Category: 882033-93-4

Synthesis and in vitro characterization of trans- and cis-[¹⁸F]-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoropiperidine-1-carboxylates as new potential PET radiotracer candidates for the NR2B subtype N-methyl-D-aspartate receptor was written by Koudih, Radouane;Gilbert, Gwenaelle;Dhilly, Martine;Abbas, Ahmed;Barre, Louisa;Debruyne, Daniele;Sobrio, Franck. And the article was included in European Journal of Medicinal Chemistry in 2012.SDS of cas: 882033-93-4 The following contents are mentioned in the article:

Diastereoisomeric compounds [¹⁸F]cis- and [¹⁸F]trans-4-methylbenzyl 4-[(pyrimidin-2-ylamino)methyl]-3-fluoro-piperidine-1-carboxylates I were successfully synthesized as new subtype-selective PET radiotracers for imaging the NR2B subunit containing NMDA receptors. Rat brain section autoradiogs. demonstrated a high specific binding in NR2B/NMDA receptor rich regions for both radioligands. The measured logD_7.4 values as well as B_max/K_d ratios indicated that both radiotracers possess the adequate properties required for PET radiotracers. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4SDS of cas: 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) 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. 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.SDS of cas: 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Discovery of SARxxxx92, a pan-PIM kinase inhibitor, efficacious in a KG1 tumor model was written by Barberis, Claude;Erdman, Paul;Czekaj, Mark;Fire, Luke;Pribish, James;Tserlin, Elina;Maniar, Sachin;Batchelor, Joseph D.;Liu, Jinyu;Patel, Vinod F.;Hebert, Andrew;Levit, Mikhail;Wang, Anlai;Sun, Frank;Huang, Shih-Min A.. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2020.Product Details of 882033-93-4 The following contents are mentioned in the article:

N-substituted azaindoles were discovered as potent pan-PIM inhibitors. Lead optimization, guided by structure and focused on physico-chem. properties allowed us to solve inherent hERG and permeability liabilities, and provided compound I, which subsequently impacted KG-1 tumor growth in a mouse model. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4Product Details of 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) 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. 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.Product Details of 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Synthesis and SAR of substituted tetrahydrocarbazole derivatives as new NPY-1 antagonists was written by Di Fabio, Romano;Giovannini, Riccardo;Bertani, Barbara;Borriello, Manuela;Bozzoli, Andrea;Donati, Daniele;Falchi, Alessandro;Ghirlanda, Damiano;Leslie, Colin P.;Pecunioso, Angelo;Rumboldt, Giovanna;Spada, Simone. And the article was included in Bioorganic & Medicinal Chemistry Letters in 2006.Product Details of 882033-93-4 The following contents are mentioned in the article:

The SAR of a new series of tetrahydrocarbazole derivatives I [R¹ = Me, 3-(1-piperidinyl)propyl, piperidin-4-ylmethyl, etc.; R² = H, 4-morpholinyl, 1-piperidinyl, 4-methyl-1-piperazinyl, etc.] is evaluated: the appropriate decoration of this template led to the identification of a new class of NPY-1 antagonists showing good in vitro potency and a promising in vivo pharmacokinetic profile in rat. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4Product Details of 882033-93-4).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) 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. Some chemotherapeutic agents have piperidine moiety within their structure, foremost among them, vinblastine and raloxifene.Product Details of 882033-93-4

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

Radiolabelling of 1,4-disubstituted 3-[¹⁸F]fluoropiperidines and its application to new radiotracers for NR2B NMDA receptor visualization was written by Koudih, Radouane;Gilbert, Gwenaelle;Dhilly, Martine;Abbas, Ahmed;Barre, Louisa;Debruyne, Daniele;Sobrio, Franck. And the article was included in Organic & Biomolecular Chemistry in 2012.Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate The following contents are mentioned in the article:

In order to develop a novel and useful building block for the development of radiotracers for positron emission tomog. (PET), we studied the radiolabelling of 1,4-disubstituted 3-[¹⁸F]fluoropiperidines. Indeed, 3-fluoropiperidine became a useful building block in medicinal chem. for the pharmacomodulation of piperidine-containing compounds The radiofluorination was studied on substituted piperidines with electron-donating and electron-withdrawing N-substituents. In the instance of electron-donating N-substituents such as benzyl or Bu, configuration retention and satisfactory fluoride-18 incorporation yields up to 80% were observed In the case of electron-withdrawing N-substituents leading to carbamate or amide functions, the incorporation yields depend on the 4-susbtitutent (2 to 63%). The radiolabelling of this building block was applied to the automated radiosynthesis of NR2B NMDA receptor antagonists and effected by a com. available radiochem. module. The in vivo evaluation of three radiotracers demonstrated minimal brain uptakes incompatible with the imaging of NR2B NMDA receptors in the living brain. Nevertheless, moderate radiometabolism was observed and, in particular, no radiodefluorination was observed which demonstrates the stability of the 3-position of the fluorine-18 atom. In conclusion, the 1,4-disubstituted 3-[¹⁸F]fluoropiperidine moiety could be of value in the development of other radiotracers for PET even if the evaluation of the NR2B NMDA receptor antagonists failed to demonstrate satisfactory properties for PET imaging of this receptor. This study involved multiple reactions and reactants, such as (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate).

(3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate (cas: 882033-93-4) 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. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising α-glucosidase inhibitors. The former are analogs of DNJ with an improved α-glucosidase inhibitory profile than that of DNJ. Boisson et al.Safety of (3S,4R)-rel-tert-Butyl 3-fluoro-4-(hydroxymethyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem