Category: 2382-10-07 00:00:00

Singh, Baljinder; Diaz-Gonzalez, Rosario; Ceballos-Perez, Gloria; Rojas-Barros, Domingo I.; Gunaganti, Naresh; Gillingwater, Kirsten; Martinez-Martinez, Maria Santos; Manzano, Pilar; Navarro, Miguel; Pollastri, Michael P. published the artcile< Medicinal Chemistry Optimization of a Diaminopurine Chemotype: Toward a Lead for Trypanosoma brucei Inhibitors>, HPLC of Formula: 2382-10-7, the main research area is diaminopurine chemotype optimization preparation Trypanosoma brucei structure.

Human African trypanosomiasis (HAT), or sleeping sickness, is caused by the protozoan parasite Trypanosoma brucei and transmitted through the bite of infected tsetse flies. The disease is considered fatal if left untreated. To identify new chemotypes against Trypanosoma brucei, previously we identified 797 potent kinase-targeting inhibitors grouped into 59 clusters plus 53 singleton compounds with at least 100-fold selectivity over HepG2 cells. From this set of hits, a cluster of diaminopurine-derived compounds was identified. Herein, we report our medicinal chem. investigation involving the exploration of structure-activity and structure-property relationships around one of the high-throughput screening (HTS) hits, N2-(thiophen-3-yl)-N6-(2,2,2-trifluoroethyl)-9H-purine-2,6-diamine (1, NEU-1106). This work led to the identification of a potent lead compound (4aa, NEU-4854) with improved in vitro absorption, distribution, metabolism, and excretion (ADME) properties, which was progressed into proof-of-concept translation of in vitro antiparasitic activity to in vivo efficacy.

Journal of Medicinal Chemistry published new progress about Pharmacokinetics. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, HPLC of Formula: 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lai, Xiao-Li; Shu, Xiao-Min; Song, Jinshuai; Xu, Hai-Chao published the artcile< Electrophotocatalytic Decarboxylative C-H Functionalization of Heteroarenes>, Application In Synthesis of 2382-10-7, the main research area is electrophotocatalyst decarboxylative heteroarene functionalization; C−H functionalization; electrochemistry; heterocycles; photocatalysis; radical reactions.

Decarboxylative C-H functionalization reactions are highly attractive methods for forging carbon-carbon bonds considering their inherent step- and atom-economical features and the pervasiveness of carboxylic acids and C-H bonds. An ideal approach to achieve these dehydrogenative transformations is through hydrogen evolution without using any chem. oxidants. However, effective couplings by decarboxylative carbon-carbon bond formation with proton reduction remain an unsolved challenge. Herein, the authors report an electrophotocatalytic approach that merges organic electrochem. with photocatalysis to achieve the efficient direct decarboxylative C-H alkylation and carbamoylation of heteroaromatic compounds through hydrogen evolution. This electrophotocatalytic method, which combines the high efficiency and selectivity of photocatalysis in promoting decarboxylation with the superiority of electrochem. in effecting proton reduction, enables the efficient coupling of a wide range of heteroaromatic bases with a variety of carboxylic acids and oxamic acids. Advantageously, this method is scalable to decagram amounts, and applicable to the late-stage functionalization of drug mols.

Angewandte Chemie, International Edition published new progress about Alkylation. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Application In Synthesis of 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Kos, Nico J.; Van der Plas, Henk C. published the artcile< Deamination of 6-amino- and 6-(alkylamino)-9-alkylpurines and demethylation of methylthiopurines by sodium in liquid ammonia>, Electric Literature of 2382-10-7, the main research area is deamination aminopurine alkylaminopurine; demethylation methylthiopurine; mercaptopurine; purine amino deamination.

Treating 6-aminopurines, e.g. I (R = NH2; R1 = H, Cl, MeO) or 6-(alkylamino)purines, e.g. I (R = MeNH, NMe2, R1 = H) with Na in NH3(l) gave deaminated products I (R = H) via 1,6-dihydropurine intermediates II. Na in NH3(l) was also used to demethylate 6- and 8-(methylthio)purines, e.g., III (R2 = MeS) to give thiols, e.g. III (R2 = SH).

Journal of Organic Chemistry published new progress about Deamination. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Electric Literature of 2382-10-7.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Roggen, Heidi; Gundersen, Lise-Lotte published the artcile< Synthetic studies directed towards agelasine analogs - synthesis, tautomerism, and alkylation of 2-substituted N-methoxy-9-methyl-9H-purin-6-amines>, Application of C6H4Cl2N4, the main research area is agelasine analog synthetic study; methoxypurinamine preparation regioselective alkylation; benzylmethoxyamino purine preparation; regioselectivity alkylation methoxypurinamine; tautomer ratio methoxypurinamine.

Methoxypurinamines I [R = H, Me, F3C, Cl, O2N; R1 = (MeO)NH], potential intermediates in the preparation of agelasine analogs, are prepared by substitution of I (R1 = Cl) with O-methylhydroxylamine hydrochloride, while I [R = MeO, EtO, Me2N, MeNH; R1 = (MeO)NH] are prepared by substitution reactions of I [R = Cl; R1 = (MeO)NH]. I [R = H, Me, MeO, EtO, MeNH; R1 = (MeO)NH] exist as mixtures of their methoxyamino and methoxyimino tautomers in solution, with the relative concentrations of the tautomers differing substantially between species. Alkylation of I [R = H, Me, MeO, EtO, Me2N, MeNH; R1 = (MeO)NH] with benzyl bromide gives mixtures of purinium bromides II (R = H, Me, EtO, Me2N, MeNH) and (benzylmethoxyamino)purines I [R = H, Me, MeO, EtO, Me2N, MeNH; R1 = (PhCH2)(MeO)N], while methoxypurinamines with strongly electron-withdrawing substituents are not reactive under similar conditions.

European Journal of Organic Chemistry published new progress about Alkylation. 2382-10-7 belongs to class chlorides-buliding-blocks, and the molecular formula is C6H4Cl2N4, Application of C6H4Cl2N4.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics