Tag: M.W=150-200

Rao, G. Venkateswara published the artcilePreferential reactivity of pyridylmagnesium chloride with N,N-dialkyl arylamides over carbonitriles: synthesis of 2-(aroyl) pyridines, COA of Formula: C10H14N2O, the publication is Synthetic Communications (2009), 39(10), 1835-1846, database is CAplus.

Reaction of 2-pyridylmagnesium chlorides with N,N-dialkyl arylamides afford exclusively 2-(aroyl)pyridines in high yields and purity without the formation of any tertiary alc. This method employs easily available raw materials and avoids the use of hazardous lithium reagents and cryogenic conditions. Further, preferential reactivity of this Grignard reagent with N,N-dialkyl arylamides over its carbonitrile counterparts offers a variety of 2-(aroyl)pyridines including the ones containing carbonitrile groups on the aryl ring.

Synthetic Communications 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 C10H14N2O, COA of Formula: C10H14N2O.

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

Admans, Gary published the artcileArtificial neural network for predicting the toxicity of organic molecules, COA of Formula: C7H5Cl2NO, the publication is Bulletin of the Chemical Society of Japan (2001), 74(12), 2451-2461, database is CAplus.

Structure-activity relationships for aquatic toxicity were studied using neural networks and linear regression anal. The structural features contributing to toxicity were identified in mols. exhibiting a level of toxicity greater than that of non-reactive organic mols. A neural network was trained for the toxicity of non-polar narcotics, polar narcotics, or reactive toxicants. Quant. structure-activity relationships (QSARs) were developed, relating a mol. aquatic toxicity to its log P and to a set of 16 structural descriptors based upon the presence of selected structural features. The inclusion of these structural descriptors into a QSAR was found to enhance the correlation of the equation, and thus to improve its ability for predicting aquatic toxicity.

Bulletin of the Chemical Society of Japan 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

Forbus, T. R. Jr. published the artcileReactions of the readily accessible electrophile, trifluoroacetyl triflate: a very reactive agent for trifluoroacetylations at oxygen, nitrogen, carbon, or halogen centers, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Journal of Organic Chemistry (1987), 52(19), 4156-9, database is CAplus.

Trifluoroacetyl triflate (I) is readily prepared in 82% yield by the dehydration (P₂O₅) of a 2:1 mixture of CF₃CO₂H and CF₃SO₃H. Reactions of this highly electrophilic trifluoroacetylating reagent with alcs., ketones, ethers, amines, and pyridines give esters, enol esters, ether cleavage, amides, and acylpyridinium ions, resp. Reactions with ionic or easily ionizable alkyl halides give the very volatile trifluoroacetyl halides and the ionic triflate. Triphenylmethyl chloride, for example, is quant. converted to triphenylcarbenium triflate in a very convenient synthetic procedure. I is used in the synthesis of the first member of a new class of pyrylium salts, 2,6-dimethoxypyrylium triflate.

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

Li, Hao published the artcileEfficient Synthesis of 1,9-Substituted Benzo[h][1,6]naphthyridin-2(1H)-ones and Evaluation of their Plasmodium falciparum Gametocytocidal Activities, Application In Synthesis of 947533-21-3, the publication is ACS Combinatorial Science (2017), 19(12), 748-754, database is CAplus and MEDLINE.

A novel three-component, two-step, 1-pot nucleophilic aromatic substitution (S_NAr)-intramol. cyclization-Suzuki coupling reaction was developed for the synthesis of benzo[h][1,6]naphthyridin-2(1H)-ones (Torins). On the basis of the new efficiently convergent synthetic route, a library of Torin 2 analogs was synthesized. The antimalarial activities of these compounds were evaluated against asexual parasites using a growth inhibition assay and gametocytes using a viability assay.

ACS Combinatorial Science published new progress about 947533-21-3. 947533-21-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Boronic acid and ester,Amine,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (6-Acetamidopyridin-3-yl)boronic acid, and the molecular formula is C7H9BN2O3, Application In Synthesis of 947533-21-3.

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

Patel, Paresma R. published the artcileIn vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents, Name: (6-Acetamidopyridin-3-yl)boronic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2016), 26(12), 2907-2911, database is CAplus and MEDLINE.

Novel imidazo[4,5-c]quinolin-2-ones, such as I, were synthesized and evaluated in asexual blood stage and late stage gametocyte assays of Plasmodium falciparum, a major causative agent of malaria. The design of these compounds is based on a recently identified lead compound from a high throughput screen. A concise synthesis was developed that allowed for generation of analogs with substitution around both the quinoline and imidazolidinone rings. Through structure-activity relationship studies, a number of potent compounds were identified that possessed excellent antimalarial activity against both the asexual and sexual stages with minimal cytotoxicity in mammalian cells. This is the first Letter describing SAR and gametocytocidal activity of imidazo[4,5-c]quinolin-2-ones, a new lead series for malaria treatment and prevention.

Bioorganic & Medicinal Chemistry Letters published new progress about 947533-21-3. 947533-21-3 belongs to amides-buliding-blocks, auxiliary class Pyridine,Boronic acid and ester,Amine,Amide,Boronic Acids,Boronic Acids,Boronic acid and ester,, name is (6-Acetamidopyridin-3-yl)boronic acid, and the molecular formula is C7H9BN2O3, Name: (6-Acetamidopyridin-3-yl)boronic acid.

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

Bose, D. Subhas published the artcileA simple method for the synthesis of nitriles from primary amides under neutral conditions, Recommanded Product: 2,4-Dichlorobenzamide, the publication is Synthetic Communications (1999), 29(23), 4235-4239, database is CAplus.

1-(3-Dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (EDCI) is a very useful reagent for the preparation of nitriles in good yields under neutral conditions. For example, dehydration of 2,4-dimethoxybenzamide gave 2,4-dimethoxybenzonitrile. Elimination reaction of 4-chlorobenzenecarbothioamide gave 4-chlorobenzonitrile.

Synthetic Communications 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, Recommanded Product: 2,4-Dichlorobenzamide.

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

Marchlewski, L. published the artcileAbsorption of ultra-violet light by some organic substances. XXIX, Formula: C10H14N2O, the publication is Bulletin International de l’Academie Polonaise des Sciences et des Lettres, Classe des Sciences Mathematiques et Naturelles, Serie A: Sciences Mathematiques (1933), 95-8, database is CAplus.

The α, β and γ isomers of C₅H₄NCONEt₂ in aqueous solution give similar absorption spectra in the ultra-violet, but the spectra are quite different from that of C₅H₅N (cf. C. A. 23, 5405). Each shows one absorption band with maximum and min. as follows: α isomer, maximum at 2625 A. U., min. at 2455 A. U.; β isomer, maximum at 2615 A. U., min. at 2475 A. U.; γ isomer, maximum at 2580 A. U., min. at 2430 A. U.

Bulletin International de l’Academie Polonaise des Sciences et des Lettres, Classe des Sciences Mathematiques et Naturelles, Serie A: Sciences Mathematiques 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 C10H14N2O, Formula: C10H14N2O.

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

Yavorskii, N. P. published the artcileComplexes of cadmium thiocyanate and bromide with nitrogen-containing drugs, Formula: C10H14N2O, the publication is Farmatsiya (Moscow, Russian Federation) (1970), 19(2), 49-53, database is CAplus.

A study of complex formation of Cd thiocyanate (I) and CdBr2 with N-containing bases is presented. Piperazine, isoniazid, and amidopyridine form complexes XCd(CNS)2 (X = base) with I, with hexamethylenetetramine X.2Cd(CNS)2, and with nicotine X2.Cd(CNS)2.2HCNS. With CdBr2, complexes of the type X.CdBr2.2HBr are obtained with N-containing bases. The formed complexes with I and with CdBr2 are poorly H2O soluble The reaction sensitivity for I ranges from 5 to 40,000 γ/ml, and for CdBr2 from 10 to 30,000 γ/ml of the investigated bases. Complexes of preparations used in the form of salts have a common composition

Farmatsiya (Moscow, Russian Federation) 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 C30H24BrCuN2P, Formula: C10H14N2O.

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

Husain, S. Shaukat published the artcilep-Trifluoromethyldiazirinyl-etomidate: A Potent Photoreactive General Anesthetic Derivative of Etomidate That Is Selective for Ligand-Gated Cationic Ion Channels, Synthetic Route of 360-92-9, the publication is Journal of Medicinal Chemistry (2010), 53(17), 6432-6444, database is CAplus and MEDLINE.

We synthesized the R- and S-enantiomers of Et 1-(1-(4-(3-(trifluoromethyl)-3H-diazirin-3-yl)phenyl)ethyl)-1H-imidazole-5-carboxylate (trifluoromethyldiazirinyl-etomidate) (I), or TFD-etomidate, a novel photoactivable derivative of the stereoselective general anesthetic etomidate [R-(2-Et 1-(phenylethyl)-1H-imidazole-5-carboxylate)]. Anesthetic potency was similar to etomidate’s, but stereoselectivity was reversed and attenuated. Relative to etomidate, TFD-etomidate was a more potent inhibitor of the excitatory receptors, nAChR (nicotinic acetylcholine receptor) ((α1)₂β1δ1γ1) and 5-HT_3AR (serotonin type 3A receptor), causing significant inhibition at anesthetic concentrations S- but not R-TFD-etomidate enhanced currents elicited from inhibitory α1β2γ2L GABA_ARs by low concentrations of GABA, but with a lower efficacy than R-etomidate, and site-directed mutagenesis suggests they act at different sites. [³H]TFD-etomidate photolabeled the α-subunit of the nAChR in a manner allosterically regulated by agonists and noncompetitive inhibitors. TFD-etomidate’s novel pharmacol. is unlike that of etomidate derivatives with photoactivable groups in the ester position, which behave like etomidate, suggesting that it will further enhance our understanding of anesthetic mechanisms.

Journal of Medicinal 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, Synthetic Route of 360-92-9.

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

Li, AnRong published the artcileA convenient trifluoroacetylation of amines with trifluoroacetic acid and titanium tetrachloride, Recommanded Product: N,N-Diethyl-2,2,2-trifluoroacetamide, the publication is Chinese Journal of Chemistry (1993), 11(2), 190-2, database is CAplus.

Treating R¹R²NH (R¹ = H, R² = Ph, cyclohexyl, allyl, Me₂CHCH₂, 2-NH₂C₆H₄, 2-HOC₆H₄; R¹ = R² = Et; R¹ = Ph, R² = Me) with CF₃CO₂H, 2 equiv Et₃N, and 2 equiv TiCl₄ in Et₂O, MeCN, or CH₂Cl₂ gave 40-75% R¹R²NCOCF₃ (same R¹, R²); in the case of o-phenylenediamine, the product is 2-(trifluoroacetyl)benzimidazole.

Chinese Journal of 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