Month: November 2022

On October 1, 2016, Tiwari, Vinay Shankar; Murugula, Raghavendra; Yadav, Shyam Raj; Haq, Wahajul published an article.Recommanded Product: 98946-18-0 The title of the article was Synthesis of 4-hydroxy-2-methylproline derivatives via pyrrolidine ring assembly: Chromatographic resolution and diastereoselective synthesis approaches. And the article contained the following:

4-Hydroxy-2-methylproline diastereomers are successfully prepared without the use of an external chiral auxiliary. Dihydroxylation of the key intermediate (I) (Z = benzyloxycarbonyl) resulted in lactone (II) as a mixture of diastereomers in good yield. Mesylation, hydrogenation and concomitant intramol. cyclization of II led to the formation of both (2R,4R)- and (2R,4S)-4-hydroxy-2-methylprolines as a mixture of diastereomers. Appropriate protection followed by chromatog. separation resulted in isolation of both cis- and trans-diastereomers in enantiomerically pure form and in equal quantity. In subsequent experiments, the synthesis of the more challenging diastereomers (2R,4R)- and (2S,4S)-4-hydroxy-2-methylproline was achieved by diastereoselective iodolactonization of (R)- or (S)-allylalanine obtained after hydrolysis of intermediate I, followed by pyrrolidine ring closer under mild alk. conditions. After selective protection and deprotection, Fmoc-(2R,4R)-α-Me-Hyp(tBu)-OH (III) (Fmoc = 9-fluorenylmethoxycarbonyl), a building block suitable for solid phase peptide synthesis was obtained. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: 98946-18-0

The Article related to hydroxymethylproline enantioselective and diastereoselective synthesis solvent effect, allylalanine ring opening diastereoselective iodo lactonization reaction mechanism hydrolysis, pyrrolidine ring assembly chromatog resolution and other aspects.Recommanded Product: 98946-18-0

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

On February 21, 2022, Nonami, Reina; Morimoto, Yusei; Kanemoto, Kazuya; Yamamoto, Yasunori; Shirai, Tomohiko published an article.Name: 2-Amino-4-chlorobenzoic acid The title of the article was Cationic Iridium-Catalyzed Asymmetric Decarbonylative Aryl Addition of Aromatic Aldehydes to Bicyclic Alkenes. And the article contained the following:

An unprecedented catalytic protocol for the enantioselective decarbonylative transformation of aryl aldehydes. In this process, the decarbonylation of aldehydes catalyzed by chiral iridium complexes enabled the formation of asym. C-C bonds through the formation of an aryl-iridium intermediate. The decarbonylative aryl addition to bicyclic alkenes were fluidly performed without a stoichiometric aryl-metal reagent, such as aryl boronic acid, with a cationic iridium complex generated in-situ from Ir(cod)2(BArF4) and the sulfur-linked bis(phosphoramidite) ligand ((R,R)-S-Me-BIPAM). This reaction has broad functional group compatibility and no waste was generated, except carbon monoxide. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Name: 2-Amino-4-chlorobenzoic acid

The Article related to formylphenyl acetamide norbornene iridium catalyst enantioselective decarbonylation, norbornanyl phenyl acetamide preparation, c−h bond activation, asymmetric catalysis, cationic iridium, decarbonylation, decarbonylative arylation and other aspects.Name: 2-Amino-4-chlorobenzoic acid

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

On September 3, 2021, Li, Ling; Zhang, Shiqi; Deng, Xiongfei; Li, Guangxun; Tang, Zhuo; Zhao, Gang published an article.Quality Control of 2-Amino-4-chlorobenzoic acid The title of the article was Preparation and Application of α-Imino Ketones through One-Pot Tandem Reactions Based on Heyns Rearrangement. And the article contained the following:

A metal-free and operationally simple strategy was developed to generate α-imino ketones with high regioselectivity. Meanwhile, the method allowed for the preparation of various N,O-ketals with high regioselectivities and diastereoselectivities through cascade reactions in one pot. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Quality Control of 2-Amino-4-chlorobenzoic acid

The Article related to amine hydroxyketone regioselective diastereoselective tandem heyns rearrangement oxidation, imino ketone preparation, hydroxyketone aminoalc regioselective diastereoselective tandem heyns rearrangement oxidation, ketal preparation and other aspects.Quality Control of 2-Amino-4-chlorobenzoic acid

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

Li, Bowen; Li, Tiejun; Aliyu, Muinat A.; Li, Zhen Hua; Tang, Wenjun published an article in 2019, the title of the article was Enantioselective Palladium-Catalyzed Cross-Coupling of α-Bromo Carboxamides and Aryl Boronic Acids.Electric Literature of 98946-18-0 And the article contains the following content:

We herein report an enantioselective palladium-catalyzed cross-coupling between α-bromo carboxamides and aryl boronic acids, generating a series of chiral α-aryl carboxamides in good yields and excellent enantioselectivities. The development of a chiral P,P=O ligand was critical in overcoming the second transmetalation issue and allows the first asym. palladium-catalyzed coupling of α-bromo carbonyl compounds The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Electric Literature of 98946-18-0

The Article related to enantioselective alpha aryl carboxamide preparation palladium catalyst, cross coupling alpha bromo carboxamide arylboronic acid phosphorus ligand, asymmetric catalysis, cross-coupling, palladium, phosphorus ligands, transmetalation and other aspects.Electric Literature of 98946-18-0

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

On August 23, 2012, Buhr, Wilm; Burckhardt, Susanna; Duerrenberger, Franz; Funk, Felix; Geisser, Peter Otto; Corden, Vincent Anthony; Courtney, Stephen Martin; Davenport, Tara; Slack, Mark; Ridgill, Mark Peter; Yarnold, Christopher John; Dawson, Graham; Boyce, Susan; Ellenbroek, Albertus Antonius published a patent.Electric Literature of 82711-97-5 The title of the patent was Novel sulfonaminoquinoline derivatives as hepcidin antagonists and their preparation and use in the treatment of iron metabolic disorders. And the patent contained the following:

The invention is related to the preparation of title compounds I [R1-6 = independently H, halo, CN, (un)substituted aroxy, heterocyclyl, etc.; R7 = H, (un)substituted alk(en/yn)yl, aryl, etc.; R8 = H, NH2 and derivatives, OH and derivatives, etc.; or R6 and R8 together form a residue II or III; X = C, N; R9-12 = independently H, NO2, CO2H and derivatives, etc.; R13 = H, (un)substituted aryl, acyl, alkyl, etc.; R14, R15 = H, halo, (un)substituted alkoxycarbonyl, aminosulfonyl, etc.] and their pharmaceutically acceptable salts as hepcidin antagonists, pharmaceutical compositions containing them, and to their use as medicaments, in particular for treating iron metabolism disorders, for example, iron deficiency diseases and anemias, in particular anemias combined with chronic inflammation diseases and anemia of inflammation. Thus, reaction of 7-methyl-8-nitroquinoline with 1,1-dimethoxy-N,N-dimethylmethanamine, oxidation of dimethyl[(E)-2-(8-nitroquinolin-7-yl)ethenyl]amine, reductive amination of 8-nitroquinoline-7-carboxaldehyde with aniline, Pd/C hydrogenation of N-[(8-nitroquinolin-7-yl)methyl]phenylamine and cyclization of [7-[(phenylamino)methyl]quinolin-8-yl]amine with 1-[(1H-imidazol-1-yl)sulfonyl]-3-methyl-1H-imidazol-3-ium trifluoromethanesulfonate gave IV. Selected I were evaluated for their hepcidin antagonistic activity. From the assay, it was determined that compound IV exhibited an IC50 value of 0.46 μM towards ferroportin. The experimental process involved the reaction of 5-Fluoro-2-nitrobenzene-1-sulfonyl chloride(cas: 82711-97-5).Electric Literature of 82711-97-5

The Article related to sulfonaminoquinoline preparation hepcidin antagonist treatment iron metabolic disorder, dioxothiatriazaphenanthrene dioxothiadiazachrysene dioxoazacyclopentanaphthalene dioxothiatriazachrysene preparation anemia hepcidin antagonist and other aspects.Electric Literature of 82711-97-5

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

On December 15, 2012, Isherwood, Matthew L.; Guzzo, Peter R.; Henderson, Alan J.; Hsia, Ming Min; Kaur, Jagjit; Nacro, Kassoum; Narreddula, Venkateswara R.; Panduga, Shailaja; Pathak, Rashmi; Shimpukade, Bharat; Tan, Valentina; Xiang, Kai; Qiang, Zhu; Ghosh, Animesh published an article.Quality Control of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate The title of the article was An efficient synthesis of (7S,10R)-2-bromo-5,6,7,8,9,10-hexahydro-7,10-epiminocyclohepta[b]indole: application in the preparation and structural confirmation of a potent 5-HT6 antagonist. And the article contained the following:

(7S,10R)-5-Methyl-2-((3-(trifluoromethyl)phenyl)sulfonyl)-5,6,7,8,9,10-hexahydro-7,10-epiminocyclohepta[b]indole I is a potent 5-HT6 antagonist (h5-HT6Ki = 1.5 nM) which is derived from an epiminocyclohept[b]indole scaffold. In order to synthesize I on a multi-gram scale to support advanced biol. testing, an efficient chiral resolution of the intermediate tert-Bu 2-bromo-5,6,7,8,9,10-hexahydro-7,10-epiminocyclohepta[b]indole-11-carboxylate II was developed. After derivatizing II with (1R)-(-)-menthyl chloroformate it was found that a single diastereomer III could be isolated by selective precipitation from n-hexane. The absolute stereochem. of III was determined by X-ray crystallog. and the structure was confirmed as (7S,10R)-tert-Bu 2-bromo-5,6,7,8,9,10-hexahydro-7,10-epiminocyclohepta[b]indole-11-carboxylate. Removal of the chiral auxiliary under basic conditions afforded intermediate II in >99% enantiomeric purity and with 80% yield based on recovery from the racemic compound II. Intermediate enantiomer II was used successfully to synthesize 5-HT6 antagonist I on a multi-gram scale. The experimental process involved the reaction of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate(cas: 14602-86-9).Quality Control of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate

The Article related to methyltrifluoromethylphenylsulfonylhexahydroepiminocycloheptaindole preparation chem resolution, substitution hydrolysis, butylbromohexahydroepiminocycloheptaindolecarboxylate menthyl chloroformate separation hydrolysis methylation and other aspects.Quality Control of (1R,2S,5R)-2-Isopropyl-5-methylcyclohexyl carbonochloridate

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

On January 3, 2022, Gui, Qing-Wen; Teng, Fan; Yang, Hao; Xun, Changping; Huang, Wen-Jie; Lu, Zi-Qin; Zhu, Meng-Xue; Ouyang, Wen-Tao; He, Wei-Min published an article.Electric Literature of 89-77-0 The title of the article was Visible-Light Photosynthesis of CHF2/CClF2/CBrF2-Substituted Ring-fused Quinazolinones in Dimethyl Carbonate. And the article contained the following:

With eco-friendly and sustainable CO2-derived di-Me carbonate as the sole solvent, the visible-light-induced cascade radical reactions have been established as a green and efficient tool for constructing various CHF2/CClF2/CBrF2-substituted ring-fused quinazolinones. The experimental process involved the reaction of 2-Amino-4-chlorobenzoic acid(cas: 89-77-0).Electric Literature of 89-77-0

The Article related to ring fused quinazolinone preparation, alkenyl quinazolinone visible light cascade difluoromethylation cyclization green chem, cascade radical reactions, difluoromethylation, dimethyl carbonate, metal-free, ring-fused quinazolinones and other aspects.Electric Literature of 89-77-0

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

On November 27, 1975, Tomari, Masazumi; Miyamatsu, Hiroki; Kiyota, Keiichi; Yasuno, Akio published a patent.Product Details of 59833-69-1 The title of the patent was 2-(Alkoxycarbonylmethylphenyl)-1,3-dihydroisoindoles. And the patent contained the following:

Dihydroisoindoles I (X = H, halo; R = H, Me; R1 = C1-4 alkyl) or their salts are prepared by cyclizing o-(ClCH2)2C6H4 (II) with aminophenylacetate esters III (R2 = C1-4 alkyl). I have antiinflammatory and analgesic effects (no data). Thus, 5.24 g II was refluxed with 6 g III (X = 2-Cl, x = 5, R = H, R2 = Me) (IV) and 6.36 g Na2CO3 in DMF 4 hr to give 70% I (X = 2-Cl, x = 5, R = H, R1 = Me). The ester was hydrolyzed with KOH in MeOH to give 51.5% I (X = 2-Cl, x = 5, R = R1 = H), also prepared in 80% yield by heating II and IV with NaOH in MeOH. Similarly prepared were I (X, x, R, R1 given): 2-Cl, 5, Me, Me; 2-Cl, 5, Me, H; H, 4, H, Me; H, 4, H, H. The experimental process involved the reaction of Methyl 2-(3-amino-4-chlorophenyl)acetate(cas: 59833-69-1).Product Details of 59833-69-1

The Article related to analgesic isoindole, antiinflammatory isoindole, isoindole carboxyalkylphenyl, cyclization bischloromethylbenzene carboxyalkylaniline, chloromethylbenzene dicyclization aniline, aminophenylalkanoate cyclization bischloromethylbenzene and other aspects.Product Details of 59833-69-1

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

On April 25, 2019, Sun, Shuai-Shuai; Chen, Junyou; Zhao, Rui; Bierer, Donald; Wang, Jun; Fang, Ge-Min; Li, Yi-Ming published an article.Product Details of 98946-18-0 The title of the article was Efficient synthesis of a side-chain extended diaminodiacid for solid-phase synthesis of peptide disulfide bond mimics. And the article contained the following:

Solid-phase incorporation of diaminodiacids is one of the most effective approaches for synthesis of peptide disulfide bond mimics. One of a limitation of current diaminodiacid toolbox is that only four-atom linkage mimics are available that may not fully meet the activity optimization requirement. In this work, we developed a new diaminodiacid that contains a five-atom thioether (C-C-S-C-C) bridge for the first time. With this diaminodiacid in hand, we successfully obtained oxytocin containing new disulfide bond mimic by solid phase peptide synthesis. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to diamino diacid synthesis solid phase incorporation peptide disulfide bond, oxytocin mimic cyclic peptide solid phase synthesis oxidative cyclization, homoserine protection sulfonation substitution hydrolysis bromination thioalkylation and other aspects.Product Details of 98946-18-0

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

On March 3, 2016, Yu, Haiqing; Li, Yanxia; Ge, Yang; Song, Zhendong; Wang, Changyuan; Huang, Shanshan; Jin, Yue; Han, Xu; Zhen, Yuhong; Liu, Kexin; Zhou, Youwen; Ma, Xiaodong published an article.Computed Properties of 99-60-5 The title of the article was Novel 4-anilinoquinazoline derivatives featuring an 1-adamantyl moiety as potent EGFR inhibitors with enhanced activity against NSCLC cell lines. And the article contained the following:

With the aim of overcoming gefitinib resistance, a series of novel quinazoline derivatives bearing an adamantyl group on the aniline ring were synthesized as potent epidermal growth factor receptor (EGFR) inhibitors. Most of these analogs are comparable to gefitinib in their ability to inhibit non-small cell lung cancer (NSCLC) cell lines, and several also exhibited significantly enhanced anti-tumor potency. Specifically, compound I, with an IC50 value of 2.06 μM against A431 cells with the wild-type EGFR and of 0.009 μM against the gefitinib-sensitive cells, displayed approx. 5-fold higher potency than the lead compound to inhibit the cells harboring the EGFRT790M mutant. In addition, the mol. simulation and Western blot anal. results also indicated that these compounds effectively interfered with the EGFRT790M activity, and may serve as a new alternative structure to develop more effective antitumor agents. The experimental process involved the reaction of 2-Chloro-4-nitrobenzoic acid(cas: 99-60-5).Computed Properties of 99-60-5

The Article related to adamantyl anilinoquinazoline preparation epidermal growth factor receptor inhibitor, egfr inhibitor adamantyl anilinoquinazoline preparation, quinazoline adamantyl preparation egfr inhibitor, adamantyl, egfr, nsclc, quinazoline, t790m and other aspects.Computed Properties of 99-60-5

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