Category: 209919-30-2

Arvanitis, Argyrios G. published the artcileImidazo[4,5-c]pyridines as corticotropin releasing factor receptor ligands, SDS of cas: 209919-30-2, the publication is Bioorganic & Medicinal Chemistry Letters (2003), 13(1), 129-131, database is CAplus and MEDLINE.

A series of high affinity CRF receptor ligands, e.g., I, with an imidazo[4,5-c]pyridine core is described. Individual analogs were synthesized and tested in vitro in rat brain receptors to determine binding affinity. I was further tested in the dog N-in-1 pharmacokinetic model to assess oral bioavailability at 1 mg/kg po.

Bioorganic & Medicinal Chemistry Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, SDS of cas: 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Komatsu, Ryutaro published the artcileManipulating the Electronic Excited State Energies of Pyrimidine-Based Thermally Activated Delayed Fluorescence Emitters To Realize Efficient Deep-Blue Emission, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is ACS Applied Materials & Interfaces (2017), 9(5), 4742-4749, database is CAplus and MEDLINE.

The electronic excited state energies of pyrimidine-based TADF emitters were molecularly manipulated to realize deep-blue emission and reduced delayed fluorescent lifetime (τ_d). The authors then systematically studied the relations among the chem. structure, properties, and device performances. The resultant novel pyrimidine emitters, called Ac-XMHPMs (X = 1, 2, and 3), contain different numbers of bulky Me substituents at acceptor moieties, increasing the excited singlet (E_S) and triplet state (E_T) energies. Among them, Ac-3MHPM, with a high E_T of 2.95 eV, exhibited a high external quantum efficiency (η_ext,max) of 18% and an η_ext of 10% at 100 cd m^-2 with Commission Internationale de l’Eclairage chromaticity coordinates of (0.16, 0.15). These efficiencies are among the highest values to date for deep-blue TADF OLEDs. The mol. design strategy provides fundamental guidance to design novel deep-blue TADF emitters.

ACS Applied Materials & Interfaces published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Cross, R. Matthew published the artcileSynthesis, Antimalarial Activity, and Structure-Activity Relationship of 7-(2-Phenoxyethoxy)-4(1H)-quinolones, Computed Properties of 209919-30-2, the publication is Journal of Medicinal Chemistry (2011), 54(24), 8321-8327, database is CAplus and MEDLINE.

Me 6-butyl-2-methyl-4-oxo-7-(2-phenoxyethoxy)-1,4-dihydroquinoline-3-carboxylate (I, ICI 56,780) displayed causal prophylactic and blood schizonticidal activity (ED₅₀ = 0.05 mg/kg) in rodent malaria models but produced rapid acquisition of parasitol. resistance in P. berghei infected mice. Herein we describe the synthesis of analogs of I with EC₅₀ as low as 0.15 nM against multidrug resistant P. falciparum. Optimal activity with low cross-resistance indexes (RI) to atovaquone was achieved by introducing ortho-substituted aryl moieties at the 3-position of the 7-(2-phenoxyethoxy)-4(1H)-quinolone core.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Computed Properties of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Wagh, Ravindra B. published the artcileSilica chloride: An efficient promoter for oxidation of arylboronic acids to phenols, Quality Control of 209919-30-2, the publication is Tetrahedron Letters (2017), 58(33), 3323-3326, database is CAplus.

This work reports simple, highly efficient protocol for the oxidation of arylboronic acids. Various arylboronic acids were selectively and completely converted into their corresponding oxidized phenols using H₂O₂ as an oxidant in presence of catalytic amount of silica chloride. The results show that silica chloride is a suitable and efficient promoter for the oxidation of arylboronic acids. Heterogeneous catalyst, mild reaction conditions, easy availability of the reagent, easy work-up, excellent yield of corresponding phenols, short reaction time and broad substrate scope makes this protocol attractive and a practical alternative to the existing methods.

Tetrahedron Letters published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8FNO2S, Quality Control of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sambaiah, M. published the artcileTandem Schiff-Base Formation/Heterocyclization: An Approach to the Synthesis of Fused Pyrazolo-Pyrimidine/Isoxazolo-Pyrimidine Hybrids, Related Products of chlorides-buliding-blocks, the publication is Synlett (2019), 30(5), 586-592, database is CAplus.

A new synthesis of pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines was described. Key steps in the synthesis involve Stille coupling of 4,6-dichloro-2-phenyl-pyrimidine with tributyl(1-ethoxyvinyl)stannane and tandem Schiff-base formation/heterocyclization of 2,6-di-aryl-5-fluoro-4-acetylpyrimidine with hydrazines or hydroxylamine to give pyrazolo[4,3-d]pyrimidines and isoxazolo[4,5-d]pyrimidines, resp. The position of the fluoro group in the pyrimidine ring is important for the success of heterocyclization reaction.

Synlett published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Cross, R. Matthew published the artcileOptimization of 1,2,3,4-Tetrahydroacridin-9(10H)-ones as Antimalarials Utilizing Structure-Activity and Structure-Property Relationships, Synthetic Route of 209919-30-2, the publication is Journal of Medicinal Chemistry (2011), 54(13), 4399-4426, database is CAplus and MEDLINE.

Antimalarial activity of 1,2,3,4-tetrahydroacridin-9(10H)-ones (THAs) has been known since the 1940s and has garnered more attention with the development of the acridinedione floxacrine in the 1970s and analogs thereof such as WR 243251 in the 1990s. These compounds failed just prior to clin. development because of suboptimal activity, poor solubility, and rapid induction of parasite resistance. Moreover, detailed structure-activity relationship (SAR) studies of the THA core scaffold were lacking and SPR studies were nonexistent. To improve upon initial findings, several series of 1,2,3,4-tetrahydroacridin-9(10H)-ones were synthesized and tested in a systematic fashion, examining each compound for antimalarial activity, solubility, and permeability. Furthermore, a select set of compounds was chosen for microsomal stability testing to identify physicochem. liabilities of the THA scaffold. Several potent compounds (EC₅₀ < 100 nM) were identified to be active against the clin. relevant isolates W2 and TM90-C2B while possessing good physicochem. properties and little to no cross-resistance.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Synthetic Route of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Josa-Cullere, Laia published the artcileA Phenotypic Screen Identifies a Compound Series That Induces Differentiation of Acute Myeloid Leukemia Cells In Vitro and Shows Antitumor Effects In Vivo, Synthetic Route of 209919-30-2, the publication is Journal of Medicinal Chemistry (2021), 64(21), 15608-15628, database is CAplus and MEDLINE.

Induction of differentiation is a promising therapeutic strategy against acute myeloid leukemia. However, current differentiation therapies are effective only to specific patient populations. To identify novel differentiation agents with wider efficacy, authors developed a phenotypic high-throughput screen with a range of genetically diverse cell lines. From the resulting hits, one chem. scaffold was optimized in terms of activity and physicochem. properties to yield OXS007417 I, a proof-of-concept tool compound, which was also able to decrease tumor volume in a murine in vivo xenograft model.

Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Synthetic Route of 209919-30-2.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Sutherland, Hamish S. published the artcileSynthesis and structure-activity relationships for a new class of tetrahydronaphthalene amide inhibitors of Mycobacterium tuberculosis, Related Products of chlorides-buliding-blocks, the publication is European Journal of Medicinal Chemistry (2022), 114059, database is CAplus and MEDLINE.

Drug resistant tuberculsosis (TB) is global health crisis that demands novel treatment strategies. Bacterial ATP synthase inhibitors such as bedaquiline and next-generation analogs (such as TBAJ-876) have shown promising efficacy in patient populations and preclin. studies, resp., suggesting that selective targeting of this enzyme presents a validated therapeutic strategy for the treatment of TB. In this work, we report tetrahydronaphthalene amides (THNAs) as a new class of ATP synthase inhibitors that are effective in preventing the growth of Mycobacterium tuberculosis (M.tb) in culture. Design, synthesis and comprehensive structure-activity relationship studies for approx. 80 THNA analogs are described, with a small selection of compounds exhibiting potent (in some cases MIC90 <1 μg/mL) in vitro M.tb growth inhibition taken forward to pharmacokinetic and off-target profiling studies. Ultimately, we show that some of these THNAs possess reduced lipophilic properties, decreased hERG liability, faster mouse/human liver microsomal clearance rates and shorter plasma half-lives compared with bedaquiline, potentially addressing of the main concerns of persistence and phospholipidosis associated with bedaquiline.

European Journal of Medicinal Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C6H12Br2, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Chen, Shuqing published the artcileThe Discovery of a Palladium(II)-Initiated Borono-Catellani Reaction, Related Products of chlorides-buliding-blocks, the publication is Angewandte Chemie, International Edition (2018), 57(24), 7161-7165, database is CAplus and MEDLINE.

Reported is a novel palladium(II)-initiated Catellani-type reaction that uses widely accessible aryl boronic acids as the substrates instead of aryl halides, thereby greatly expanding the existing scope of this powerful transformation. This borono-Catellani reaction was promoted by cooperative catalysis between Pd(OAc)₂ and the inexpensive 5-norbornene-2-carbonitrile. Practicality is the striking feature of the reaction: it is run open to air at ambient temperature and no phosphine ligand is needed. This mild, chemoselective, and scalable protocol is compatible with a large range of readily available functionalized aryl boronic acids and bromides, as well as terminating olefins (50 examples, 39-97% yields). Moreover, the orthogonal reactivity between the borono-Catellani and classical Catellani reaction was demonstrated. This work is expected to open new avenues for developing novel Catellani-type reactions.

Angewandte Chemie, International Edition published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Related Products of chlorides-buliding-blocks.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics

Luan, Pengqian published the artcileAqueous chemoenzymatic one-pot enantioselective synthesis of tertiary α-aryl cycloketones via Pd-catalyzed C-C formation and enzymatic C=C asymmetric hydrogenation, Recommanded Product: 4-Chloro-2-methylphenylboronic acid, the publication is Green Chemistry (2021), 23(5), 1960-1964, database is CAplus.

An aqueous chemoenzymic cascade reaction combining Pd-catalyzed C-C formation and enzymic C=C asym. hydrogenation (AH) was developed for enantioselective synthesis of tertiary α-aryl cycloketones in good yields and excellent enantioselectivities. The stereopreference of the enzyme in AH of α-aryl cyclohexenones was studied. An enantiocomplementary enzyme was obtained by site-directed mutation.

Green Chemistry published new progress about 209919-30-2. 209919-30-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is 4-Chloro-2-methylphenylboronic acid, and the molecular formula is C7H8BClO2, Recommanded Product: 4-Chloro-2-methylphenylboronic acid.

Referemce:
https://en.wikipedia.org/wiki/Chloride,
Chlorides – an overview | ScienceDirect Topics