Category: 144222-22-0

Jin, Tingting et al. published their research in ChemMedChem in 2021 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 144222-22-0

Design, Synthesis, and Biological Evaluation of Orally Bioavailable CHK1 Inhibitors Active against Acute Myeloid Leukemia was written by Jin, Tingting;Wang, Peipei;Long, Xiubing;Jiang, Kailong;Song, Pinrao;Wu, Wenbiao;Xu, Gaoya;Zhou, Yubo;Li, Jia;Liu, Tao. And the article was included in ChemMedChem in 2021.Recommanded Product: 144222-22-0 This article mentions the following:

Checkpoint kinase 1 (CHK1) is a central component in DNA damage response and has emerged as a target for antitumor therapeutics. Herein, we describe the design, synthesis, and biol. evaluation of a novel series of potent diaminopyrimidine CHK1 inhibitors. The compounds exhibited moderate to potent CHK1 inhibition and could suppress the proliferation of malignant hematol. cell lines. The optimized compound 13 had a CHK1 IC50 value of 7.73卤0.74 nM, and MV-4-11 cells were sensitive to it (IC50=0.035卤0.007渭M). Furthermore, compound 13 was metabolically stable in mouse liver microsomes in vitro and displayed moderate oral bioavailability in vivo. Moreover, treatment of MV-4-11 cells with compound 13 for 2 h led to robust inhibition of CHK1 autophosphorylation on serine 296. Based on these biochem. results, we consider compound 13 to be a promising CHK1 inhibitor and potential anticancer therapeutic agent. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Piperidine derivatives bearing a masked aldehyde function in the 蔚-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Kozlova, Arina et al. published their research in Journal of Medicinal Chemistry in 2021 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.HPLC of Formula: 144222-22-0

Rational Design of Original Fused-Cycle Selective Inhibitors of Tryptophan 2,3-Dioxygenase was written by Kozlova, Arina;Thabault, Leopold;Liberelle, Maxime;Klaessens, Simon;Prevost, Julien R. C.;Mathieu, Caroline;Pilotte, Luc;Stroobant, Vincent;Van den Eynde, Benoit;Frederick, Raphael. And the article was included in Journal of Medicinal Chemistry in 2021.HPLC of Formula: 144222-22-0 This article mentions the following:

Tryptophan 2,3-dioxygenase (TDO2) is a heme-containing enzyme constitutively expressed at high concentrations in the liver and responsible for L-tryptophan (L-Trp) homeostasis. Expression of TDO2 in cancer cells results in the inhibition of immune-mediated tumor rejection due to an enhancement of L-Trp catabolism via the kynurenine pathway. In the study herein, we disclose a new 6-(1H-indol-3-yl)-benzotriazole scaffold of TDO2 inhibitors developed through rational design, starting from existing inhibitors. Rigidification of the initial scaffold led to the synthesis of stable compounds displaying a nanomolar cellular potency and a better understanding of the structural modulations that can be accommodated inside the active site of hTDO2. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Several piperidine alkaloids isolated from natural herbs, were found to exhibit antiproliferation and antimetastatic effects on various types of cancers both in vitro and in vivo for example Piperine, Evodiamine, Matrine, Berberine and Tetrandine.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Rabal, Obdulia et al. published their research in Journal of Medicinal Chemistry in 2018 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives.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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0

Detailed Exploration around 4-Aminoquinolines Chemical Space to Navigate the Lysine Methyltransferase G9a and DNA Methyltransferase Biological Spaces was written by Rabal, Obdulia;Sanchez-Arias, Juan Antonio;San Jose-Eneriz, Edurne;Agirre, Xabier;de Miguel, Irene;Garate, Leire;Miranda, Estibaliz;Saez, Elena;Roa, Sergio;Martinez-Climent, Jose Angel;Liu, Yingying;Wu, Wei;Xu, Musheng;Prosper, Felipe;Oyarzabal, Julen. And the article was included in Journal of Medicinal Chemistry in 2018.Recommanded Product: 144222-22-0 This article mentions the following:

Epigenetic regulators that exhibit aberrant enzymic activities or expression profiles are potential therapeutic targets for cancers. Specifically, enzymes responsible for methylation at histone-3 lysine-9 (like G9a) and aberrant DNA hypermethylation (DNMTs) have been implicated in a number of cancers. Recently, mols. bearing a 4-aminoquinoline scaffold were reported as dual inhibitors of these targets and showed a significant in-vivo efficacy in animal models of hematol. malignancies. Here, we report a detailed exploration around three growing vectors born by this chemotype. Exploring this chem. space led to the identification of features to navigate G9a and DNMT1 biol. spaces; not only their corresponding exclusive areas, selective compounds, but also common spaces. Thus, we identified from selective G9a and first-in-class DNMT1 inhibitors, > 1 log unit between their IC50 values, with IC50 < 25nM (e.g. 43 and 26, resp.) to equipotent inhibitors with IC50 < 50nM for both targets (e.g. 13). Their ADME/Tox profiling and antiproliferative efficacies, vs. some cancer cell lines, are also reported. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Recommanded Product: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives.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. Piperidine derivatives are being utilized in different ways as anticancer, antiviral, antimalarial, antimicrobial, antifungal, antihypertension, analgesic, anti-inflammatory, anti-Alzheimer, antipsychotic and/or anticoagulant agents.Recommanded Product: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Gijsen, Harrie J. M. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.HPLC of Formula: 144222-22-0

5-Sulfonyl-benzimidazoles as selective CB2 agonists – Part 2 was written by Gijsen, Harrie J. M.;De Cleyn, Michel A. J.;Surkyn, Michel;Van Lommen, Guy R. E.;Verbist, Bie M. P.;Nijsen, Marjoleen J. M. A.;Meert, Theo;Van Wauwe, Jean;Aerssens, Jeroen. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.HPLC of Formula: 144222-22-0 This article mentions the following:

In a previous communication, the SAR of a series of potent and selective 5-sulfonylbenzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic stability. In this Letter, we report on further optimization of this series, leading to the relatively polar and peripherically acting CB2 agonists I and II. Although both compounds were not active in acute pain models, the less selective compound I displayed good, sustained activity in a chronic model of neuropathic pain without the tolerance observed with morphine. In addition, both I and II delayed the onset of clin. symptoms in an exptl. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Gijsen, Harrie J. M. et al. published their research in Bioorganic & Medicinal Chemistry Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.HPLC of Formula: 144222-22-0

5-Sulfonyl-benzimidazoles as selective CB2 agonists – Part 2 was written by Gijsen, Harrie J. M.;De Cleyn, Michel A. J.;Surkyn, Michel;Van Lommen, Guy R. E.;Verbist, Bie M. P.;Nijsen, Marjoleen J. M. A.;Meert, Theo;Van Wauwe, Jean;Aerssens, Jeroen. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2012.HPLC of Formula: 144222-22-0 This article mentions the following:

In a previous communication, the SAR of a series of potent and selective 5-sulfonylbenzimidazole CB2-receptor agonists was described. The lack of in vivo activity of compounds from this series was attributed to their poor solubility and metabolic stability. In this Letter, we report on further optimization of this series, leading to the relatively polar and peripherically acting CB2 agonists I and II. Although both compounds were not active in acute pain models, the less selective compound I displayed good, sustained activity in a chronic model of neuropathic pain without the tolerance observed with morphine. In addition, both I and II delayed the onset of clin. symptoms in an exptl. model for multiple sclerosis. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0HPLC of Formula: 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. Piperidine is a saturated organic heteromonocyclic parent, an azacycloalkane, a secondary amine and a member of piperidines. Fluorinated piperidines are also the subject of continued interest in medicinal chemistry, for example in the synthesis of selective dipeptidyl peptidase II (DPP II) inhibitors. Piperidine derivatives are also used in solid-phase peptide synthesis (SPPS) and many degradation reactions.HPLC of Formula: 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Chuckowree, Irina et al. published their research in Tetrahedron Letters in 2012 | CAS: 144222-22-0

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Related Products of 144222-22-0

Synthesis of a 1,3,5-benzotriazepine-2,4-dione based library was written by Chuckowree, Irina;Ali Syed, Murtaza;Getti, Giulia;Parbhu Patel, Asha;Garner, Hannah;Tizzard, Graham J.;Coles, Simon J.;Spencer, John. And the article was included in Tetrahedron Letters in 2012.Related Products of 144222-22-0 This article mentions the following:

A library of benzotriazepines has been synthesized employing microwave-mediated synthesis, supported resins and parallel synthesis methodol. In the experiment, the researchers used many compounds, for example, 1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0Related Products of 144222-22-0).

1-Boc-4-(Aminomethyl)piperidine (cas: 144222-22-0) belongs to piperidine derivatives. The piperidine moiety constitutes an important building block for the synthesis of a variety of bioactive natural products, alkaloids and other drugs. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Related Products of 144222-22-0

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

New learning discoveries about 144222-22-0

This compound(1-Boc-4-(Aminomethyl)piperidine)Application of 144222-22-0 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Application of 144222-22-0. So far, in addition to halogen atoms, other non-metallic atoms can become part of the aromatic heterocycle, and the target ring system is still aromatic. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Reductive Cross-Coupling between Unactivated C(aryl)-N and C(aryl)-O Bonds by Chromium Catalysis Using a Bipyridyl Ligand.

Reductive cross-coupling between two chem. inert bonds remains a great challenge in synthetic chem. We report here the reductive cross-coupling between unactivated C(aryl)-N and C(aryl)-O bonds that was achieved by chromium catalysis. The simple and inexpensive CrCl2 salt, combined with important bipyridyl ligand and magnesium reductant, shows high reactivity in the successive cleavage of C(aryl)-N bonds of aniline derivatives and C(aryl)-O bonds of aryl esters, allowing the cross-coupling of these two unactivated and different bonds to occur in a reductive fashion to form a C(aryl)-C(aryl) bond. Mechanistic studies by deuterium-labeling experiments indicate that the C(aryl)-N bonds in anilines are preferentially cleaved by reactive Cr species, in which the ligation of bipyridyl with Cr by adopting a coordination model in 1:1 ratio can be considered.

This compound(1-Boc-4-(Aminomethyl)piperidine)Application of 144222-22-0 was discussed at the molecular level, the effects of temperature and reaction time on the properties of the compound were discussed, and the optimum reaction conditions were selected.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Simple exploration of 144222-22-0

Different reactions of this compound(1-Boc-4-(Aminomethyl)piperidine)Synthetic Route of C11H22N2O2 require different conditions, so the reaction conditions are very important.

The three-dimensional configuration of the ester heterocycle is basically the same as that of the carbocycle. Compound: 1-Boc-4-(Aminomethyl)piperidine(SMILESS: NCC1CCN(C(OC(C)(C)C)=O)CC1,cas:144222-22-0) is researched.Safety of tert-Butyl ((1S,2S)-2-hydroxycyclohexyl)carbamate. The article 《Syntheses and Binding Testing of N1-Alkylamino-Substituted 2-Aminobenzimidazole Analogues Targeting the Hepatitis C Virus Internal Ribosome Entry Site*》 in relation to this compound, is published in Australian Journal of Chemistry. Let’s take a look at the latest research on this compound (cas:144222-22-0).

A series of 2-aminobenzimidazole analogs have been synthesized and tested for binding to a previously established RNA target for viral translation inhibitors in the internal ribosome entry site (IRES) of the hepatitis C virus (HCV). Synthesis of new inhibitor compounds followed a highly convergent strategy which allowed for incorporation of diverse tertiary amino substituents in high overall yields (eight-steps, 4-22%). Structure-activity relationship (SAR) studies focussed on the tertiary amine substituent involved in hydrogen bonding with the RNA backbone at the inhibitor binding site. The SAR study was further correlated with in silico docking experiments Analogous compounds showed promising activities (half maximal effective concentration, EC50: 21-89μM). Structures of the synthesized analogs and a correlation to their mode of binding, provided the opportunity to explore parameters required for selective targeting of the HCV IRES at the subdomain IIa which acts as an RNA conformational switch in HCV translation.

Different reactions of this compound(1-Boc-4-(Aminomethyl)piperidine)Synthetic Route of C11H22N2O2 require different conditions, so the reaction conditions are very important.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

The effect of the change of synthetic route on the product 144222-22-0

《Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(1-Boc-4-(Aminomethyl)piperidine)Product Details of 144222-22-0.

Epoxy compounds usually have stronger nucleophilic ability, because the alkyl group on the oxygen atom makes the bond angle smaller, which makes the lone pair of electrons react more dissimilarly with the electron-deficient system. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins.Product Details of 144222-22-0.

Pan-bromodomain and extra terminal domain (BET) inhibitors interact equipotently with the eight bromodomains of the BET family of proteins and have shown profound efficacy in a number of in vitro phenotypic assays and in vivo pre-clin. models in inflammation or oncol. A number of these inhibitors have progressed to the clinic where pharmacol.-driven adverse events have been reported. To better understand the contribution of each domain to their efficacy and improve their safety profile, selective inhibitors are required. This article discloses the profile of GSK046, also known as iBET-BD2(I), a highly selective inhibitor of the second bromodomains of the BET proteins that has undergone extensive pre-clin. in vitro and in vivo characterization.

《Design and Synthesis of a Highly Selective and In Vivo-Capable Inhibitor of the Second Bromodomain of the Bromodomain and Extra Terminal Domain Family of Proteins》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(1-Boc-4-(Aminomethyl)piperidine)Product Details of 144222-22-0.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

Fun Route: New Discovery of 144222-22-0

《Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(1-Boc-4-(Aminomethyl)piperidine)Related Products of 144222-22-0.

Related Products of 144222-22-0. The mechanism of aromatic electrophilic substitution of aromatic heterocycles is consistent with that of benzene. Compound: 1-Boc-4-(Aminomethyl)piperidine, is researched, Molecular C11H22N2O2, CAS is 144222-22-0, about Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors. Author is Plewe, Michael B.; Sokolova, Nadezda V.; Gantla, Vidyasagar Reddy; Brown, Eric R.; Naik, Shibani; Fetsko, Alexandra; Lorimer, Donald D.; Dranow, David M.; Smutney, Hayden; Bullen, Jameson; Sidhu, Rana; Master, Arshil; Wang, Junru; Kallel, E. Adam; Zhang, Lihong; Kalveram, Birte; Freiberg, Alexander N.; Henkel, Greg; McCormack, Ken.

We identified and explored the structure-activity-relationship (SAR) of an adamantane carboxamide chem. series of Ebola virus (EBOV) inhibitors. Selected analogs exhibited half-maximal inhibitory concentrations (EC50 values) of ~10-15 nM in vesicular stomatitis virus (VSV) pseudotyped EBOV (pEBOV) infectivity assays, low hundred nanomolar EC50 activity against wild type EBOV, aqueous solubility >20 mg/mL, and attractive metabolic stability in human and nonhuman liver microsomes. X-ray cocrystallog. characterizations of a lead compound with the EBOV glycoprotein (GP) established the EBOV GP as a target for direct compound inhibitory activity and further provided relevant structural models that may assist in identifying optimized therapeutic candidates.

《Discovery of Adamantane Carboxamides as Ebola Virus Cell Entry and Glycoprotein Inhibitors》 provides a strategy for the preparation of materials with excellent comprehensive properties, which is conducive to broaden the application field of this compound(1-Boc-4-(Aminomethyl)piperidine)Related Products of 144222-22-0.

Reference:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem