Author: Jessica.F

James, C. S. published the artcilePlant growth-regulating substances. XXVI. Isatic and anthranilic acids, Formula: C7H5Cl2NO2, the main research area is isatic acid growth regulation; anthranilic acid growth regulation; growth regulation anthranilic acid.

The plant growth-regulating activities of isatic acid and 26 isatic acid derivatives, together with the 27 corresponding anthranilic acids, were assessed in the wheat cylinder, the pea segment, and pea curvature tests. Activity was sustained by substitution in the 4-and 5-positions of isatic acid as in Na 4-chloroisatate and Na 5-bromoisatate but decreased by substitution in the 3- and 6-positions as in Na 3-chloroisatate and Na 6-chloroisatate. In the anthranilic acid series, the parent acid was inactive but the introduction of a large grouping (Br or I) into the 5-position as in Na 5-iodoanthranilate conferred activity. The 3,6- and 5,6-dichloro and the 3,6-dibromo acids such as Na 3,6-dichloroisatate were also active; compounds substituted in the 4-position to the carboxyl group or disubstituted in the 3 and 5 positions as in Na 3,5-dichloroisatate, were, as expected, inactive. Wheat coleoptile and pea stem segments metabolized Na isatate and Na 5-chloroisatate to the corresponding Na anthranilate and Na 5-chloroanthranilate, together with an unidentified nonacidic metabolite in each case. The acids apparently possess activity per se since there was no evidence that the growth regulating activity of isatic acids was related to this breakdown. 19 references.

Annals of Applied Biology published new progress about Hormones, plant Role: BIOL (Biological Study). 3032-32-4 belongs to class chlorides-buliding-blocks, name is 2-Amino-3,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Formula: C7H5Cl2NO2.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Jung, Michael E. published the artcileStructure-Activity Relationship of Semicarbazone EGA Furnishes Photoaffinity Inhibitors of Anthrax Toxin Cellular Entry, COA of Formula: C8H4ClF3O, the main research area is phenyl azide photoaffinity inhibitor anthrax toxin semicarbazone EGA SAR; Photoaffinity labeling; anthrax lethal toxin; aryl azide; endosomal trafficking; semicarbazone.

[In this abstract compounds 1-5 are represented by graphic structure I as follows: 1: X, Y = H, Z = Br; 2: X = F, Y = H, Z = Br; 3: X = F, Y = H, Z = N3; 4: X, Y = H, Z = N3; 5: X, Y = F, Z = N3]. EGA, 1, prevents the entry of multiple viruses and bacterial toxins into mammalian cells by inhibiting vesicular trafficking. The cellular target of 1 is unknown, and a structure-activity relationship study was conducted in order to develop a strategy for target identification. A compound with mid-nanomolar potency was identified (2), and three photoaffinity labels were synthesized (3-5). For this series, the expected photochem. of the Ph azide moiety is a more important factor than the IC50 of the photoprobe in obtaining a successful photolabeling event. While 3 was the most effective reversible inhibitor of the series, it provided no protection to cells against anthrax lethal toxin (LT) following UV irradiation Conversely, 5, which possessed weak bioactivity in the standard assay, conferred robust irreversible protection vs LT to cells upon UV photolysis.

ACS Medicinal Chemistry Letters published new progress about Alkylation, regioselective (of semicarbazone core). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, COA of Formula: C8H4ClF3O.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Warsitz, Michael published the artcileTwo-Step Procedure for the Synthesis of 1,2,3,4-Tetrahydro-quinolines, Related Products of chlorides-buliding-blocks, the main research area is chlorostyrene aniline alkyl titanium regioselective hydroaminoalkylation catalyst; amine aryl alkyl preparation palladium Buchwald Hartwig amination; tetrahydroquinoline preparation.

A new two-step procedure that includes an initial regioselective intermol. hydroaminoalkylation of ortho-chlorostyrenes with N-methylanilines and a subsequent intramol. Buchwald-Hartwig amination gives direct access to 1,2,3,4-tetrahydroquinolines. The hydroaminoalkylation reaction of the ortho-chlorostyrenes is catalyzed by a 2,6-bis(phenylamino)pyridinato titanium complex which delivers the linear regioisomers with high selectivities. In addition, the formation of unexpected dihydroaminoalkylation products from styrenes and N-methylanilines is reported.

European Journal of Organic Chemistry published new progress about Aminoalkylation (regioselective hydroaminoalkylation). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Related Products of chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Dhungana, Roshan K. published the artcileNi-catalyzed regioselective 1,2-dialkylation of alkenes enabled by the formation of two C(sp3)-C(sp3) bonds, Application In Synthesis of 886496-91-9, the main research area is alkene regioselective dialkylation benzyl halide alkylzinc reagent nickel catalysis.

The authors disclosed a Ni-catalyzed vicinal difunctionalization of alkenes with benzyl halides and alkylzinc reagents, which produces products with two new alkyl-alkyl bonds. This alkene dialkylation is effective in combining secondary benzyl halides and secondary alkylzinc reagents with internal alkenes, which furnishes products with three contiguous all-carbon secondary stereocenters. The products can be readily elaborated to access complex tetraene, benzosuberene, and bicyclodecene cores. The reaction also features as the most efficient alkene difunctionalization process to date with catalyst loadings down to 500 ppm and the catalytic turnover number (TON) and turnover frequency (TOF) registering up to 2 x 103 and 165 h-1 at rt, resp.

Journal of the American Chemical Society published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent). 886496-91-9 belongs to class chlorides-buliding-blocks, name is 1-(Bromomethyl)-3-chloro-5-(trifluoromethyl)benzene, and the molecular formula is C8H5BrClF3, Application In Synthesis of 886496-91-9.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Lemrova, Barbora published the artcileSolid-Phase Synthesis of 4,7,8-Trisubstituted 1,2,3,4-Tetrahydro-benzo[e][1,4]diazepin-5-ones, Application In Synthesis of 35112-05-1, the main research area is benzodiazepinone solid phase preparation chlorofluoronitrobenzoic acid synthon; benzodiazocinone thiazine thiazepine derivative solid phase preparation.

Solid-phase synthesis of 1,2,3,4-tetrahydro-benzo[e][1,4]diazepin-5-ones with the use of a polystyrene resin is described. The starting material was polymer-supported 1,2-diaminoethane and 4-chloro-2-fluoro-5-nitrobenzoic acid was used as a key synthon. The synthetic approach allows the preparation of derivatives with variable substitution at positions 4 and 8. Addnl., a skeletal diversity was increased when the nitro group was reduced and some benzene fused heterocycles were prepared An expansion of a diazepinone to a benzodiazocinone scaffold was also successful, although some limitations in the diversity of the target derivatives were observed

ACS Combinatorial Science published new progress about Alcohols Role: RCT (Reactant), RACT (Reactant or Reagent). 35112-05-1 belongs to class chlorides-buliding-blocks, name is 4-Chloro-2-fluoro-5-nitrobenzoic acid, and the molecular formula is C7H3ClFNO4, Application In Synthesis of 35112-05-1.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Wang, Huan published the artcileCationic palladium(II)-catalyzed synthesis of 2-substituted 3-hydroxymethylbenzo[b]furans, Application of 2-Chloro-3-(trifluoromethyl)benzaldehyde, the main research area is hydroxymethylbenzofuran preparation; benzofuran hydroxymethyl preparation; alkynyl phenol preparation heterocyclization aldehyde palladium catalyst.

A tandem reaction involving an intramol. oxypalladation of an alkyne and an addition to the carbonyl group to quench the carbon-palladium bond to complete the catalytic cycle was developed. The reaction of 2-alkynylphenols with aldehydes to prepare substituted 3-(hydroxymethyl)benzofurans in one pot is described. E.g, reaction of 2-(phenylethynyl)phenol and p-nitrobenzaldehyde, catalyzed by [Pd(dppp)(H2O)2](BF4)2, gave 90% benzofuran (I). The reaction was catalyzed with the cationic palladium(II) species without the necessity of a redox system.

Synlett published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Application of 2-Chloro-3-(trifluoromethyl)benzaldehyde.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Pieroni, Marco published the artcileSynthesis, Biological Evaluation, and Structure-Activity Relationships for 5-[(E)-2-Arylethenyl]-3-isoxazolecarboxylic Acid Alkyl Ester Derivatives as Valuable Antitubercular Chemotypes, Category: chlorides-buliding-blocks, the main research area is arylethenylisoxazolecarboxylic acid stereoselective preparation tuberculosis antituberculosis structure activity; bromomethylisoxazole triphenylphosphine aldehyde Wittig olefination.

Tuberculosis (TB), mostly caused by Mycobacterium tuberculosis (Mtb), is one of the leading causes of death from infectious disease worldwide. Its coinfection with HIV and the emergence of multidrug-resistant TB (MDR-TB) and extensively drug-resistant TB (XDR-TB) strains have further worsened the TB pandemic. Despite its global impact, TB is considered a neglected disease and no new anti-TB therapeutics have been introduced over the last four decades. The nonreplicating persistent form of TB (NRP-TB) is responsible for the length of the treatment and is the putative cause of treatment failure. Therefore, new anti-TB agents, which are active against both the replicating form of Mtb (R-TB) and NRP-TB, are urgently needed. The synthesis and structure-activity relationships (SAR) of a series of 5-[(E)-2-arylethenyl]-3-isoxazolecarboxylic acid alkyl esters e.g. I, as potent anti-TB agents are reported. Several compounds had submicromolar min. inhibitory concentrations (MIC) against R-TB and were active against NRP-TB in the low micromolar range, thus representing attractive lead compounds for the possible development of new anti-TB agents.

Journal of Medicinal Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 286474-59-7 belongs to class chlorides-buliding-blocks, name is 6-Chloro-2-fluoro-3-methylbenzaldehyde, and the molecular formula is C8H6ClFO, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Khera, Rasheed Ahmad published the artcileSynthesis of fluorinated 2,3-dihydropyran-4-ones by cyclocondensation of 1,3-dicarbonyl dianions with aldehydes, Category: chlorides-buliding-blocks, the main research area is pyranone dihydrotrifluoromethyl preparation; pentanedione fluorinated aldehyde cyclocondensation.

The reaction of the dianion of 1,1,1-trifluoro-pentane-2,4-dione with aldehydes and subsequent addition of hydrochloric acid afforded 2,3-dihydro-6-trifluoromethyl-pyran-4-ones. The reaction of the dianion of acetylacetone with fluorinated benzaldehydes gave the corresponding fluorinated 2-aryl-2,3-dihydro-6-methyl-pyran-4-ones. All reactions proceeded in very good yield and with very good regioselectivity. While 2 crystal structures were determined, no data are reported here.

Journal of Fluorine Chemistry published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Bernardo, Paul H. published the artcileSynthesis of a rhodanine-based compound library targeting Bcl-XL and Mcl-1, Computed Properties of 480438-56-0, the main research area is mol docking anticancer agent rhodanine pyridine amino acid preparation.

Symposium report presented at the 18th International Conference on Organic Synthesis (ICOS) Bergen, Norway 1-6 August, 2010. A small library of pyridine-based rhodanine analogs of BH-3I-1 [i.e., 5-[(4-bromophenyl)methylene]-α-(1-methylethyl)-4-oxo-2-thioxo-3-thiazolidineacetic acid] was designed, the synthesis of the target compound was achieved using amino acids as starting materials and the products thus obtained were screened against B-cell lymphoma (extra large, Bcl-XL, antiapoptotic protein, inhibitor of apoptosis proteins) and myeloid cell leukemia sequence 1 (Mcl-1) for the ability to displace 5-(carboxy)fluorescein-labeled Bak peptide (Flu-Bak). Differences in selectivity toward Bcl-XL and Mcl-1 were observed and the binding modes of selected compounds were studied further. The results may be useful in designing potent small-mol. inhibitors of Bcl-XL and Mcl-1 as well as selective Mcl-1 inhibitors.

Pure and Applied Chemistry published new progress about Amino acids Role: RCT (Reactant), RACT (Reactant or Reagent). 480438-56-0 belongs to class chlorides-buliding-blocks, name is 3-Chloro-4-isopropoxyphenylboronic acid, and the molecular formula is C9H12BClO3, Computed Properties of 480438-56-0.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

Saha, Debasmita published the artcileA sequential synthetic strategy towards unexplored dibenzo[b,f][1,4]thiazepine carboxamides: copper catalyzed C-S cyclization followed by Ugi type 3CC cascade, Category: chlorides-buliding-blocks, the main research area is carboxamide dibenzothiazepine preparation; dibenzothiazepine preparation isocyanide carboxylic acid Ugi reaction; aminothiophenol halo benzaldehyde copper catalyst cyclization.

A two-step diversity oriented synthetic protocol to a novel class of dihydrodibenzo[b,f][1,4]thiazepine-11-carboxamides was developed. The first step ensured the synthesis of dibenzothiazepine via copper-mediated condition followed by Ugi-Joullie reaction of the resultant cyclic imine in the second step.

RSC Advances published new progress about Amides Role: SPN (Synthetic Preparation), PREP (Preparation). 93118-03-7 belongs to class chlorides-buliding-blocks, name is 2-Chloro-3-(trifluoromethyl)benzaldehyde, and the molecular formula is C8H4ClF3O, Category: chlorides-buliding-blocks.

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics