Tag: 100-200

On October 31, 1996, Al-Darwich, M. J.; Plenevaux, A.; Lemaire, C.; Fiore, G. D.; Christiaens, L.; Comar, D.; Luxen, A. published an article.Quality Control of 4-Chloro-2-fluorotoluene The title of the article was Enantioselective syntheses of no-carrier-added (n.c.a.) (S)-4-chloro-2-[18F] fluorophenylalanine and (S)-(α-methyl)-4-chloro-2-[18f] fluorophenylalanine. And the article contained the following:

Title compounds I (R = H, Me) were prepared and labeled with no carrier added 18F through a radiochem. synthesis relying on the highly enantioselective reaction between 4-chloro-2-[18F]fluorobenzyl iodide and the lithium enolate of 1,3-imidazolidinones II. Quantities of about 20-25 mCi were obtained at the end of synthesis, ready for injection after hydrolysis and high performance liquid chromatog. (HPLC) purification, with a radiochem. yield of 17%-20% corrected to the end of bombardment after a total synthesis time of 90-105 min from [18F] fluoride. The enantiomeric excesses were ≥97% for both mols. without chiral separation and the radiochem. and chem. purities were ≥98%. The experimental process involved the reaction of 4-Chloro-2-fluorotoluene(cas: 452-75-5).Quality Control of 4-Chloro-2-fluorotoluene

The Article related to asym preparation fluorine 18 chlorofluorophenylalanine, phenylalanine chlorofluoromethyl fluorine 18 asym preparation, stereoselective alkylation imidazolidinone chlorofluorobenzyl iodide and other aspects.Quality Control of 4-Chloro-2-fluorotoluene

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

On February 28, 1993, Nadir, Upender K.; Arora, Anjali published an article.Safety of trimethyloxosulphonium chloride The title of the article was A facile synthesis of N-arylsulfonylazetidines through the reaction of N-arylsulfonylaziridines with dimethyloxosulfonium methylide and a PTC [phase-transfer catalyst]. And the article contained the following:

N-Arylsulfonylazetidines (I; R1 = e.g., H, C6H4Me-p; R2 = alkyl, aryl) can be prepared in 18-55% yield by the reaction of corresponding aziridines (II) with dimethyloxosulfonium methylide in the presence of a PTC (e.g., tetrabutylammonium hydrogen sulfate). Aziridines substituted at positions 2 and 3 failed to react. The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Safety of trimethyloxosulphonium chloride

The Article related to ring expansion arylsulfonylaziridine sulfur ylide, aziridine arylsulfonyl ring expansion sulfur ylide, phase transfer ring expansion catalyst arylsulfonylaziridine, azetidine arylsulfonyl and other aspects.Safety of trimethyloxosulphonium chloride

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

On May 20, 1995, Miyamoto, Yoshiko; Kohno, Hitoshi; Pfleiderer, Wolfgang; Boeger, Peter; Wakabayashi, Ko published an article.Application of 452-75-5 The title of the article was Synthesis of 1,2,4-triazolo[1,5-a]-1,3,5-triazine derivatives for phytotoxic activity. And the article contained the following:

Treatment of benzylideneaminoguanidines (I) with Et N-cyanoformimidate (II) in MeCN at room temperature gave 1-benzylideneamino-2-cyanoiminomethylguanidines (III). I (R1 = 2-F and 4-Cl, R2 = H, R3 = Me) and I (R1 = 4-Cl, R2 = H, R3 = Me) were treated with II directly to give 7-methylamino-2-halophenyl-1,2,4-triazolo[1,5-a]-1,3,5-triazines V (R1 = 2-F and 4-Cl, R2 = H, R3 = Me) and V (R1 = 4-Cl, R2 = H, R3 = Me) under similar conditions. III were readily cyclized to the corresponding 1,2-dihydro-1,2,4-triazolo[1,5-a]-1,3,5-triazines (IV) by brief heating in MeOH. IV were oxidized with iodine in EtOH to give the corresponding V. Phytotoxic activities of III, IV, and V were assayed using green microalgae, Scenedesmus acutus. V (R1 = 2-F and 4-Cl, R2 = R3 = H) and some other compounds were found to suppress the cell growth and chlorophyll formation of Scenedesmus, but those activities were still not good enough to be utilized as a herbicide or plant growth regulator. The experimental process involved the reaction of 4-Chloro-2-fluorotoluene(cas: 452-75-5).Application of 452-75-5

The Article related to triazolotriazine synthesis phytotoxicity, condensation benzylideneaminoguanidine cyanoformimidate, cyclization benzylideneaminocyanoiminomethylguanidine, oxidation hydrotriazolotriazine and other aspects.Application of 452-75-5

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

On April 23, 2009, Glatthar, Ralf; Carcache, David published a patent.Computed Properties of 38939-88-7 The title of the patent was Preparation of benzimidazoles and related compounds as modulators of metabotropic glutamate receptor-5 for treating gastrointestinal, urinary, and nervous system disorders. And the patent contained the following:

The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula I (wherein X1 -X4 each independently represent CR2 or N; R2 is H, halo, OH. etc.; R1 is C1-6alkyl, C1-6halogenalkyl, C3-12cycloalkyl, etc.; B is aryl, nitrogen-containing ring, etc.; C is a 5-12-membered aromatic (un)substituted ring system that may contain hetero atoms) and salts, solvates, hydrates and N-oxides thereof. Synthetic procedures for preparing I are exemplified. Example compound II, prepared by reacting 3-chloro-5-iodo-N-2-propylbenzene-1,2-diamine and 5-chloro-6-(6-methylpyridin-3-ylamino)nicotinoyl chloride, caused 97% inhibition of mGluR5 activity at 0.1 μM. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Computed Properties of 38939-88-7

The Article related to benzimidazole derivative preparation therapeutic metabotropic glutamate receptor 5 modulator, benzimidazole derivative mglur5 modulator gastrointestinal urinary nervous system disorder and other aspects.Computed Properties of 38939-88-7

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

On October 30, 2008, Glatthar, Ralf; Carcache, David published a patent.Quality Control of 2-Chloro-4-methyl-1-nitrobenzene The title of the patent was Preparation of benzimidazoles and related compounds as modulators of metabotropic glutamate receptor-5 for treating gastrointestinal, urinary, and nervous system disorders. And the patent contained the following:

The present invention relates to novel benzimidazole derivatives, their preparation, their use as pharmaceuticals and pharmaceutical compositions containing them, wherein the compounds have the Formula I (wherein X1 -X4 each independently represent CR2 or N; R2 is H, halo, OH. etc.; R1 is C1-6alkyl, C1-6halogenalkyl, C3-12cycloalkyl, etc.; B is aryl, nitrogen-containing ring, etc.; C is a 5-12-membered aromatic (un)substituted ring system that may contain hetero atoms) and salts, solvates, hydrates and N-oxides thereof. Synthetic procedures for preparing I are exemplified. Example compound II, prepared by reacting 3-chloro-5-iodo-N-2-propylbenzene-1,2-diamine and 5-chloro-6-(6-methylpyridin-3-ylamino)nicotinoyl chloride, caused 97% inhibition of mGluR5 activity at 0.1 μM. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Quality Control of 2-Chloro-4-methyl-1-nitrobenzene

The Article related to benzimidazole derivative preparation therapeutic metabotropic glutamate receptor 5 modulator, benzimidazole derivative mglur5 modulator gastrointestinal urinary nervous system disorder and other aspects.Quality Control of 2-Chloro-4-methyl-1-nitrobenzene

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

Bujok, Robert; Cmoch, Piotr; Wrobel, Zbigniew; Wojciechowski, Krzysztof published an article in 2017, the title of the article was Transition-metal-free synthesis of 3-(1-pyrrolidinyl)quinolines and 3-(1-pyrrolidinyl)quinoline 1-oxides via a one-pot reaction of 3-(1-pyrrolidinyl)crotonates with nitrobenzenes.Product Details of 38939-88-7 And the article contains the following content:

A carbanion of tert-Bu 3-(1-pyrrolidinyl)crotonate added to nitrobenzenes to form σH-adducts, which in the presence of pivaloyl chloride and triethylamine were converted into 3-(1-pyrrolidinyl)quinolines or 3-(1-pyrrolidinyl)quinoline 1-oxides depending on the nitrobenzene structure. This was the first methodol. in which a quinoline ring was constructed from a substrate bearing a pyrrolidinyl ring. Starting from optically pure enamines, the method allowed synthesis of the corresponding chiral products without racemization. The experimental process involved the reaction of 2-Chloro-4-methyl-1-nitrobenzene(cas: 38939-88-7).Product Details of 38939-88-7

The Article related to tert butyl pyrrolidinylcrotonate enantioselective diastereoselective preparation nitrobenzene cyclization, pyrrolidinyl quinolinecarboxylate preparation, quinoline oxide pyrrolidinyl preparation and other aspects.Product Details of 38939-88-7

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

On June 9, 2016, Park, Chan Hee; Lee, Sang Hwi; Im, Junhwan; Lee, Soon Ok; Kim, Jongmin; Ko, Kwang Seok; Kim, Byungho; Kong, Minjung; Kim, Mi Sun; Moon, Hyung Jo published a patent.Name: 4-Chloro-2-fluorotoluene The title of the patent was Preparation of heterocyclic derivatives for preventing or treating diseases associated with the activation of STAT3 protein. And the patent contained the following:

The title compounds I [one of X1-X4 = C(Rx1), and the others = (independently) C(Rx2) or N; one of Y and Z = S or NH, and the other = CH or N; Rx1 = L1S(:O)(:Xs)Rs (wherein Xs = O or NH; L1 = (un)subsitituted CH2 or NH; Rs = alkyl, haloalkyl, alkoxyalkyl, etc.); Rx2 = H, halo, NO2, etc.; A and B = (independently) a monocyclic- or bicyclic-saturated or unsaturated C3-10 carbocycle or 5-12 membered heterocycle; R1 = H, halo, CN, etc.; R2 = H, halo, OH, etc.; R3 = O, NH, N(alkyl), N(OH); R4 = H, alkyl; or R4 is linked to R1 to form a chain; L2 = (un)substituted (CH2)m, (CH2)nO, O, etc. (m = 0-3; n = 1-3); p = 0-4, and, when p is 2 or higher, R1 moieties are the same as or different from each other; q = 0-4, and, when q is 2 or higher, R2 moieties are the same as or different from each other] which have an inhibitory effect on the activation of STAT3 protein, and are useful for the prevention or treatment of diseases associated with the activation of STAT3 protein, were prepared E.g., a multi-step synthesis of N-(3-chloro-5-(2-(3-ethoxy-5-(trifluoromethoxy)phenyl)propan-2-yl)phenyl)-5-(2-(methylsulfonyl)propan-2-yl)benzo[b]thiophene-2-carboxamide, starting from 3-chloro-5-nitrobenzoic acid, was described. Exemplified compounds I were evaluated on their inhibitory effect on the dimerization of STAT3 and STAT1 (data given). Pharmaceutical composition comprising compound I was disclosed. The experimental process involved the reaction of 4-Chloro-2-fluorotoluene(cas: 452-75-5).Name: 4-Chloro-2-fluorotoluene

The Article related to heterocyclic amide preparation stat3 protein activation inhibitor antitumor antiinflammatory, benzothiophenecaboxamide preparation stat3 protein activation inhibitor antitumor antiinflammatory and other aspects.Name: 4-Chloro-2-fluorotoluene

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

On May 31, 2020, Onuki, Yuta; Nambu, Hisanori; Yakura, Takayuki published an article.Computed Properties of 5034-06-0 The title of the article was Ring-opening cyclization of spirocyclopropanes using sulfoxonium ylides. And the article contained the following:

Ring-opening cyclization of cyclohexane-1,3-dione-2-spirocyclopropanes I (R = H, Me, Ph; R1 = H, Me; R2 = H, Ph, 4-methylphenyl, 4-bromophenyl, n-butyl; n = 1) using dimethylsulfoxonium methylide proceeded regioselectively to produce 2,3,4,6,7,8-hexahydro-5H-1-benzopyran-5-ones II (R3 = H; n = 1) in good to high yields. The reactions of cycloheptane- and cyclopentane-1,3-dione-2-spirocyclopropanes I (R = H; R1 = H; R2 = phenyl; n = 0 or 2) could construct [7.6]- and [5.6]-fused ring systems II (R3 = H; n = 0 or 2). This reaction was also carried out using triethyl(oxo)-sulfanylium chloride, tributyl(oxo)-sulfanylium chloride, and benzyldimethyloxo-sulfanylium chloride, resulting in the formation of the corresponding 2,3-trans-disubstituted products III (R4 = Ph; R5 = Me, Pr, phenyl) and II (R = H; R1 = H; R2 = H; R3 = Ph; n = 1) in good to high yields, and it was shown that the di-Me group can act as a dummy substituent. It was found that the 2- and 3-phenyhexahydrobenzopyran-5-ones II (R = H; R1 = H; R2 = H, phenyl; n = 1) can be readily converted into 5-hydroxyflavan and 5-hydroxyisoflavan, resp. The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Computed Properties of 5034-06-0

The Article related to hexahydrobenzopyranone preparation regioselective, spirocyclopropane sulfonium ylide ring opening cyclization, flavan, isoflavan, ring-opening cyclization, spirocyclopropane, sulfoxonium ylide and other aspects.Computed Properties of 5034-06-0

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

Sone, Toshihiko; Lu, Gang; Matsunaga, Shigeki; Shibasaki, Masakatsu published an article in 2009, the title of the article was Catalytic asymmetric synthesis of 2,2-disubstituted oxetanes from ketones by using a one-pot sequential addition of sulfur ylide.Computed Properties of 5034-06-0 And the article contains the following content:

Enantiopure 2-Me-2-R-substituted oxetanes (R = n-octyl, 9-decenyl, cyclohexyl, Ph, 4-ClC6H4, 4-FC6H4, PhCH2CH2, 2-naphthyl) were synthesized from the corresponding ketones RCOMe and dimethyloxosulfonium methylide via one-pot double methylene transfer catalyzed by a heterobimetallic La/Li complex. Chiral amplification in the second step was the key to obtain oxetanes in high enantiomeric excess. The experimental process involved the reaction of trimethyloxosulphonium chloride(cas: 5034-06-0).Computed Properties of 5034-06-0

The Article related to oxetane disubstituted asym synthesis, ketone asym addition sulfur ylide heterobimetallic lanthanum lithium catalyst, oxirane kinetic resolution sulfur ylide addition lanthanum lithium catalyst and other aspects.Computed Properties of 5034-06-0

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

Bunik, Victoria I.; Artiukhov, Artem V.; Kazantsev, Alexey V.; Aleshin, Vasily A.; Boyko, Alexandra I.; Ksenofontov, Alexander L.; Lukashev, Nikolay V.; Graf, Anastasia V. published an article in 2022, the title of the article was Administration of phosphonate inhibitors of dehydrogenases of 2-oxoglutarate and 2-oxoadipate to rats elicits target-specific metabolic and physiological responses.SDS of cas: 35444-44-1 And the article contains the following content:

In vitro and in cell cultures, succinyl phosphonate (SP) and adipoyl phosphonate (AP) selectively target dehydrogenases of 2-oxoglutarate (OGDH, encoded by OGDH/OGDHL) and 2-oxoadipate (OADH, encoded by DHTKD1), resp. To assess the selectivity in animals, the effects of SP, AP, and their membrane-penetrating tri-Et esters (TESP and TEAP) on the rat brain metabolism and animal physiol. are compared. Opposite effects of the OGDH and OADH inhibitors on activities of OGDH, malate dehydrogenase, glutamine synthetase, and levels of glutamate, lysine, citrulline, and carnosine are shown to result in distinct physiol. responses. ECG is changed by AP/TEAP, whereas anxiety is increased by SP/TESP. The potential role of the ester moiety in the uncharged precursors of the 2-oxo acid dehydrogenase inhibitors is estimated TMAP is shown to be less efficient than TEAP, in agreement with lower lipophilicity of TMAP vs. TEAP. Non-monotonous metabolic and physiol. impacts of increasing OADH inhibition are revealed. Compared to the non-treated animals, strong inhibition of OADH decreases levels of tryptophan and beta-aminoisobutyrate and activities of malate dehydrogenase and pyruvate dehydrogenase, increasing the R-R interval of ECG. Thus, both metabolic and physiol. actions of the OADH-directed inhibitors AP/TEAP are different from those of the OGDH-directed inhibitors SP/TESP, with the Et ester being more efficient than Me ester. The experimental process involved the reaction of Methyl 6-chloro-6-oxohexanoate(cas: 35444-44-1).SDS of cas: 35444-44-1

The Article related to phosphonate oxoglutarate oxoadipate dehydrogenase inhibitor, 2-oxoadipate dehydrogenase, 2-oxoglutarate dehydrogenase, dhtkd1, phosphonate analog of 2-oxo acid, regulation of brain metabolism and other aspects.SDS of cas: 35444-44-1

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