Category: chlorides-buliding-blocks

McManus, E. C. published the artcileUse of coccidia to study the structure-activity relations of a series of p-aminobenzoic acid antagonists, Computed Properties of 5204-46-6, the publication is Develop. Ind. Microbiol. (1965), 44-7, database is CAplus.

Young coccidiosis-susceptible chicks were fed a standard laboratory ration with graded concentrations of test chemicals added just prior to use. On the 2nd day of the test, the chicks were inoculated orally with 100,000 sporulated oocysts of Eimeria maxima; 6 days later birds were killed and weighed, the small intestine homogenized with water, and the oocysts counted. The min. effective diet concentrations of 28 derivatives of p-aminobenzoic acid (I) were determined together with the percent reduction of oocyst count. Remarkably potent anticoccidial compounds were found in a series of ortho-substituted derivatives of I. Groups with high coccidiostatic activity conferring effects were lower alkoxy, alkylthio, and alkyl amino with approx. similar size and shape. The most active compounds, capable of reducing the oocyst count below 25% were the ο-ethoxy derivative, its esters, and N-acyl derivatives, and the ο-chloro, ο-methoxy, ο-isopropoxy, ο-ethyl, and ο-thioethyl derivatives of I. Me 4-acetamido-2-ethoxybenzoate (ethopabate) (II) reduced the oocyst count to nil. The methyl, chloro, nitro, and methoxy derivatives conferred anticoccidial activity when substituted in the ortho position, but not in meta position. Disubstituted derivatives were inactive. The in vivo anticoccidial activity of II and sulfaquinoxaline (III) was overcome completely by simultaneous administration of I. Both II and III potentiated the anticoccidial activity of pyrimethamine. Cross resistance occurred between II and III for many strains of coccidia. The dose-response curves of II and III were parallel, and their anticoccidial activities were additive. II was about 150-fold more potent than III for control of certain strains of E. maxima and Ε. brunetti, and less potent for Ε. tenella. Both II and III were assumed to inhibit biosynthesis of folic acid-type compounds at different steps in the sequence of reactions for synthesis of tetrahydrofolic acid.

Develop. Ind. Microbiol. published new progress about 5204-46-6. 5204-46-6 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Carboxylic acid,Amine,Benzene, name is 4-Amino-2,6-dichlorobenzoic acid, and the molecular formula is C7H5Cl2NO2, Computed Properties of 5204-46-6.

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

Cremlyn, Richard J. published the artcileThe chemistry of sulfonylcoumarin derivatives, Category: chlorides-buliding-blocks, the publication is Journal of the Chemical Society of Pakistan (1988), 10(1), 97-104, database is CAplus.

6-(Chlorosulfonyl)coumarin was amidated to give amides I (R¹ = H, alkyl; R² = H, alkyl, PhCH₂, tolyl; or NR¹R² = morpholino). Similarly, hydrazones II [R³ = Me, H; R⁴ = Me, Ph, ClC₆H₄, O₂NC₆H₄; or R³R⁴ = (CH₂)₄] were prepared from the sulfonyl chloride via the resp. hydrazide. Some I and II showed fungicidal activity.

Journal of the Chemical Society of Pakistan published new progress about 10543-42-7. 10543-42-7 belongs to chlorides-buliding-blocks, auxiliary class Other Aromatic Heterocyclic,Chloride,Sulfonyl chlorides,Ester, name is Coumarin-6-sulfonyl chloride, and the molecular formula is C9H5ClO4S, Category: chlorides-buliding-blocks.

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

Rubin, Heather published the artcileScalable Synthesis of N-Acylaziridines from N-Tosylaziridines, Name: Sodium chloro(tosyl)amide trihydrate, the publication is Journal of Organic Chemistry (2013), 78(17), 8865-8871, database is CAplus and MEDLINE.

N-Acylaziridines are important starting materials for the synthesis of chiral amine derivatives The traditional methods for producing these activated aziridines have significant drawbacks. The gram scale synthesis of N-acylaziridines by deprotection of N-tosylaziridines and reprotection with N-hydroxysuccinimide derivatives is described. Mono- and disubstituted aziridines perform well, with complete retention of stereochem. purity. The consistently moderate yields are linked to the N-tosylaziridine deprotection step, while acylation with N-hydroxysuccinimide derivatives is highly efficient.

Journal of Organic Chemistry published new progress about 7080-50-4. 7080-50-4 belongs to chlorides-buliding-blocks, auxiliary class Halogenation Reagent,Inhibitor, name is Sodium chloro(tosyl)amide trihydrate, and the molecular formula is C7H13ClNNaO5S, Name: Sodium chloro(tosyl)amide trihydrate.

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

Harmse, Rozanne published the artcileActivities of 11-Azaartemisinin and N-Sulfonyl Derivatives against Asexual and Transmissible Malaria Parasites, Related Products of chlorides-buliding-blocks, the publication is ChemMedChem (2017), 12(24), 2086-2093, database is CAplus and MEDLINE.

Dihydroartemisinin (DHA), either used in its own right or as the active drug generated in vivo from the other artemisinins in current clin. use-artemether and artesunate-induces quiescence in ring-stage parasites of Plasmodium falciparum (Pf). This induction of quiescence is linked to artemisinin resistance. Thus, we have turned to structurally disparate artemisinins that are incapable of providing DHA on metabolism Accordingly, 11-azaartemisinin 5 and selected N-sulfonyl derivatives were screened against intraerythrocytic asexual stages of drug-sensitive Pf NF54 and drug-resistant K1 and W2 parasites. Most displayed appreciable activities against all three strains, with IC₅₀ values <10.5 nM. The p-trifluoromethylbenzenesulfonyl-11-azaartemisinin derivative 11 [(4′-trifluoromethyl)benzenesulfonylazaartemisinin] was the most active, with IC₅₀ values between 2 and 3 nM. The compounds were screened against Pf NF54 early and transmissible late intraerythrocytic-stage gametocytes using luciferase and parasite lactate dehydrogenase (pLDH) assays. The 2′-thienylsulfonyl derivative 16 (2′-thiophenesulfonylazaartemisinin) was notably active against late-stage (IV-V) gametocytes with an IC₅₀ value of 8.7 nm. All compounds were relatively nontoxic to human fetal lung WI-38 fibroblasts, showing selectivity indexes of >2000 toward asexual parasites. Overall, the readily accessible 11-azaartemisinin 5 and the sulfonyl derivatives 11 and 16 represent potential candidates for further development, in particular for transmission blocking of artemisinin-resistant parasites.

ChemMedChem published new progress about 21286-54-4. 21286-54-4 belongs to chlorides-buliding-blocks, auxiliary class Chiral,Chloride,Sulfonyl chlorides,Aliphatic cyclic hydrocarbon,Ketone, name is ((1S,4R)-7,7-Dimethyl-2-oxobicyclo[2.2.1]heptan-1-yl)methanesulfonyl chloride, and the molecular formula is C10H15ClO3S, Related Products of chlorides-buliding-blocks.

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

Unterhalt, B. published the artcileSynthesis of methadone-nitrile as well as isomethadone-nitrile, and related compounds, Name: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, the publication is Scientia Pharmaceutica (2000), 68(3), 229-234, database is CAplus.

R₂NCH₂CHMeCl [R₂ = Me₂, (CH₂)₅, (CH₂)₂O(CH₂)₂, (CH₂)₄] are reacted with Ph₂CHCN under phase-transfer conditions to give a mixture of the corresponding nitriles R₂NCHMeCH₂CPh₂CN and R₂NCH₂CHMeCPh₂CN. Both R₂NCH₂CHPhCl and R₂NCHPhCH₂Cl [R₂ = Me₂, (CH₂)₅, (CH₂)₂O(CH₂)₂, (CH₂)₄] led to resp. R₂NCH₂CHPhCPh₂CN.

Scientia Pharmaceutica published new progress about 4584-49-0. 4584-49-0 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Salt,Amine,Aliphatic hydrocarbon chain, name is 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride, and the molecular formula is C10H2F12NiO4, Name: 2-Chloro-N,N-dimethylpropan-1-amine hydrochloride.

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

Maximo, Patricia published the artcilePhotomodulation of ultrastable host-guest complexes in water and their application in light-controlled steroid release, Synthetic Route of 219537-97-0, the publication is Organic Chemistry Frontiers (2022), 9(16), 4238-4249, database is CAplus.

The cucurbit[8]uril (CB8) synthetic receptor was shown to form high-affinity host-guest complexes with dicationic dithienylethene (DTE) photoswitches I [R = H, Me; R¹ = 1-iodo-1-methyl-2-pyridyl, 1-iodo-1-methyl-3-pyridyl, 1-iodo-1-methyl-4-pyridyl] in water. ITC experiments combined with computational studies suggest that the formation of the inclusion complexes was mainly driven by a combination of hydrophobic effects, ion-dipole, hydrogen- and chalcogen-bonding interactions. The binding affinities were observed to be much higher for the DTE closed isomers, reaching values in the picomolar range (up to 10¹¹ M^-1) while the open isomers display up to 10 000-fold lower affinities, setting ideal conditions for the development of robust photoswitchable host-guest complexes. The light-responsive affinity of these photoswitches toward CB8 was explored to control the encapsulation and release of nanomolar affinity steroids via competitive guest replacement.

Organic Chemistry Frontiers published new progress about 219537-97-0. 219537-97-0 belongs to chlorides-buliding-blocks, auxiliary class Fused/Partially Saturated Cycles,Cyclopentenes, name is 5-Chloro-3-[2-(5-chloro-2-methylthien-3-yl)cyclopent-1-en-1-yl]-2-methylthiophene, and the molecular formula is C15H14Cl2S2, Synthetic Route of 219537-97-0.

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

Slack, Eric D. published the artcileUnderstanding the Activation of Air-Stable Ir(COD)(Phen)Cl Precatalyst for C-H Borylation of Aromatics and Heteroaromatics, Synthetic Route of 929626-16-4, the publication is Organic Letters (2021), 23(5), 1561-1565, database is CAplus and MEDLINE.

A newly developed robust catalyst [Ir(COD)(Phen)Cl] (A) was used for the C-H borylation of three dozen aromatics and heteroaromatics with excellent yield and selectivity. Activation of the catalyst was identified using catalytic amounts of H₂O, alcs., etc., when B₂pin₂ was used in noncoordinating solvents, while for THF catalytic use of HBpin was required. The results were on par with the in situ based expensive system [Ir(OMe)(COD)]₂/dtbbpy or Me₄Phen.

Organic Letters published new progress about 929626-16-4. 929626-16-4 belongs to chlorides-buliding-blocks, auxiliary class Chloride,Boronic acid and ester,Benzene,Ether,Boronic Acids,Boronate Esters, name is 2-(3-Chloro-5-methoxyphenyl)-4,4,5,5-tetramethyl-1,3,2-dioxaborolane, and the molecular formula is C10H18O, Synthetic Route of 929626-16-4.

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

Wood, Gordon W. published the artcileMethyl transfer in field desorption mass spectrometry of ammonioalkanecarboxylate hydrochloride salts, COA of Formula: C7H16ClNO2, the publication is Organic Mass Spectrometry (1983), 18(1), 42-5, database is CAplus.

Field desorption mass spectra of simple N,N,N-trimethylammoniocarboxylate hydrochloride salts and their N,N,N-perdeuteriotrimethylammonium analogs are reported in which Me transfer was observed Mechanisms for this and other fragmentation and rearrangement processes are dependent on anode heating current. Addition of the protonating agent p-MeC₆H₄SO₃H suppressed most ions except the protonated mol. ion.

Organic Mass Spectrometry 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 C18H35NO, COA of Formula: C7H16ClNO2.

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

Grandin, Catherine published the artcileA practical synthesis of cycloalkylphosphonates from trichloromethylphosphonates, Application In Synthesis of 866-23-9, the publication is Synthesis (1995), 239-41, database is CAplus.

Cycloalkylophosphonates I (R = Et, CHMe₂, n = 1,2,3,4, X = H) with ring size varying from 4 to 6 were synthesized in good overall yields, in two steps from trichloromethylphosphonates and ω-dibromalkanes, via the corresponding α-trimethylsilyl cycloalkylphosphonates I (X = SiMe₃, R and n = same).

Synthesis published new progress about 866-23-9. 866-23-9 belongs to chlorides-buliding-blocks, auxiliary class Aliphatic Chain, name is Diethyltrichloromethylphosphonate, and the molecular formula is C5H10Cl3O3P, Application In Synthesis of 866-23-9.

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

Zhang, Huaisheng published the artcileDiscovery of a quinoline-based phenyl sulfone derivative as an antitrypanosomal agent, Application of 3-Chloro-4-hydroxyphenylacetic acid, the publication is Bioorganic & Medicinal Chemistry Letters (2018), 28(9), 1647-1651, database is CAplus and MEDLINE.

A series of natural products-based Ph sulfone derivative and their property-based analogs were investigated as potential growth inhibitors of Trypanosoma brucei. Trypanosoma brucei is a kinetoplastid protozoan parasite that causes trypanosomiasis. In this work, the authors found that nopol- and quinoline-based Ph sulfone derivative were the most active and selective for T. brucei, and they were not reactive towards the active thiol of T. brucei’s cysteine protease rhodesain. A thiol reactive variant of the quinoline-based Ph sulfone was subsequently investigated and found to be a moderate inhibitor of rhodesain. The quinoline-based compound that is not reactive towards rhodesain can serve a template for phenotypic-based lead discovery while its thiol-active congener can serve as template for structure-based investigation of new antitrypanosomal agents.

Bioorganic & Medicinal Chemistry Letters 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 C24H12, Application of 3-Chloro-4-hydroxyphenylacetic acid.

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