMPA permeability, greatly improved physiochem. parameters, and superior oral bioavailability (%F = 24). A binding rationale for 31 within CXCR4 was elucidated from docking and mol. simulation studies. The experimental process involved the reaction of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7COA of Formula: C10H20N2O2)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) 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).COA of Formula: C10H20N2O2

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

In 2022,Xu, Xi; Chang, Xiujin; Huang, Jingxuan; Zhang, Di; Wang, Min; Jing, Tian; Zhuang, Yu; Kou, Junping; Qiu, Zhixia; Wang, Jubo; Li, Zhiyu; Bian, Jinlei published an article in European Journal of Medicinal Chemistry. The title of the article was 《Discovery of novel glutaminase 1 allosteric inhibitor with 4-piperidinamine linker and aromatic heterocycles》.Related Products of 87120-72-7 The author mentioned the following in the article:

Glutaminase 1 (GLS1) is overexpressed in multiple types of malignant tumors and is viewed as a promising target in cancer therapy. Thus, the discovery for small-mol. GLS1 inhibitors is urgent. Based on the authors’ previous study of compound I, a potent GLS1 allosteric inhibitor yet with a limited metabolic stability, a structure-based optimization was carried out, with a series of novel GLS1 allosteric inhibitors rationally designed, synthesized and biol. evaluated. Such endeavor has culminated in the identification of compound II, a promising GLS1 allosteric inhibitor with a 4-piperidinamine linker and aromatic heterocycles. Compound II displayed robust GLS1 binding affinity, superior liver microsome metabolic stability, and moderate anti-tumor activity (TGI: 47.5%) in HCT116 xenograft model with no considerable toxicity in vivo. The mechanism underlying the anti-proliferative effect of compound II on HCT116 cells was studied, revealing that the compound blocked the glutamine metabolism, induced the production of ROS, and triggered apoptosis. These findings merit further investigation of compound II as a targeted cancer therapeutic. The experimental part of the paper was very detailed, including the reaction process of tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7Related Products of 87120-72-7)

tert-Butyl 4-aminopiperidine-1-carboxylate(cas: 87120-72-7) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Related Products of 87120-72-7

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