Category: 98946-18-0

Coppock, Matthew B.; Warner, Candice R.; Dorsey, Brandi; Orlicki, Joshua A.; Sarkes, Deborah A.; Lai, Bert T.; Pitram, Suresh M.; Rohde, Rosemary D.; Malette, Jacquie; Wilson, Jere A.; Kearney, Paul; Fang, Kenneth C.; Law, Scott M.; Candelario, Sherri L.; Farrow, Blake; Finch, Amethist S.; Agnew, Heather D.; Heath, James R.; Stratis-Cullum, Dimitra N. published an article in 2017, the title of the article was Protein Catalyzed Capture Agents with Tailored Performance for In Vitro and In Vivo Applications.Reference of tert-Butyl trichloroacetimidate And the article contains the following content:

We report on peptide-based ligands matured through the Protein Catalyzed Capture (PCC) agent method to tailor mol. binders for in vitro sensing/diagnostics and in vivo pharmacokinetics parameters. A Vascular Endothelial Growth Factor (VEGF) binding peptide and a peptide against the Protective Antigen (PA) protein of Bacillus anthracis discovered through phage and bacterial display panning technologies, resp., were modified with click handles and subjected to iterative in situ click chem. screens using synthetic peptide libraries. Each azide-alkyne cycloaddition iteration, promoted by the resp. target proteins, yielded improvements in metrics for the application of interest. The anti-VEGF PCC was explored as a stable in vivo imaging probe. It exhibited excellent stability against proteases and a mean elimination in vivo half-life (T1/2) of 36 min. I.p. injection of the reagent results in slow clearance from the peritoneal cavity and kidney retention at extended times, while i.v. injection translates to rapid renal clearance. The ligand competed with the com. antibody for binding to VEGF in vivo. The anti-PA ligand was developed for detection assays that perform in demanding phys. environments. The matured anti-PA PCC exhibited no solution aggregation, no fragmentation when heated to 100 oC, and a > 81% binding activity for PA after heating at 90°C for 1 h. We discuss the potential of the PCC agent screening process for the discovery and enrichment of next generation antibody alternatives. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Reference of tert-Butyl trichloroacetimidate

The Article related to vegf binding peptide pet imaging agent pharmacokinetics, biological stability, peptide, protective antigen, protein catalyzed capture agent, synthetic antibody, thermal stability, vascular endothelial growth factor and other aspects.Reference of tert-Butyl trichloroacetimidate

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

On September 8, 2016, Masuda, Yuichi; Maruyama, Chitose; Kawabata, Kyuichi; Hamano, Yoshimitsu; Doi, Takayuki published an article.Application of 98946-18-0 The title of the article was Synthesis of (2S,3R,4R)-3,4-dihydroxyarginine and its inhibitory activity against nitric oxide synthase. And the article contained the following:

A synthesis of (2S,3R,4R)-3,4-dihydroxyarginine, a metabolic intermediate of streptothricin, was accomplished. The (3R,4R)-dihydroxy groups were constructed by asym. syn-dihydroxylation of (E)-alkene, which was obtained by cross-metathesis of allylamine and L-vinylglycine derivatives The synthesis of (2S,3S,4S)-3,4-dihydroxyarginine was also achieved in the same manner. The (2S,3R,4R)-3,4-dihydroxyarginine exhibited inhibitory activity against inducible nitric oxide synthase, unlike (2S,3S,4S)-3,4-dihydroxyarginine. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application of 98946-18-0

The Article related to arginine dihydroxy enantioselective diastereoselective synthesis metabolic intermediate streptothricin, nitric oxide synthase inhibitor dihydroxyarginine, allylamine vinylglycine cross metathesis alkene asym syn dihydroxylation and other aspects.Application of 98946-18-0

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

On November 15, 2019, De Luca, Stefania; Digilio, Giuseppe; Verdoliva, Valentina; Tovillas, Pablo; Jimenez-Oses, Gonzalo; Peregrina, Jesus M. published an article.Category: chlorides-buliding-blocks The title of the article was Lanthionine peptides by S-alkylation with substituted cyclic sulfamidates promoted by activated molecular sieves: Effects of the sulfamidate structure on the yield. And the article contained the following:

A green and efficient method for preparing lanthionine peptides by a highly chemoselective and stereochem. controlled procedure is presented. It involves an S-alkylation reaction, promoted by activated mol. sieves, on chiral cyclic sulfamidates, both N-protected and unprotected. Of note, the reaction yield was high also for cyclic sulfamidates bearing a free amine group, while other strategies failed to achieve a ring-opening nucleophilic reaction with N-unprotected substrates. To prove the feasibility of the procedure, the synthesis of a thioether ring B mimetic of the natural lantibiotic haloduracin β was performed. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks

The Article related to lanthionine peptide enantioselective synthesis green chem, solid phase peptide synthesis, chiral cyclic sulfamidate s alkylation thioetherification cyclization, thioether ring b preparation natural lantibiotic beta haloduracin and other aspects.Category: chlorides-buliding-blocks

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

Fandrick, Keith R.; Li, Wenjie; Zhang, Yongda; Tang, Wenjun; Gao, Joe; Rodriguez, Sonia; Patel, Nitinchandra D.; Reeves, Diana C.; Wu, Jiang-Ping; Sanyal, Sanjit; Gonnella, Nina; Qu, Bo; Haddad, Nizar; Lorenz, Jon C.; Sidhu, Kanwar; Wang, June; Ma, Shengli; Grinberg, Nelu; Lee, Heewon; Tsantrizos, Youla; Poupart, Marc-Andre; Busacca, Carl A.; Yee, Nathan K.; Lu, Bruce Z.; Senanayake, Chris H. published an article in 2015, the title of the article was Concise and practical asymmetric synthesis of a challenging atropisomeric HIV integrase inhibitor.Recommanded Product: 98946-18-0 And the article contains the following content:

A practical and efficient synthesis of a complex chiral atropisomeric HIV integrase inhibitor, I, has been accomplished. The combination of a copper-catalyzed acylation along with the implementation of the biaryl monophosphorus (BI-DIME) ligands for a ligand-controlled Suzuki cross-coupling and an unprecedented bis(trifluoromethane)sulfonamide-catalyzed tert-butylation rendered the synthesis of this complex mol. robust, safe, and economical. Furthermore, the overall synthesis was conducted in a diastereoselective fashion with respect to the imbedded atropisomer. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Recommanded Product: 98946-18-0

The Article related to bisquinoline integrase inhibitor diastereoselective preparation thermal equilibration, boronic acid aryl chloride suzuki cross coupling, suzuki couplings, acylation, asymmetric synthesis, phosphine ligands, tert-butylation and other aspects.Recommanded Product: 98946-18-0

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

David, Nadege; Pasceri, Raffaele; Kitson, Russell R. A.; Pradal, Alexandre; Moody, Christopher J. published an article in 2016, the title of the article was Formal total synthesis of diazonamide A by indole oxidative rearrangement.COA of Formula: C6H10Cl3NO And the article contains the following content:

A short formal total synthesis of the marine natural product diazonamide A is described. The route is based on indole oxidative rearrangement, and a number of options were investigated involving migration of tyrosine or oxazole fragments upon oxidation of open chain or macrocyclic precursors. The final route proceeds from 7-bromoindole by sequential palladium-catalyzed couplings of an oxazole fragment at C-2, followed by a tyrosine fragment at C-3. With the key 2,3-disubstituted indole readily in hand, formation of a macrocyclic lactam set the stage for the crucial oxidative rearrangement to a 3,3-disubstituted oxindole. Notwithstanding the concomitant formation of the unwanted indoxyl isomer, the synthesis successfully delivered, after deprotection, the key oxindole intermediate, thereby completing a formal total synthesis of diazonamide A. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).COA of Formula: C6H10Cl3NO

The Article related to natural product diazonamide a synthon total synthesis macrocyclic peptidomimetic, peptide coupling iodination oxazole tyrosine indole oxidative rearrangement macrocyclization, natural products, oxindoles, total synthesis and other aspects.COA of Formula: C6H10Cl3NO

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

On March 4, 2020, Kayser, Silke; Hansen, Jacob C.; Staudt, Markus; Moroz, Aleksandra; Larsen, Younes; Temperini, Piero; Yi, Feng; Syrenne, Jed T.; Krogsgaard-Larsen, Niels; Iliadis, Stylianos; Nielsen, Birgitte; Hansen, Kasper B.; Pickering, Darryl S.; Bunch, Lennart published an article.HPLC of Formula: 98946-18-0 The title of the article was Stereoselective Synthesis of New (2S,3R)-3-Carboxyphenyl)pyrrolidine-2-carboxylic Acid Analogues Utilizing a C(sp3)-H Activation Strategy and Structure-Activity Relationship Studies at the Ionotropic Glutamate Receptors. And the article contained the following:

Competitive antagonists for ionotropic glutamate receptors (iGluRs) are highly valuable tool compounds for studying health and disease states in the central nervous system. However, only few subtype selective tool compounds are available and the discovery of antagonists with novel iGluR subtype selectivity profiles remains a profound challenge. In this paper, we report an elaborate structure-activity relationship (SAR) study of the parental scaffold 2,3-trans-3-carboxy-3-phenyl-proline by the synthesis of 40 new analogs. Three synthetic strategies were employed with two new strategies of which one being a highly efficient and fully enantioselective strategy based on C(sp3)-H activation methodol. The SAR study led to the conclusion that selectivity for the NMDA receptors was a general trend when adding substituents in the 5′-position. Selective NMDA receptor antagonists were obtained with high potency (IC50 values as low as 200 nM) and 3-34-fold preference for GluN1/GluN2A over GluN1/GluN2B-D NMDA receptors. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).HPLC of Formula: 98946-18-0

The Article related to stereoselective preparation carboxyphenyl pyrrolidine carboxylate analog ionotropic glutamate receptor, c(sp3)−h activation, electrophysiology, ionotropic glutamate receptors, nmda receptor antagonist, proline analogues and other aspects.HPLC of Formula: 98946-18-0

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

Bendre, Shreya; Zhang, Zhengxing; Kuo, Hsiou-Ting; Rousseau, Julie; Zhang, Chengcheng; Merkens, Helen; Roxin, Aron; Benard, Francois; Lin, Kuo-Shyan published an article in 2020, the title of the article was Evaluation of Met-Val-Lys as a renal brush border enzyme-cleavable linker to reduce kidney uptake of 68Ga-labeled DOTA-conjugated peptides and peptidomimetics.Related Products of 98946-18-0 And the article contains the following content:

High kidney uptake is a common feature of peptide-based radiopharmaceuticals, leading to reduced detection sensitivity for lesions adjacent to kidneys and lower maximum tolerated therapeutic dose. In this study, we evaluated if the Met-Val-Lys (MVK) linker could be used to lower kidney uptake of 68Ga-labeled DOTA-conjugated peptides and peptidomimetics. A model compound, [68Ga]Ga-DOTA-AmBz-MVK(Ac)-OH (AmBz: aminomethylbenzoyl), and its derivative, [68Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH, coupled with the PSMA (prostate-specific membrane antigen)-targeting motif of the previously reported HTK01166 were synthesized and evaluated to determine if they could be recognized and cleaved by the renal brush border enzymes. Addnl., positron emission tomog. (PET) imaging, ex vivo biodistribution and in vivo stability studies were conducted in mice to evaluate their pharmacokinetics. [68Ga]Ga-DOTA-AmBz-MVK(Ac)-OH was effectively cleaved specifically by neutral endopeptidase (NEP) of renal brush border enzymes at the Met-Val amide bond, and the radio-metabolite [68Ga]Ga-DOTA-AmBz-Met-OH was rapidly excreted via the renal pathway with minimal kidney retention. [68Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH retained its PSMA-targeting capability and was also cleaved by NEP, although less effectively when compared to [68Ga]Ga-DOTA-AmBz-MVK(Ac)-OH. The kidney uptake of [68Ga]Ga-DOTA-AmBz-MVK(HTK01166)-OH was 30% less compared to that of [68Ga]Ga-HTK01166. Our data demonstrated that derivatives of [68Ga]Ga-DOTA-AmBz-MVK-OH can be cleaved specifically by NEP, and therefore, MVK can be a promising cleavable linker for use to reduce kidney uptake of radiolabeled DOTA-conjugated peptides and peptidomimetics. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Related Products of 98946-18-0

The Article related to renal brush border enzyme cleavable linker kidney uptake, cancer imaging and therapy, cleavable linkers, kidney uptake, neutral endopeptidase (nep), prostate-specific membrane antigen (psma), radiopharmaceuticals, renal brush border enzymes and other aspects.Related Products of 98946-18-0

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

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 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