Category: 651057-01-1

An Old Story in the Parallel Synthesis World: An Approach to Hydantoin Libraries was written by Bogolubsky, Andrey V.;Moroz, Yurii S.;Savych, Olena;Pipko, Sergey;Konovets, Angelika;Platonov, Maxim O.;Vasylchenko, Oleksandr V.;Hurmach, Vasyl V.;Grygorenko, Oleksandr O.. And the article was included in ACS Combinatorial Science in 2018.Recommanded Product: 1-(Methylsulfonyl)piperidin-4-amine hydrochloride This article mentions the following:

An approach to the parallel synthesis of hydantoin libraries by reaction of in situ generated 2,2,2-trifluoroethylcarbamates and 浼?amino esters was developed. To demonstrate utility of the method, a library of 1158 hydantoins designed according to the lead-likeness criteria (MW 200-350, cLogP 1-3) was prepared The success rate of the method was analyzed as a function of physicochem. parameters of the products, and it was found that the method can be considered as a tool for lead-oriented synthesis. A hydantoin-bearing submicromolar primary hit acting as an Aurora kinase A inhibitor was discovered with a combination of rational design, parallel synthesis using the procedures developed, in silico and in vitro screenings. In the experiment, the researchers used many compounds, for example, 1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1Recommanded Product: 1-(Methylsulfonyl)piperidin-4-amine hydrochloride).

1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1) 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 浼?glucosidase inhibitors. The former are analogs of DNJ with an improved 浼?glucosidase inhibitory profile than that of DNJ. Boisson et al.Recommanded Product: 1-(Methylsulfonyl)piperidin-4-amine hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

6-Benzhydryl-4-amino-quinolin-2-ones as Potent Cannabinoid Type 1 (CB₁) Receptor Inverse Agonists and Chemical Modifications for Peripheral Selectivity was written by Zhang, Yue-Mei;Greco, Michael N.;Macielag, Mark J.;Teleha, Christopher A.;DesJarlais, Renee L.;Tang, Yuting;Ho, George;Hou, Cuifen;Chen, Cailin;Zhao, Shuyuan;Kauffman, Jack;Camacho, Raul;Qi, Jenson;Murray, William;Demarest, Keith;Leonard, James. And the article was included in Journal of Medicinal Chemistry in 2018.Application In Synthesis of 1-(Methylsulfonyl)piperidin-4-amine hydrochloride This article mentions the following:

A novel series of 6-benzhydryl-4-amino-quinolin-2-ones was discovered as cannabinoid type 1 receptor (CB₁R) inverse agonists based on the high-throughput screening hit, compound 1a. Structure-activity relationships were studied to improve in vitro/in vivo pharmacol. and restrict distribution to the peripheral circulation. We adopted several strategies such as increasing topol. polar surface area, incorporating discrete polyethylene glycol side chains, and targeting P-glycoprotein (P-gp) to minimize access to the brain. Compound 6a is a P-gp substrate and a potent and highly selective CB₁R inverse agonist, demonstrating excellent in vivo metabolic stability and a low brain to plasma ratio. However, brain receptor occupancy studies showed that compound 6a may accumulate in brain with repeat dosing. This was evidenced by compound 6a inhibiting food intake and inducing weight loss in diet-induced obese mice. Thus, a strategy based on P-gp efflux may not be adequate for peripheral restriction of the disclosed quinolinone series. In the experiment, the researchers used many compounds, for example, 1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1Application In Synthesis of 1-(Methylsulfonyl)piperidin-4-amine hydrochloride).

1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1) belongs to piperidine derivatives. The piperidine structural motif is present in numerous natural alkaloids. These include piperine, which gives black pepper its spicy taste. Piperidine derivatives bearing a masked aldehyde function in the ε-position are easily transformed into quinolizidine compounds through intramolecular reductive amination.Application In Synthesis of 1-(Methylsulfonyl)piperidin-4-amine hydrochloride

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem

A radical chlorodifluoromethylation protocol for late-stage difluoromethylation and its application to an oncology candidate was written by Meng, Depei;Li, Lingchun;Brown, Adam;Desrosiers, Jean-Nicolas;Duan, Shengquan;Hayward, Cheryl M.;He, Zhengbiao;Hu, Jinbo;Makowski, Teresa;Maloney, Mark;Monfette, Sebastien;Perfect, Hahdi;Piper, Jared L.;Zhou, Min;Widlicka, Daniel W.. And the article was included in Cell Reports Physical Science in 2021.Related Products of 651057-01-1 This article mentions the following:

An efficient radical chlorodifluoromethylation protocol with sodium chlorodifluoromethanesulfinate, which is complementary to the existing late-stage difluoromethylation strategies has been described. CF₂Cl radical is a suitable surrogate for accessing the CF₂H group while possessing completely different electronic properties compared to the CF₂H radical. This method is chemoselective and regioselective for the chlorodifluoromethylation of (hetero)arenes RH [R = 2,4,6-trimethylphenyl, 2,3-dihydro-1,4-benzodioxin-5-yl, 4-oxo-1H,4H,5H-pyrazolo[3,4-d]pyrimidin-3-yl, etc.] and electron-rich alkenes R¹C(=CH₂)OAc (R¹ = Ph, 2-naphthyl, 2-thienyl, etc.) and shows good functionality, tolerance, and generality on scope. The preparation of the sodium chlorodifluoromethanesulfinate is thoroughly investigated and can be scaled up to hundreds of kilograms. The method is successfully implemented on the synthesis of an oncol. candidate compound I. In the experiment, the researchers used many compounds, for example, 1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1Related Products of 651057-01-1).

1-(Methylsulfonyl)piperidin-4-amine hydrochloride (cas: 651057-01-1) belongs to piperidine derivatives. Piperidine and its derivatives have become increasingly popular in many synthetic schemes. Industrially, piperidine is produced by the hydrogenation of pyridine, usually over a molybdenum disulfide catalyst. Pyridine can also be reduced to piperidine via a modified Birch reduction using sodium in ethanol.Related Products of 651057-01-1

Referemce:
Piperidine – Wikipedia,
Piperidine | C5H11N – PubChem