Tag: M.W=150-200

Burkhard, C. A. published the artcileAlkylation of hydrochlorosilanes, Computed Properties of 14799-94-1, the publication is Journal of the American Chemical Society (1947), 2687-9, database is CAplus.

HSiCl₃ adds with ease to olefinic double bonds in the presence of peroxides or ultraviolet light; the reaction appears to proceed exclusively by the addition of the SiH bond. In general, 0.5 or 0.75 mole olefin was used with 1 mole of the chlorosilane and 0.013-0.026 mole of peroxide (30% Ac₂O₂ in o-C₆H₄(CO₂Me)₂ used unless otherwise indicated); this mixture was heated 4-24 hrs. at 70-100°. 1-Pentene and HSiCl₃ give 73% AmSiCl₃, b. 166-9°, and MeHSiCl₂ gives 37% pentylmethyldichlorosilane, b. 164-8°. 2-Pentene and MeHSiCl₂ give 71% 2-pentylmethyldichlorosilane, b₁₀₀ 100°. Cyclohexene and HSiCl₃ give 64% cyclohexyltrichlorosilane, b. 199°; iso-C₄H₈ and HSiCl₃ (tert-Bu perbenzoate as catalyst) give iso-BuSiCl₃, b. 136°. CH₂:CHSiCl₃ (I) and HSiCl₃ give 19% (CH₂SiCl₃)₂, b. 199°; this results in 3% yield from C₂H₂ (Bz₂O₂ as catalyst), I being postulated as an intermediate. CH₂:CHCH₂SiCl₃ and HSiCl₃ give 83% 1,3-bis(trichlorosilyl)propane, b₂₀ 111°. HSiCl₃ (135 g.) and 78 g. uninhibited PhCH:CH₂, heated 4 hrs. at 100°, give 70 g. of a glassy solid; alc.-NaOH gives no H, indicating that Si-C bonds had been formed.

Journal of the American Chemical Society published new progress about 14799-94-1. 14799-94-1 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Dichloro(hexyl)(methyl)silane, and the molecular formula is C7H16Cl2Si, Computed Properties of 14799-94-1.

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

Nagaraju, Tumula published the artcilePhI(OAc)₂-Mediated Regioselective Synthesis of 5-Guanidino-1,2,4-thiadiazoles and 1,2,4-Triazolo[1,5-a]pyridines via Oxidative N-S and N-N Bond Formation, HPLC of Formula: 3696-23-9, the publication is Synthesis (2019), 51(19), 3600-3610, database is CAplus.

An effective and expeditious approach for the construction of biol. important 5-guanidino-1,2,4-thiadiazoles I [R¹ = n-Pr, Ph, 3-ClC₆H₄, etc.; R² = Ph, 2-MeOC₆H₄, 4-ClC₆H₄, etc.] and 1,2,4-triazolo[1,5- a]pyridine derivatives II [R³ = H, 7-Me, 7-Cl; R⁴ = Ph, 2-thienyl, 3-O₂NC₆H₄, etc.] were developed with high efficiency and excellent regioselectivity. This new protocol involved the phenyliodine(III) diacetate-mediated oxidative cyclization of thioureas/2-aminopyridines and imidates via N-S and N-N bond formation at ambient temp to afford target compounds I and II resp.

Synthesis published new progress about 3696-23-9. 3696-23-9 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Thiourea,Amine,Benzene,Amide, name is 1-(4-Chlorophenyl)thiourea, and the molecular formula is C7H7ClN2S, HPLC of Formula: 3696-23-9.

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

Makane, Vitthal B. published the artcileSynthesis and evaluation of α-aminoacyl amides as antitubercular agents effective on drug resistant tuberculosis, Name: 2-Chloroisonicotinic acid, the publication is European Journal of Medicinal Chemistry (2019), 665-677, database is CAplus and MEDLINE.

Synthesis, SAR and evaluation of α-aminoacyl amides R¹C(O)N(R²)CH(R³)C(O)NHR⁴ [R¹ = 2-pyrrolyl, 2-furyl, 2-thienyl, etc.; R² = Ph, 4-MeC₆H₄, 2-HOC₆H₄, etc.; R³ = Ph, 3-ClC₆H₄, 4-MeOC₆H₄, etc.; R⁴ = t-Bu, cyclohexyl, Bn, 2-naphthyl] as antitubercular agents were reported via Ugi reaction of benzaldehydes, isocyanides, anilines and carboxylic acids. The systematic medicinal chem. approach led to identification of optimal substitutions required for the activity. Compound R¹C(O)N(R²)CH(R³)C(O)NHR⁴ [R¹ = 2,4-di-methylthiazol-5-yl; R² = 2,4-di-MeC₆H₃; R³ = 3-pyridyl; R⁴ = cyclohexyl] was identified as antitubercular lead with drug like properties. Further, R¹C(O)N(R²)CH(R³)C(O)NHR⁴ [R¹ = 2,4-di-methylthiazol-5-yl; R² = 2,4-di-MeC₆H₃; R³ = 3-pyridyl; R⁴ = cyclohexyl] selectively inhibited M. tuberculosis H37Rv with MIC value of 0.78 μM and was found to be non-toxic to CHO-K1 cells. The lead compound inhibited multi drug resistant and Pre-Extensively drug resistant strains of Mycobacterium at 2 μg/mL and 8 μg/mL resp.

European Journal of Medicinal Chemistry published new progress about 6313-54-8. 6313-54-8 belongs to chlorides-buliding-blocks, auxiliary class Pyridine,Chloride,Carboxylic acid, name is 2-Chloroisonicotinic acid, and the molecular formula is C6H4ClNO2, Name: 2-Chloroisonicotinic acid.

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

Saini, Parul published the artcileExternal Catalyst-Free Oxidation of Benzyl Halides to Benzoic Acids Using NaOH/TBHP in Water, Recommanded Product: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Asian Journal of Organic Chemistry (2021), 10(9), 2355-2359, database is CAplus.

An efficient and metal-free methodol. for the oxidation of benzyl halides to benzoic acids using an inexpensive and green oxidant (TBHP) in aqueous basic medium has been developed. This protocol offers an excellent way to avoid adding catalysts and involves the use of an in-situ generated halide ion as catalyst. It is also the first report on the oxidation of benzyl iodides to benzoic acids. A series of carboxylic acids were prepared from benzyl halides in high yields under mild reaction conditions by this method which does not require chromatog. purification Gram scale reactions for the synthesis of the carboxylic acids in good yields have been successfully carried out using benzyl chloride, bromide and iodide. As an industrial application, the synthesis of a key monomer used for the synthesis of polyethylene terephthalate (PET), i. e., terephthalic acid (PTA), has also been accomplished in good yields.

Asian Journal of Organic Chemistry published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C8H6ClF3, Recommanded Product: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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

Eckstein, Aleksandra published the artcileAuxin and chloroplast movements, Name: 3-Chloro-4-hydroxyphenylacetic acid, the publication is Physiologia Plantarum (2016), 156(3), 351-366, database is CAplus and MEDLINE.

Auxin is involved in a wide spectrum of physiol. processes in plants, including responses controlled by the blue light photoreceptors phototropins: phototropic bending and stomatal movement. However, the role of auxin in phototropin-mediated chloroplast movements has never been studied. To address this question we searched for potential interactions between auxin and the chloroplast movement signaling pathway using different exptl. approaches and two model plants, Arabidopsis thaliana and Nicotiana tabacum. We observed that the disturbance of auxin homeostasis by shoot decapitation caused a decrease in chloroplast movement parameters, which could be rescued by exogenous auxin application. In several cases, the impairment of polar auxin transport, by chem. inhibitors or in auxin carrier mutants, had a similar neg. effect on chloroplast movements. This inhibition was not correlated with changes in auxin levels. Chloroplast relocations were also affected by the antiauxin p-chlorophenoxyisobutyric acid and mutations in genes encoding some of the elements of the SCF^TIR1-Aux/IAA auxin receptor complex. The observed changes in chloroplast movement parameters are not prominent, which points to a modulatory role of auxin in this process. Taken together, the obtained results suggest that auxin acts indirectly to regulate chloroplast movements, presumably by regulating gene expression via the SCF^TIR1-Aux/IAA-ARF pathway. Auxin does not seem to be involved in controlling the expression of phototropins.

Physiologia Plantarum published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, Name: 3-Chloro-4-hydroxyphenylacetic acid.

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

Takahashi, Hidehiko published the artcileRelation between the hypotensive activity and chemical structure of γ-aminobutyric acid in the rabbit, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, the publication is Japan. J. Physiol. (1962), 97-105, database is CAplus.

γ-Aminobutyric acid applied intrathecalty gave a stronger and longer depressor response than that given intravenously. Me esters and N-substitution of γ-aminobutyric acid gave little response when applied intrathecally.

Japan. J. Physiol. published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C18H19ClN4, Application of 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride.

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

Ogris, Manfred published the artcileNovel biocompatible cationic copolymers based on polyaspartylhydrazide being potent as gene vector on tumor cells, COA of Formula: C7H16ClNO2, the publication is Pharmaceutical Research (2007), 24(12), 2213-2222, database is CAplus and MEDLINE.

The reaction between α,β-poly(aspartylhydrazide) (PAHy), a water soluble synthetic polymer and 3-(carboxypropyl)trimethyl-ammonium chloride (CPTACl) produced copolymers bearing permanent pos. charges (PAHy-CPTA) with mol. weight of 10 kDa and PAHy-CPTA copolymers differing in pos. charge amount (18-58%) were chosen for biol. investigations. Biophys. properties of DNA/PAHy-CPTA polyplexes were evaluated in terms of DNA condensation, zeta potential and size distribution. Cytotoxicity studies on Neuro2A murine neuroblastoma cells evidenced absence of toxicity of these copolymers up to 300 μg/mL unlike linear polyethylenimine (LPEI) that was highly toxic already at 20 μg/mL. PAHy-CPTA copolymers did not induce any erythrocyte aggregation up to 1 mg/mL. Cellular interaction studies of PAHy-CPTA polyplexes evidenced a faster binding of these polyplexes with cells compared to DNA/LPEI polyplexes. The in vitro transfection ability of PAHy-CPTA polyplexes was strongly affected by exptl. conditions reaching about 10% of the transfection efficiency of optimized LPEI polyplexes. Finally, in vivo application studies confirmed the biocompatibility of PAHy-CPTA copolymers. With LPEI, clear signs of microvesicular fatty liver were observed and with LPEI polyplexes significant weight loss. In strong contrast, PAHy-CPTA did not induce histopathol. changes or weight loss.

Pharmaceutical Research published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C7H16ClNO2, COA of Formula: C7H16ClNO2.

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

Gee, Clifford T. published the artcileFragment Screening and Druggability Assessment for the CBP/p300 KIX Domain through Protein-Observed ¹⁹F NMR Spectroscopy, COA of Formula: C8H7ClO3, the publication is Angewandte Chemie, International Edition (2015), 54(12), 3735-3739, database is CAplus and MEDLINE.

¹⁹F NMR spectroscopy of labeled proteins is a sensitive method for characterizing structure, conformational dynamics, higher-order assembly, and ligand binding. Fluorination of aromatic side chains has been suggested as a labeling strategy for small-mol. ligand discovery for protein-protein interaction interfaces. Using a model transcription factor binding domain of the CREB binding protein (CBP)/p300, KIX, we report the first full small-mol. screen using protein-observed ¹⁹F NMR spectroscopy. Screening of 508 compounds and validation by ¹H-¹⁵N HSQC NMR spectroscopy led to the identification of a minimal pharmacaphore for the MLL-KIX interaction site. Hit rate anal. for the CREB-KIX and MLL-KIX sites provided a metric to assess the ligandability or “druggability” of each interface informing future medicinal chem. efforts. The structural information from the simplified spectra and data collection speed, affords a new screening tool for anal. of protein interfaces and discovery of small mols.

Angewandte Chemie, International Edition published new progress about 33697-81-3. 33697-81-3 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Benzene,Phenol, name is 3-Chloro-4-hydroxyphenylacetic acid, and the molecular formula is C8H7ClO3, COA of Formula: C8H7ClO3.

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

Tosi, Umberto published the artcileReal-Time, in Vivo Correlation of Molecular Structure with Drug Distribution in the Brain Striatum Following Convection Enhanced Delivery, Computed Properties of 6249-56-5, the publication is ACS Chemical Neuroscience (2019), 10(5), 2287-2298, database is CAplus and MEDLINE.

The blood-brain barrier (BBB) represents a major obstacle in delivering therapeutics to brain lesions. Convection-enhanced delivery (CED), a method that bypasses the BBB through direct, cannula-mediated drug delivery, is one solution to maintaining increased, effective drug concentration at these lesions. CED was recently proven safe in a phase I clin. trial against diffuse intrinsic pontine glioma (DIPG), a childhood cancer. Unfortunately, the exact relationship between drug size, charge, and pharmacokinetic behavior in the brain parenchyma are difficult to observe in vivo. PET imaging of CED-delivered agents allows us to determine these relationships. In this study, we label different modifications of the PDGFRA inhibitor dasatinib with fluorine-18 or via a nanofiber-zirconium-89 system so that the effect of drug structure on post-CED behavior can accurately be tracked in vivo, via PET. Relatively unchanged bioactivity is confirmed in patient- and animal-model-derived cell lines of DIPG. In naïve mice, significant individual variability in CED drug clearance is observed, highlighting a need to accurately understand drug behavior during clin. translation. Generally, the half-life for a drug to clear from a CED site is short for low mol. weight dasatinib analogs that bare different charge; 1-3 (1, 32.2 min (95% CI: 27.7-37.8), 2, 44.8 min (27.3-80.8), and 3, 71.7 min (48.6-127.6) minutes) and is much longer for a dasatinib-nanofiber conjugate, 5, (42.8-57.0 days). Positron emission tomog. allows us to accurately measure the effect of drug size and charge in monitoring real-time drug behavior in the brain parenchyma of live specimens.

ACS Chemical Neuroscience published new progress about 6249-56-5. 6249-56-5 belongs to chlorides-buliding-blocks, auxiliary class Phase Transfer Catalyst,Inhibitor,Natural product, name is 3-Carboxy-N,N,N-trimethylpropan-1-aminium chloride, and the molecular formula is C18H10, Computed Properties of 6249-56-5.

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

Struwe, Julia published the artcilePhoto-Induced Ruthenium-Catalyzed C-H Benzylations and Allylations at Room Temperature, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene, the publication is Chemistry – A European Journal (2021), 27(65), 16237-16241, database is CAplus and MEDLINE.

The ruthenium-catalyzed synthesis of diarylmethane compounds was realized under exceedingly mild photoredox conditions without the use of exogenous photocatalysts. The versatility and robustness of the ruthenium-catalyzed C-H benzylation was reflected by an ample scope, including multifold C-H functionalizations, as well as transformable pyrazoles, imidates and sensitive nucleosides. Mechanistic studies were indicative of a photoactive cyclometalated ruthenium complex, which also enabled versatile C-H allylations.

Chemistry – A European Journal published new progress about 939-99-1. 939-99-1 belongs to chlorides-buliding-blocks, auxiliary class Fluoride,Chloride,Benzyl chloride,Benzene, name is 1-(Chloromethyl)-4-(trifluoromethyl)benzene, and the molecular formula is C17H14O5, Name: 1-(Chloromethyl)-4-(trifluoromethyl)benzene.

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