Category: 98946-18-0

Dragovich, Peter S.; Blake, Robert A.; Chen, Chunjiao; Chen, Jinhua; Chuh, Josefa; den Besten, Willem; Fan, Fang; Fourie, Aimee; Hartman, Steven J.; He, Changrong; He, Jintang; Ingalla, Ellen Rei; Kozak, Katherine R.; Leong, Steven R.; Lu, Jiawei; Ma, Yong; Meng, Lingyao; Nannini, Michelle; Oeh, Jason; Ohri, Rachana; Lewis Phillips, Gail; Pillow, Thomas H.; Rowntree, Rebecca K.; Sampath, Deepak; Vandlen, Richard; Vollmar, Breanna; Wai, John; Wertz, Ingrid E.; Xu, Keyang; Xu, Zijin; Zhang, Donglu published an article in 2018, the title of the article was Conjugation of Indoles to Antibodies through a Novel Self-Immolating Linker.Synthetic Route of 98946-18-0 And the article contains the following content:

A novel strategy to attach indole-containing payloads to antibodies through a carbamate moiety and a self-immolating, disulfide-based linker is described. This new strategy was employed to connect a selective estrogen receptor down-regulator (SERD) to various antibodies in a site-selective manner. The resulting conjugates displayed potent, antigen-dependent down-regulation of estrogen receptor levels in MCF7-neo/HER2 and MCF7-hB7H4 cells. They also exhibited similar antigen-dependent modulation of the estrogen receptor in tumors when administered i.v. to mice bearing MCF7-neo/HER2 tumor xenografts. The indole-carbamate moiety present in the new linker was stable in whole blood from various species and also exhibited good in vivo stability properties in mice. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Synthetic Route of 98946-18-0

The Article related to conjugation indole antibody selfimmolation linker, antibodies, antibody-drug conjugates, drug delivery, indole, selective estrogen receptor down-regulator, Pharmaceuticals: Formulation and Compounding and other aspects.Synthetic Route of 98946-18-0

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

Xiong, Yaoyao; Vargas Jentzsch, Andreas; Osterrieth, Johannes W. M.; Sezgin, Erdinc; Sazanovich, Igor V.; Reglinski, Katharina; Galiani, Silvia; Parker, Anthony W.; Eggeling, Christian; Anderson, Harry L. published an article in 2018, the title of the article was Spironaphthoxazine switchable dyes for biological imaging.Computed Properties of 98946-18-0 And the article contains the following content:

Recent developments in super-resolution microscopy have significantly expanded the requirements for switchable dyes, leading to demand for specially designed mol. switches. We report the synthesis and characterization of a spironaphthoxazine photochromic switch (a derivative of palatinate purple) displaying high photoconversion (85-95%) under readily accessible 405 nm light, broad absorption in the visible, and excellent fatigue resistance. The indole substituent on this spironaphthoxazine is twisted out of conjugation with the naphthalene unit, yet it is crucial for activation with visible light. The open colored merocyanine form of the spironaphthoxazine reverts to the closed form with a lifetime of 4.7 s in dichloromethane at 20°C; this thermal reversion is even faster in more polar solvents. The photochem. quantum yields for ring-opening and ring-closing are approx. 8% and 1%, resp., in dichloromethane. The ring-opening and ring-closing reactions have been characterized by time-resolved IR and transient absorption spectroscopies. Ring opening occurs rapidly (τ = 2.1 ns) and efficiently (∼90%) from the singlet excited state to form an intermediate (assigned as a cisoid merocyanine), which returns to the closed ground state (τ = 4.5 ns) in competition with relaxation to the transoid open form (τ = 40 ns). Photochem. ring closing is a faster and simpler process: the excited state proceeds to the closed spirooxazine with a time constant of 0.28 ns. This photochromic switch can be used in conjunction with com. fluorescent dyes to create a small-mol. switchable fluorescent dyad that shows high contrast and good fatigue resistance in living cells. These properties make the dyads suitable for application in RESOLFT microscopy. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Computed Properties of 98946-18-0

The Article related to spironaphthoxazine switchable dye biol imaging, Biochemical Methods: Spectral and Related Methods and other aspects.Computed Properties of 98946-18-0

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

On March 31, 2020, Ohsawa, Kosuke; Zhao, Hongbin; Tokunaga, Takuya; Thomas, Carys; Ganesan, A.; Masuda, Yuichi; Doi, Takayuki published an article.Category: chlorides-buliding-blocks The title of the article was Stereoselective synthesis of protected L-allo-enduracididine and L-enduracididine via asymmetric nitroaldol reaction. And the article contained the following:

The diastereoselecetive and scalable synthesis of cyclic guanidine-containing nonproteinoginic amino acids, enduracididines, has been achieved. Both diastereomers, L-allo-enduracididine and L-enduracididine, were prepared via catalyst-controlled asym. nitroaldol reaction with the aldehyde precursor derived from L-aspartic acid. The cyclic guanidine of di-Cbz-protected (Cbz = benzyloxycarbonyl) L-allo-enduracididine was fully protected with an allyl group to suppress nucleophilic side reactions. Introduced allyl group was efficiently removed via π-allylpalladium chem. without attaching the Cbz group on the cyclic guanidine moiety. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Category: chlorides-buliding-blocks

The Article related to enduracididine enantioselective synthesis cyclic guanidine containing amino acid, aspartic acid aldehyde nitroaldol reaction cobalt catalyst, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Category: chlorides-buliding-blocks

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

On April 30, 2020, Leppkes, Jakob; Hohmann, Thomas; Koksch, Beate published an article.Formula: C6H10Cl3NO The title of the article was Improved enantioselective gram scale synthesis route to N-Fmoc-protected monofluoroethylglycine. And the article contained the following:

Fluorine, as a substituent in amino acids, has found its way into peptide and protein engineering. The basis for the use of this valuable tool is the synthetic accessibility of various fluorinated amino acids as building blocks of peptides and proteins. In this context, we present a straightforward eight-step synthesis of N-Fmoc-L-monofluoroethylglycine (MfeGly) via homoserine (Hse) as intermediate and using various nucleophilic fluorination strategies. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Formula: C6H10Cl3NO

The Article related to amino acid fluoroethylglycine fmoc protected enantioselective synthesis, glycine nucleophilic fluorination homoserine solvent effect, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Formula: C6H10Cl3NO

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

On January 11, 2018, Zlatopolskiy, Boris D.; Zischler, Johannes; Schaefer, Dominique; Urusova, Elizaveta A.; Guliyev, Mehrab; Bannykh, Olesia; Endepols, Heike; Neumaier, Bernd published an article.Electric Literature of 98946-18-0 The title of the article was Discovery of 7-[18F]Fluorotryptophan as a Novel Positron Emission Tomography (PET) Probe for the Visualization of Tryptophan Metabolism in Vivo. And the article contained the following:

Tryptophan and its metabolites are involved in different physiol. and pathophysiol. processes. Consequently, positron emission tomog. (PET) tracers addressing tryptophan metabolic pathways should allow the detection of different pathologies like neurol. disorders and cancer. Herein we report an efficient method for the preparation of fluorotryptophans labeled in different positions with 18F and their biol. evaluation. 4-7-[18F]Fluorotryptophans ([18F]FTrps) were prepared according to a modified protocol of alc.-enhanced Cu-mediated radiofluorination in 30-53% radiochem. yields. In vitro experiments demonstrated high cellular uptake of 4-7-[18F]FTrps in different tumor cell lines. 4, 5-, And 6-[18F]FTrps, although stable in vitro, suffered from rapid in vivo defluorination. In contrast, 7-[18F]FTrp demonstrated a high in vivo stability and enabled a clear delineation of serotonergic areas and melatonin-producing pineal gland in rat brains. Moreover 7-[18F]FTrp accumulated in different tumor xenografts in a chick embryo CAM model. Thus, 7-[18F]FTrp represents a highly promising PET probe for imaging of Trp metabolism The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Electric Literature of 98946-18-0

The Article related to alc enhanced copper mediated radiofluorination radiofluorinated tryptophan preparation, pet tracer imaging tryptophan metabolism, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Electric Literature of 98946-18-0

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

On April 30, 2015, Hudson, Alex S.; Caron, Laurent; Colgin, Neil; Cobb, Steven L. published an article.Related Products of 98946-18-0 The title of the article was A direct method for the synthesis of orthogonally protected furyl- and thienyl- amino acids. And the article contained the following:

The synthesis of unnatural amino acids plays a key part in expanding the potential application of peptide-based drugs and in the total synthesis of peptide natural products. Herein, we report a direct method for the synthesis of orthogonally protected 5-membered heteroaromatic amino acids. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Related Products of 98946-18-0

The Article related to negishi cross coupling heteroaromatic amino acid preparation, Amino Acids, Peptides, and Proteins: Amino Acids and other aspects.Related Products of 98946-18-0

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

Humpert, Swen; Omrane, Mohamed A.; Urusova, Elizaveta A.; Gremer, Lothar; Willbold, Dieter; Endepols, Heike; Krasikova, Raisa N.; Neumaier, Bernd; Zlatopolskiy, Boris D. published an article in 2021, the title of the article was Rapid 18F-labeling via Pd-catalyzed S-arylation in aqueous medium.Formula: C6H10Cl3NO And the article contains the following content:

Radiolabeling of thiol-containing substrates via Pd-catalyzed S-arylation with 2-[18F]fluoro-5-iodopyridine, which is readily accessible using the “minimalist” radiofluorination method, is reported. The practicality of the procedure was confirmed by preparation of a novel PSMA-specific PET-tracer as well as labeling of glutathione, Aβ oligomer-binding RD2 peptide, bovine serum albumin and PSMA I&S. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Formula: C6H10Cl3NO

The Article related to radiofluorinated amino acid peptide preparation pet tracer, fluoro iodopyridine thiol arylation palladium catalyst, Heterocyclic Compounds (One Hetero Atom): Pyridines and other aspects.Formula: C6H10Cl3NO

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

On February 28, 2019, Modemann, Daniel J.; Zlatopolskiy, Boris D.; Urusova, Elizaveta A.; Zischler, Johannes; Craig, Austin; Ermert, Johannes; Guliyev, Mehrab; Endepols, Heike; Neumaier, Bernd published an article.Application In Synthesis of tert-Butyl trichloroacetimidate The title of the article was 2-[ 18 F]Fluorophenylalanine: Synthesis by Nucleophilic 18 F-Fluorination and Preliminary Biological Evaluation. And the article contained the following:

2-[ 18F]Fluorophenylalanine (2-[ 18F]FPhe), a promising PET tracer for imaging of cerebral infarction and tumors, was efficiently prepared from an easily accessible iodonium salt precursor using Cu-mediated radiofluorination under ‘low base’ or ‘minimalist’ conditions. Whereas significant racemization was initially observed if the ‘minimalist’ protocol was applied for radiolabeling, it was completely suppressed by the careful adjustment of 18F -preprocessing. The initial biol. study revealed a higher uptake of 2-[ 18F]FPhe in different tumor cells in comparison to that of [ 18F]FET. In contrast to 4-[ 18F]FPhe, which suffered from rapid defluorination in vivo, 2-[ 18F]FPhe demonstrated a sufficient in vivo stability. Conclusively, 2-[ 18F]FPhe is a promising PET probe that is now readily available using Cu-mediated radiofluorination under ‘minimalist’ or ‘low base’ conditions. The simplicity of the translation of the proposed procedures to automated synthesis modules allows a broad biol. evaluation of 2-[ 18F]FPhe. Notably, a novel protocol for the preparation of N-Boc protected amino acids from the resp. Ni-Schiff base complexes was developed that avoided application of strongly acidic conditions. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Application In Synthesis of tert-Butyl trichloroacetimidate

The Article related to fluorine 18 fluorophenylalanine preparation pet imaging cerebral infarction tumor, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Application In Synthesis of tert-Butyl trichloroacetimidate

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

On December 22, 2016, Tamborini, Lucia; Chen, Ying; Foss, Catherine A.; Pinto, Andrea; Horti, Andrew G.; Traynelis, Stephen F.; De Micheli, Carlo; Mease, Ronnie C.; Hansen, Kasper B.; Conti, Paola; Pomper, Martin G. published an article.Product Details of 98946-18-0 The title of the article was Development of Radiolabeled Ligands Targeting the Glutamate Binding Site of the N-Methyl-D-aspartate Receptor as Potential Imaging Agents for Brain. And the article contained the following:

Abnormal activity of various N-methyl-D-aspartate receptor (NMDAR) subtypes has been implicated in a wide variety of neurol. disorders such as Alzheimer’s disease, schizophrenia, and epilepsy. Imaging agents for PET and SPECT that target NMDARs in a subtype-selective fashion may enable better characterization of those disorders and enhance drug development. On the basis of a pyrazoline derivative that demonstrated neuroprotective effects in vivo, we synthesized a series of para-substituted analogs and measured their affinities to various NMDAR subtypes. Compounds 4a-c and 4e showed greater, nanomolar affinity for the GluN1/2A subtype vs. GluN1/2B. Dicarbomethoxy (pro-drug) analogs of [124/125I]4d and [11C]4e (i.e., [124/125I]11d and [11C]11e) were generated and tested for NMDAR binding specificity in ex vivo autoradiog. and brain biodistribution studies. Although NMDAR-specific binding could be demonstrated for [125I]11d and [11C]11e through autoradiog. and biodistribution studies, imaging of neither [124I]11d nor [11C]11e could demonstrate brain penetration sufficient for detection by PET. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Product Details of 98946-18-0

The Article related to preparation nmda receptor targeting radiolabeled ligand brain imaging, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Product Details of 98946-18-0

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

On February 21, 2020, Adams, Casey J.; Krueger, Ruby; Meade, Thomas J. published an article.Quality Control of tert-Butyl trichloroacetimidate The title of the article was A Multimodal Ca(II) Responsive Near IR-MR Contrast Agent Exhibiting High Cellular Uptake. And the article contained the following:

Ca(II) ions are critical for the proper function of neurons by contributing to synaptic signaling and regulating neuronal plasticity. Dysregulation of Ca(II) is associated with a number of pathologies that cause neurodegeneration; therefore the ability to monitor Ca(II) intracellularly is an important target for mol. imaging. Contrast-enhanced MR imaging is a promising modality for imaging changes in Ca(II) concentrations However, the majority of Ca(II) responsive MR agents are limited to the extracellular space or hindered by poor cellular uptake. Here, we describe a new class of multimodal, bioresponsive Ca(II) magnetic resonance agents that are coupled to the NIR probe IR-783. This new design is based on previous generations of our Ca(II) MR agents but overcomes two significant challenges: (1) the presence of the NIR probe dramatically increases cellular uptake of the agent and (2) provides histol. validation of the MR signal using NIR fluorescence imaging. IR-783 targets organic anion transporter polypeptides, and we demonstrate that the agents are not toxic in HT-22 or U-87 MG cells up to 20μM. The cellular uptake of complex 1 was measured to be greater than 16 fmol per cell (where ∼1 fmol/cell is detectable in acquired MR images). Complex 1 is simultaneously detectable by both MR and NIR fluorescence imaging in vitro and is activated (turned on) by intracellular Ca(II) at concentrations between 1 and 10μM. The experimental process involved the reaction of tert-Butyl trichloroacetimidate(cas: 98946-18-0).Quality Control of tert-Butyl trichloroacetimidate

The Article related to calcium nearir mr contrast agents preparation cancer imaging, Radiation Biochemistry: Disease Diagnosis and Therapy and other aspects.Quality Control of tert-Butyl trichloroacetimidate

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