Tag: M.W=150-200

Yuan, Huihui published the artcileA solvent-free method for the preparation of phosphinates from P(O)-OH compounds with alkyl chlorides, Name: 3-Chlorobenzylchloride, the publication is Tetrahedron Letters (2021), 153529, database is CAplus.

Herein, a new solvent-free synthetic method using P(O)-OH compound and alkyl chloride for phosphinate compounds is disclosed. This transformation proceeds smoothly under the promotion of a lone base and presents the advantages of an easily available raw material source, a simple post treatment process, good functional group tolerance and high reaction efficiency. Good yield was obtained when the reaction was magnified to gram scale(coating), and the molar ratio of P(O)-OH compounds and alkyl chlorides can be decreased to 1:2. This protocol provides a practical method for the preparation of phosphorus derivatives Furthermore, the reaction mechanism was explored by ³¹P NMR.

Tetrahedron Letters published new progress about 620-20-2. 620-20-2 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Benzyl chloride,Benzene, name is 3-Chlorobenzylchloride, and the molecular formula is C9H13NO2, Name: 3-Chlorobenzylchloride.

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

Xu, Yanjun published the artcilePyridine derivatives(X): synthesis and herbicidal activities of 2-sec-butylamino-5-(2-aryloxy-4-pyridinyl)-4-yl)-1,3,4-thiadiazoles, Application of 2-Chloroisonicotinic acid, the publication is Nongyaoxue Xuebao (2007), 9(2), 189-192, database is CAplus.

A method for the synthesis of the title compounds [i.e., N-(1-methylpropyl)-5-[2-(phenoxy)-4-pyridinyl]-1,3,4-thiadiazol-2-amine derivatives] is reported here. 2-(Sec-butylamino)-5-(2-chloro-4-pyridinyl)-1,3,4-thiadiazole (BCPT) is a lead compound for herbicide development. In order to improve its herbicidal activity and study the relationship between chem. structure and bioactivity, an aryl ether moiety was introduced to the sketch. A new series of compounds was synthesized and the structures were confirmed by NMR and elementary anal. A preliminary bioassay showed that all the synthesized compounds showed a poor inhibition rate (0-45%) at 500 mg/L, much weaker than (BCPT) (72%-87%). A chloro-atom on the 2-position of pyridine ring may be indispensable for herbicidal activity.

Nongyaoxue Xuebao 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 C6H8O4, Application of 2-Chloroisonicotinic acid.

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

Zhu, Chen published the artcileMild and Rapid Hydroxylation of Aryl/Heteroaryl Boronic Acids and Boronate Esters with N-Oxides, Product Details of C7H8BClO2, the publication is Organic Letters (2012), 14(13), 3494-3497, database is CAplus and MEDLINE.

Aryl and heteroaryl boronic acids and boronate esters are rapidly, often within minutes, transformed into the corresponding phenols by N-oxides in an open flask at ambient temperature This transformation has broad compatibility with a variety of functional groups.

Organic 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 C6H10F3NO, Product Details of C7H8BClO2.

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

Wang, Shuai published the artcileStructure-Based Design, Synthesis, and Biological Evaluation of New Triazolo[1,5-a]Pyrimidine Derivatives as Highly Potent and Orally Active ABCB1 Modulators, Computed Properties of 939-99-1, the publication is Journal of Medicinal Chemistry (2020), 63(24), 15979-15996, database is CAplus and MEDLINE.

ABCB1 is a promising therapeutic target for overcoming multidrug resistance (MDR). In this work, we reported the structure-based design of triazolo[1,5-a]pyrimidines as new ABCB1 modulators, of which WS-691 significantly increased sensitization of ABCB1-overexpressed SW620/Ad300 cells to paclitaxel (PTX) (IC₅₀ = 22.02 nM). Mechanistic studies indicated that WS-691 significantly increased the intracellular concentration of PTX and [³H]-PTX while decreasing the efflux of [³H]-PTX in SW620/Ad300 cells by inhibiting the efflux function of ABCB1. The cellular thermal shift assay suggested that WS-691 could stabilize ABCB1 by directly binding to ABCB1. WS-691 could stimulate the activity of ABCB1 ATPase but had almost no inhibitory activity against CYP3A4. Importantly, WS-691 increased the sensitivity of SW620/Ad300 cells to PTX in vivo without observed toxicity. Collectively, WS-691(I) is a highly potent and orally active ABCB1 modulator capable of overcoming MDR. The triazolo[1,5-a]pyrimidine may be a promising scaffold for developing more potent ABCB1 modulators.

Journal of Medicinal 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 C13H10O3, Computed Properties of 939-99-1.

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

Christianson, D. D. published the artcileChromatography of quaternary nitrogen compounds on buffered cation-exchange resins, Application In Synthesis of 6249-56-5, the publication is Journal of Chromatography (1963), 432-8, database is CAplus and MEDLINE.

Betaines and other naturally occurring quaternary N compounds were detected and determined by a modification of the method of W., et al. (CA 54, 18198b) based on ultraviolet absorbance by their periodides. Columns used were uniformly sized, pulverized, sulfonated polystyrene resin, with Na citrate buffers of pH 2.2, 3.25, and 4.25 for elution. Better separation of betaine, stachydrine, choline, trigoneltine, N-methylnicotinamide, and carnitine was obtained with these eluents than with HCl because of greater differences in degrees of ionization in the buffer system. Corn-grain extracts were separated in 2 days into trigonelline, choline, and an unknown substance yielding a periodide derivative

Journal of Chromatography 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, Application In Synthesis of 6249-56-5.

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

Christianson, Donald D. published the artcileSeparation and determination of quaternary nitrogen compounds and other nitrogenous substances by ion-exchange chromatography. Application to analysis of corn extracts, HPLC of Formula: 6249-56-5, the publication is Anal. Chem. (1960), 874-8, database is CAplus.

cf. preceding abstract A known mixture of quaternary N compounds (q.n.c.) (including carnitine, choline, betaine, trigonelline, thiamine, γ-butyrobetaine, and stachydrine) and certain related amines and amino acids were separated on a column of the acid form of Dowex-50W with increasing concentrations of aqueous HCl as the eluant (CA 47, 11348i). Recovery was quant. for all q.n.c. except N-methylnicotinamide and ergothioneine. The procedure was applied to an aqueous concentrate from a 80% EtOH extraction of whole corn grain. From this were characterized and determined 3 of q.n.c., 16 amino acids and amides, and one purine. In order of decreasing amounts: asparagine, choline, alanine, and γ-aminobutyric acid were the major free N compounds found. Two of the substances, if not others, originally present in the corn extract were altered during the separation process by acid hydrolysis. It is suggested that this separation technique can be used to fractionate as little as 300 γ of each q.n.c. for routine analysis.

Anal. Chem. 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, HPLC of Formula: 6249-56-5.

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

Subasinghe, Nalin L. published the artcileA novel series of pyrazolylpiperidine N-type calcium channel blockers, HPLC of Formula: 871332-95-5, the publication is Bioorganic & Medicinal Chemistry Letters (2012), 22(12), 4080-4083, database is CAplus and MEDLINE.

Selective blockers of the N-type calcium channel have proven to be effective in animal models of chronic pain. However, even though intrathecally delivered synthetic ω-conotoxin MVIIA from Conus magnus (ziconotide [Prialt]) has been approved for the treatment of chronic pain in humans, its mode of delivery and narrow therapeutic window have limited its usefulness. Therefore, the identification of orally active, small-mol. N-type calcium channel blockers would represent a significant advancement in the treatment of chronic pain. A novel series of pyrazole-based N-type calcium channel blockers was identified by structural modification of a high-throughput screening hit and further optimized to improve potency and metabolic stability. In vivo efficacy in rat models of inflammatory and neuropathic pain was demonstrated by a representative compound from this series.

Bioorganic & Medicinal Chemistry Letters published new progress about 871332-95-5. 871332-95-5 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Nitrile,Boronic acid and ester,Benzene,Boronic Acids,Boronic acid and ester, name is (4-Chloro-3-cyanophenyl)boronic acid, and the molecular formula is C5H11NO2S, HPLC of Formula: 871332-95-5.

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

Pieroni, Marco published the artcileDesign, synthesis and investigation on the structure-activity relationships of N-substituted 2-aminothiazole derivatives as antitubercular agents, Name: 1-(4-Chlorophenyl)thiourea, the publication is European Journal of Medicinal Chemistry (2014), 26-34, database is CAplus and MEDLINE.

Tuberculosis (TB) is one of the deadliest infectious diseases of all times, and its recent resurgence is a supreme matter of concern. Co-infection with HIV and, in particular, the continuous isolation of new resistant strains, makes the discovery of novel anti-TB agents a strategic priority. The research of novel agents should be driven by the accessibility of the synthetic procedure and, in particular, by the lack of cross-resistance with the drugs already marketed. Moreover, in order to shorten the duration of the therapy, and therefore decrease the rate of resistance, these mols. should be active also against the nonreplicating persistent form (NRP-TB) of the infection. The availability of an inhouse small library of compounds prompted us to investigate their anti-TB activity. Two compounds, embodying a 2-aminothiazole scaffold, were found to possess a certain inhibitory activity toward Mycobacterium tuberculosis H₃₇Rv, and therefore a medicinal chem. campaign was initiated in order to increase the activity of the hit compounds and, especially, construct a plausible body of structure-activity relationships. The potency of the hit compound was successfully improved, and, much more importantly, some of the mols. synthesized were found to be active toward the persistent phenotype, and, also, toward a panel of resistant strains. These findings encourage further investigations around this interesting antitubercular chemotype.

European Journal of Medicinal Chemistry 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, Name: 1-(4-Chlorophenyl)thiourea.

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

Li, Xiuyun published the artcileSynthesis and fungicidal activities of biaryl methanone o-benzyl oximes, Product Details of C6H4ClNO2, the publication is Gaodeng Xuexiao Huaxue Xuebao (2015), 36(12), 2415-2420, database is CAplus.

To discover new strobilurin analogs with high pesticidal activity, 11 novel methoxy acrylates bearing biaryl methanone oxime ether moieties were synthesized from aroyl pyridines, and characterized by ¹H and ¹³C NMR and HRMS. In vitro fungicidal evaluation indicated that all of the target compounds exhibited excellent activities against tested seven phytopathogenic fungi, and compounds I (R = H, R₁ = 3-Cl-4-Me) and I (R = H, R₁ = 2,3-Cl)displayed comparable overall activities to azoxystrobin and trifloxystrobin. Some of the target compounds also exhibited excellent in vivo control effects at 400 mg/L, for example, compound I (R = H, R₁ = 4-t-Bu) could 100% control wheat powdery mildew and cucumber anthracnose. Furthermore, at 25 mg/L, these compounds, including control agents, completely inhibited spores germination of rice blast, but no effect at all for cucumber gray mold. These results suggested that this class of compounds might deserve to be developed as new potential agricultural fungicides.

Gaodeng Xuexiao Huaxue Xuebao 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, Product Details of C6H4ClNO2.

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

Chen, Suming published the artcileMass Spectrometry for Paper-Based Immunoassays: Toward On-Demand Diagnosis, SDS of cas: 6249-56-5, the publication is Journal of the American Chemical Society (2016), 138(20), 6356-6359, database is CAplus and MEDLINE.

Current anal. methods, either point-of-care or centralized detection, are not able to meet recent demands of patient-friendly testing and increased reliability of results. Here, the authors describe a two-point separation on-demand diagnostic strategy based on a paper-based mass spectrometry immunoassay platform that adopts stable and cleavable ionic probes as mass reporter; these probes make possible sensitive, interruptible, storable, and restorable on-demand detection. In addition, a new touch paper spray method was developed for on-chip, sensitive, and cost-effective analyte detection. This concept is successfully demonstrated via (i) the detection of Plasmodium falciparum histidine-rich protein 2 antigen and (ii) multiplexed and simultaneous detection of cancer antigen 125 and carcinoembryonic antigen.

Journal of the American Chemical Society 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, SDS of cas: 6249-56-5.

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