Category: 160296-40-2

Shaw, Simon J. et al. published their research in Bioorganic & Medicinal Chemistry in 2022 | CAS: 160296-40-2

tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate (cas: 160296-40-2) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Safety of tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate

Structure activity relationships leading to the identification of the indirect activator of AMPK, R419 was written by Shaw, Simon J.;Goff, Dane A.;Carroll, David C.;Singh, Rajinder;Sweeny, David J.;Park, Gary;Jenkins, Yonchu;Markovtsov, Vadim;Sun, Tian-Qiang;Issakani, Sarkiz D.;Hitoshi, Yasumichi;Payan, Donald G.. And the article was included in Bioorganic & Medicinal Chemistry in 2022.Safety of tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate This article mentions the following:

Using an in-cell AMPK activation assay, we have developed structure-activity relationships around a hit pyridine dicarboxamide 5 that resulted in 40 (R419). A particular focus was to retain the on-target potency while also improving microsomal stability and reducing off-target activities, including hERG inhibition. We were able to show that removing a tertiary amino group from the piperazine unit of hit compound 5 improved microsomal stability while hERG inhibition was improved by modifying the substitution of the central core pyridine ring. The SAR resulted in 40, which continues to maintain on-target potency. Compound 40 was able to activate AMPK in vivo after oral administration and showed efficacy in animal models investigating activation of AMPK as a therapy for glucose control (both db/db and DIO mouse models). In the experiment, the researchers used many compounds, for example, tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate (cas: 160296-40-2Safety of tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate).

tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate (cas: 160296-40-2) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. The piperidine and polyhydroxylated indolizidine derivatives have shown to be promising 伪-glucosidase inhibitors. The former are analogs of DNJ with an improved 伪-glucosidase inhibitory profile than that of DNJ. Boisson et al.Safety of tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

 

New learning discoveries about 160296-40-2

The synthetic route of 160296-40-2 has been constantly updated, and we look forward to future research findings.

160296-40-2, tert-Butyl 4-(4-fluorobenzoyl)piperidine-1-carboxylate is a piperidines compound, ?involved in a variety of chemical synthesis. Rlated chemical reaction is continuously updated

60% Sodium hydride (717mg, [18MMOL)] was suspended in anhydrous dimethylformamide [(50ML)] under nitrogen at [5C.] To this was added portion-wise 6-bromo naphthalene-2-thiol (3.89g, 16mmol). The mixture was stirred at [5C] for 30 minutes. 1- (t- [BUTOXYCARBONYL)-4- (4-FLUOROBENZOYL) PIPERIDINE] (Reference Example 12; [5.] 00g 16mmol) was then added to the solution and the reaction heated at [60C] for 16 hours. The solution was poured into water [(75ML)] and washed with EtOAc [(2X75ML).] The organic phases were combined then washed with water then brine. The solution was dried over MgS04, after filtration and evaporation a solid was isolated. This was recrystallised from EtOAc/isohexane resulting in a cream solid (2.96g, 35%). NMR (DMSO-d6) 1.37 (s, [11H),] 1.72 (m, 2H), 2.86 (m, 2H), 3.52 (m, 1H), 3.92 (m, 2H), 7.31 (d, 2H), 7.55 (d, 1H), 7.69 (d, 1H), 7.93 (m, 4H), 8.17 (s, 1H), 8.26 (s, 1H) ; m/z 470., 160296-40-2

The synthetic route of 160296-40-2 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; ASTRAZENECA AB; ASTRAZENECA UK LIMITED; WO2004/33427; (2004); A1;,
Piperidine – Wikipedia
Piperidine | C5H11N – PubChem