Tag: M.W=150-200

Scott, Fraser J. published the artcileAn evaluation of Minor Groove Binders as anti-Trypanosoma brucei brucei therapeutics, Quality Control of 64559-06-4, the publication is European Journal of Medicinal Chemistry (2016), 116-125, database is CAplus and MEDLINE.

A series of 32 structurally diverse MGBs, derived from the natural product distamycin, was evaluated for activity against Trypanosoma brucei brucei. Four compounds have been found to possess significant activity, in the nanomolar range, and represent hits for further optimization towards novel treatments for Human and Animal African Trypanosomiases. Moreover, SAR indicates that the head group linking moiety is a significant modulator of biol. activity.

European Journal of Medicinal Chemistry published new progress about 64559-06-4. 64559-06-4 belongs to amides-buliding-blocks, auxiliary class Amine,Benzene,Amide,Ether, name is 3-Methoxybenzothioamide, and the molecular formula is C14H21BO2, Quality Control of 64559-06-4.

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

Liu, Yang published the artcilePyridazinone derivatives displaying highly potent and selective inhibitory activities against c-Met tyrosine kinase, Application In Synthesis of 849833-86-9, the publication is European Journal of Medicinal Chemistry (2016), 322-333, database is CAplus and MEDLINE.

Over activation of c-Met tyrosine kinase is known to promote tumorigenesis and metastasis, as well as therapeutic resistance. Herein the authors describe the design, synthesis and biol. activities of novel, ATP-competitive, c-Met tyrosine kinase inhibitors that are members of the 6-aryl-2-(3-(heteroarylamino)benzyl)pyridazinone family. A structure-activity relationship (SAR) study of these substances led to identification of a pyridazinone derivative as a highly selective and potent c-Met tyrosine inhibitor, which displays favorable pharmacokinetic properties in mice and significant antitumor activity against a c-Met driven EBC-1 tumor xenograft. The synthesis of the target compounds was achieved using [(3-iodophenyl)methyl]-3-pyridazinone derivatives as key intermediates.

European Journal of Medicinal Chemistry published new progress about 849833-86-9. 849833-86-9 belongs to amides-buliding-blocks, auxiliary class Fluoride,Boronic acid and ester,Amine,Benzene,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester, name is (3-Fluoro-4-(methylcarbamoyl)phenyl)boronic acid, and the molecular formula is C8H9BFNO3, Application In Synthesis of 849833-86-9.

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

de Lipthay, Julia R. published the artcileBacterial diversity and community structure of a sub-surface aquifer exposed to realistic low herbicide concentrations, Synthetic Route of 2447-79-2, the publication is FEMS Microbiology Ecology (2004), 49(1), 59-69, database is CAplus and MEDLINE.

An increasing number of herbicides are found in our groundwater environments. This underlines the need for examining the effects of herbicide exposure on the indigenous groundwater microbial communities, as microbial degradation is the major process responsible for the complete removal of most contaminants. We examined the effect of in situ exposure to realistic low concentrations of herbicides on the microbial diversity and community structure of sub-surface sediments from a shallow aquifer near Vejen (Denmark). Three different community analyses were performed: colony morphol. typing, sole C source utilization in Biolog EcoPlates, and denaturing gradient gel electrophoresis. Cluster anal. demonstrated that the microbial communities of those aquifer sediments that acclimated to the herbicide exposure also had similar community structure. This observation was concurrent for all 3 community analyses. In contrast, no significant effect was found on the bacterial diversity, except for the culturable fraction where a significantly increased richness and Shannon index was found in the herbicide acclimated sediments. The results of this study show that in situ exposure of sub-surface aquifers to realistic low concentrations of herbicides may alter the overall structure of a natural bacterial community, although significant effects on the genetic diversity and C substrate usage cannot be detected. The observed impact was probably due to indirect effects. In future studies, the inclusion of methods that specifically detect relevant microbial sub-populations and functional genes is recommended.

FEMS Microbiology Ecology published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Synthetic Route of 2447-79-2.

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

Pierce, Arleen C. published the artcileAction of primary and secondary amines on trihalogenated esters, Application of N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Journal of Organic Chemistry (1963), 658-62, database is CAplus.

The reactions of a series of trichloro- and trifluoroacetates with primary and secondary amines were investigated at room temperature When the trichlorinated esters were treated with primary amines, acyl-oxygen cleavage occurred predominantly. A haloform-type cleavage took place when the same esters were treated with secondary amines. Trifluorinated esters were found to yield exclusively amides regardless of the amine used. In the trichloroacetate series the order of decreasing acyl-oxygen cleavage with BuNH₂ was found to be: PhO > CH₂:CHO > MeO equal or nearly equal to EtO > Me₃CO > PhCH₂O. When the same esters were treated with piperidine, the order of decreasing acyl-oxgyen cleavage was found to be: PhO > CH₂:CHO > CH₂:CHCH₂O equal or nearly equal to PhCH₂O > Me₃CO > MeO equal or nearly equal to EtO. Steric hindrance in both the ester and the amine influenced the type of cleavage that occurred. Solvents such as MeCN or dioxane increased the percent of haloform-type cleavage while CCl₄ induced exclusive acyl-oxygen cleavage. The infrared carbonyl stretching frequencies of all esters, amides, and carbamates prepared in this study were measured with a precision of ±2 cm^-1.

Journal of Organic Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Application of N,N-Diethyl-2,2,2-trifluoroacetamide.

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

Pierce, Arleen C. published the artcileReactions of trihalogenated esters with triethylamine and anions, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Journal of Organic Chemistry (1962), 3968-73, database is CAplus.

The reactions of several trihalogenated esters with triethylamine were studied at room temperature All the trihalogenated esters formed quaternary ammonium compounds with triethylamine. In the case of the trifluoro esters, the formation of N,N-diethyltrifluoroacetamide and an ether was a competing reaction. Amide formation was not observed for the tribromo and trichloro esters, at room temperature, but occurred with methyl thioltrichloroacetate. During this study it was observed that methyl trichloroacetate behaved as an alkylating agent toward sodium phenoxide, while ethyl trifluoroacetate behaved as an acylating agent. A significant feature of this work is the alkylating ability of alkyl trichloroacetates, at room temperature This property makes methyl trichloroacetate a potentially useful methylating agent to replace toxic compounds such as diazomethane or dimethyl sulfate.

Journal of Organic Chemistry published new progress about 360-92-9. 360-92-9 belongs to amides-buliding-blocks, auxiliary class Trifluoromethyl,Fluoride,Amine,Aliphatic hydrocarbon chain,Amide, name is N,N-Diethyl-2,2,2-trifluoroacetamide, and the molecular formula is C6H10F3NO, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide.

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

Broderius, Steven J. published the artcileUse of joint toxic response to define the primary mode of toxic action for diverse industrial organic chemicals, HPLC of Formula: 2447-79-2, the publication is Environmental Toxicology and Chemistry (1995), 14(9), 1591-605, database is CAplus.

We have explored the use of 96-h acute toxicity tests with juvenile fathead minnows and primarily binary chem. mixtures to define the primary acute mode of toxic action for diverse industrial organic chems. Our investigation mainly considered the two special cases of noninteractive joint action known as concentration (simple similar) and response (independent) addition The different forms of joint toxicity with binary mixtures were graphically illustrated by isobole diagrams. Designated as the mode of action-specific reference toxicants were 1-octanol, phenol, and 2,4-dinitrophenol. It was observed from binary isobole diagrams that a chem. with a similar primary mode of toxic action to that of a reference toxicant would display a concentration-addition type of joint action with the reference toxicant over the entire mixture ratio range. Dissimilar chems. with very steep concentration-response curves generally showed an interaction that was less-than-concentration additive, but consistently demonstrated a joint toxicity that was greater than predicted by the response-addition model. The more-than-concentration additive complex isoboles that are indicative of interactive toxicity were not commonly observed in our experiments

Environmental Toxicology and Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, HPLC of Formula: 2447-79-2.

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

Yakovleva, N. L. published the artcileReaction of carboxy-, carbethoxy-, and hydroxymethylpyridines with phosphorous amides, Safety of N,N-Diethylisonicotinamide, the publication is Khimiko-Farmatsevticheskii Zhurnal (1980), 14(1), 67-9, database is CAplus.

Heating nicotinic acid, isonicotinic acid or their Et esters with P(NEt₂)₃ gave 34.8-88% resp. diethylamides; yields were higher (88%, 79.5%) using the acids. Amines I and II were prepared in 21.5 and 14.8% yield resp. from the corresponding hydroxymethyl derivatives

Khimiko-Farmatsevticheskii Zhurnal published new progress about 530-40-5. 530-40-5 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N,N-Diethylisonicotinamide, and the molecular formula is C10H9NO, Safety of N,N-Diethylisonicotinamide.

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

Ghosh, Santanu published the artcileMetal-Free Thermal Activation of Molecular Oxygen Enabled Direct α-CH₂-Oxygenation of Free Amines, COA of Formula: C7H5Cl2NO, the publication is Journal of Organic Chemistry (2018), 83(1), 260-266, database is CAplus and MEDLINE.

Direct oxidation of α-CH₂ group of free amines is hard to achieve due to the higher reactivity of amine moiety. Therefore, oxidation of amines involves the use of sophisticated metallic reagents/catalyst in the presence or absence of hazardous oxidants under sensitive reaction conditions. A novel method for direct C-H oxygenation of aliphatic amines through a metal-free activation of mol. oxygen has been developed. Both activated and unactivated free amines were oxygenated efficiently to provide a wide variety of amides (primary, secondary) and lactams under operationally simple conditions without the aid of metallic reagents and toxic oxidants. The method has been applied to the synthesis of highly functionalized amide-containing medicinal drugs, such as O-Me-alibendol and -buclosamide.

Journal of Organic Chemistry published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, COA of Formula: C7H5Cl2NO.

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

Ghosh, Santanu published the artcileAminofluorene-Mediated Biomimetic Domino Amination-Oxygenation of Aldehydes to Amides, Application of 2,4-Dichlorobenzamide, the publication is Organic Letters (2016), 18(22), 5788-5791, database is CAplus and MEDLINE.

A conceptually novel biomimetic strategy based on a domino amination-oxygenation reaction was developed for direct amidation of aldehydes under metal-free conditions employing mol. oxygen as the oxidant. 9-Aminofluorene derivatives acted as pyridoxamine-5′-phosphate equivalent for efficient, chemoselective, and operationally simple amine-transfer oxygenation reaction. Unprecedented RNH transfer involving secondary amines to produce secondary amides was achieved. In the presence of ¹⁸O₂, ¹⁸O-amide was formed with excellent (95%) isotopic purity.

Organic Letters published new progress about 2447-79-2. 2447-79-2 belongs to amides-buliding-blocks, auxiliary class Chloride,Amine,Benzene,Amide, name is 2,4-Dichlorobenzamide, and the molecular formula is C7H5Cl2NO, Application of 2,4-Dichlorobenzamide.

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

Kim, Joong-Gon published the artcileA convenient one-pot method for the synthesis of N-methoxy-N-methyl amides from carboxylic acids, Synthetic Route of 100377-32-0, the publication is Bulletin of the Korean Chemical Society (2010), 31(1), 171-173, database is CAplus.

A mild and convenient 1-pot synthesis of Weinreb amides from carboxylates using Cl₃CCN and PPh₃ was developed. The process is general for the preparation of Weinreb amides from a variety of carboxylates. The reaction was also applicable to the preparation of α-amino Weinreb amides and proceeded without deprotection of the N-Fmoc protecting group or racemization.

Bulletin of the Korean Chemical Society published new progress about 100377-32-0. 100377-32-0 belongs to amides-buliding-blocks, auxiliary class Pyridine,Amine,Amide, name is N-Methoxy-N-methylisonicotinamide, and the molecular formula is C8H10N2O2, Synthetic Route of 100377-32-0.

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