Month: December 2022

Lahnif, Hanane published the artcileHybrid Chelator-Based PSMA Radiopharmaceuticals: Translational Approach, Related Products of catalysis-chemistry, the publication is Molecules (2021), 26(21), 6332, database is CAplus and MEDLINE.

Prostate-specific membrane antigen (PSMA) has been extensively studied in the last decade. It became a promising biol. target in the diagnosis and therapy of PSMA-expressing cancer diseases. Although there are several radiolabeled PSMA inhibitors available, the search for new compounds with improved pharmacokinetic properties and simplified synthesis is still ongoing. In this study, we developed PSMA ligands with two different hybrid chelators and a modified linker. Both compounds have displayed a promising pharmacokinetic profile. DATA5m.SA.KuE and AAZTA5.SA.KuE were synthesized. DATA5m.SA.KuE was labeled with gallium-68 and radiochem. yields of various amounts of precursor at different temperatures were determined Complex stability in phosphate-buffered saline (PBS) and human serum (HS) was examined at 37 ¡ãC. Binding affinity and internalization ratio were determined in in vitro assays using PSMA-pos. LNCaP cells. Tumor accumulation and biodistribution were evaluated in vivo and ex vivo using an LNCaP Balb/c nude mouse model. All experiments were conducted with PSMA-11 as reference DATA5m.SA.KuE was synthesized successfully. AAZTA5.SA.KuE was synthesized and labeled according to the literature. Radiolabeling of DATA5m.SA.KuE with gallium-68 was performed in ammonium acetate buffer (1 M, pH 5.5). High radiochem. yields (>98%) were obtained with 5 nmol at 70 ¡ãC, 15 nmol at 50 ¡ãC, and 60 nmol (50 ¦Ìg) at room temperature [68Ga]Ga-DATA5m.SA.KuE was stable in human serum as well as in PBS after 120 min. PSMA binding affinities of AAZTA5.SA.KuE and DATA5m.SA.KuE were in the nanomolar range. PSMA-specific internalization ratio was comparable to PSMA-11. In vivo and ex vivo studies of [177Lu]Lu-AAZTA5.SA.KuE, [44Sc]Sc-AAZTA5.SA.KuE and [68Ga]Ga-DATA5m.SA.KuE displayed specific accumulation in the tumor along with fast clearance and reduced off-target uptake. Both KuE-conjugates showed promising properties especially in vivo allowing for translational theranostic use.

Molecules published new progress about 140-28-3. 140-28-3 belongs to catalysis-chemistry, auxiliary class Benzenes, name is N1,N2-Dibenzylethane-1,2-diamine, and the molecular formula is C16H20N2, Related Products of catalysis-chemistry.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Vastakaite, Greta published the artcilePeptide-Catalyzed Stereoselective Conjugate Addition Reaction of Aldehydes to C-Substituted Maleimides, HPLC of Formula: 71989-31-6, the publication is Chemistry – A European Journal (2022), 28(18), e202200215, database is CAplus and MEDLINE.

Catalytic stereoselective additions with maleimides I (R = C₆H₅, 4-ClC₆H₄, 2-BrC₆H₄, etc.) are useful one-step reactions to yield chiral succinimides II (R¹ = CH₃, CH₂CH₃, CH₂C₆H₅, etc.), mols. that are widespread among therapeutically active compounds but challenging to prepare when the maleimide is C-substituted. The tripeptide H-Pro-Pro-Asp-NHC₁₂H₂₅ as a catalyst for conjugate addition reactions between aldehydes R¹CH₂CHO and C-substituted maleimides I to form succinimides II with three contiguous stereogenic centers in high yields and stereoselectivities has been described. The peptidic catalyst is so chemoselective that no protecting group is needed at the imide nitrogen of the maleimides I. Derivatization of the succinimides was straightforward and provided access to chiral pyrrolidines, lactones e.g., III, and lactams. Kinetic studies, including a Hammett plot, provided detailed insight into the reaction mechanism.

Chemistry – A European Journal published new progress about 71989-31-6. 71989-31-6 belongs to catalysis-chemistry, auxiliary class Amino acide derivatives,pyrrolidine, name is Fmoc-Pro-OH, and the molecular formula is C6H10N2, HPLC of Formula: 71989-31-6.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Ma, Kai Kai published the artcileFunctional and physical properties of commercial pulse proteins compared to soy derived protein, COA of Formula: C5H11NO2S, the publication is Future Foods (2022), 100155, database is CAplus.

In this study, the techno-functional and phys. attributes of various com. available pulse protein isolates were compared with those of soy protein isolate to evaluate their potential application as replacer for soy proteins in liquid and solid food formulations such as meat and dairy analogs. The water holding capacity, oil holding capacity, gelation properties, emulsifying properties, and color of faba bean (FPI), pea (PPI), lentil (LPI), and soy (SPI) protein isolates were therefore measured. SPI had a significantly higher water holding capacity (7.6 g/g) than the pulse protein isolates (2.2-5.1 g/g), but similar oil holding capacities were identified for SPI, FPI, and LPI. Especially LPI was more effective in droplet size reduction already at low concentrations (0.1-0.2%) compared to all other tested proteins, whereas FPI showed similar droplet size reduction efficiencies than SPI at higher concentrations (2-5%). Nevertheless, all of the plant proteins were capable of forming relatively small oil droplets (D32 = 1-3¦Ìm) at a protein-to-oil ratio of 1:10. Finally, FPI exhibited similar min. gelling concentrations to SPI, and especially LPI had a low coloring potential.

Future Foods published new progress about 63-68-3. 63-68-3 belongs to catalysis-chemistry, auxiliary class Natural product, name is (S)-2-Amino-4-(methylthio)butanoic acid, and the molecular formula is C5H11NO2S, COA of Formula: C5H11NO2S.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Xiong, Yang published the artcileVisible Light-Mediated Dearomative Hydrogen Atom Abstraction/ Cyclization Cascade of Indoles, Quality Control of 118-90-1, the publication is Angewandte Chemie, International Edition (2022), 61(18), e202200555, database is CAplus and MEDLINE.

The photochem. synthesis of yet unknown 2-oxospiro[azetidine-3,3′-indolines] (17 examples, 80-95% yield), 2,4-dioxospiro[azetidine-3,3′-indolines] (eight examples, 87-97% yield), and 1-oxo-1,3-dihydrospiro[indene-2,3′-indolines] (17 examples, 85-97% yield) is described. Starting from readily accessible 3-substituted indoles, a dearomatization of the indole core was accomplished upon irradiation at ¦Ë=420 nm in the presence of thioxanthen-9-one (10 mol%) as the sensitizer. Based on mechanistic evidence (triplet energy determination, deuteration experiments, byproduct anal.) it is proposed that the reaction proceeds by energy transfer via a 1,4- or 1,5-diradical intermediate. The latter intermediates are formed by excited state hydrogen atom transfer from suitable alkyl groups within the C3 substituent to the indole C2 carbon atom. Subsequent ring closure proceeds with pronounced diastereoselectivity to generate a 4- or 5-membered spirocyclic dearomatized product with several options for further functionalization.

Angewandte Chemie, International Edition published new progress about 118-90-1. 118-90-1 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Natural product, name is 2-Methylbenzoic acid, and the molecular formula is C7H11N, Quality Control of 118-90-1.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Tomazin, Ursa published the artcileCombinatorial Synthesis of Acacen-Type Ligands and Their Coordination Compounds, Application In Synthesis of 10517-44-9, the publication is ACS Combinatorial Science (2017), 19(6), 386-396, database is CAplus and MEDLINE.

A highly modular synthetic method for the preparation of acacen-type ligands and their coordination compounds was developed. 46 Acacen-type ligands were synthesized by a combinatorial acid-catalyzed transamination between six primary diamines and eight enaminones. The bis-enaminone products were used as tetradentate ligands for coordination of copper(II), nickel(II), cobalt(II), and palladium(II). Dependence of the preferred E- or Z-configuration of the enaminone ligand on the ¦Á-substituent of the enaminone moiety in solution was determined by NMR and confirmed by x-ray diffraction. The copper(II) complexes were tested for their suitability as catalysts in 3 + 2 cycloaddition of azomethine imine to Me propiolate.

ACS Combinatorial Science published new progress about 10517-44-9. 10517-44-9 belongs to catalysis-chemistry, auxiliary class Salt,Amine,Aliphatic hydrocarbon chain, name is Propane-1,3-diamine dihydrochloride, and the molecular formula is C7H8INO, Application In Synthesis of 10517-44-9.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Wang, Honggen published the artcileMild Rh(III)-catalyzed C-H activation and annulation with alkyne MIDA boronates: short, efficient synthesis of heterocyclic boronic acid derivatives, Recommanded Product: O-Pivaloylhydroxylamine trifluoromethanesulfonate, the publication is Journal of the American Chemical Society (2012), 134(48), 19592-19595, database is CAplus and MEDLINE.

¦Á-Alkynyl MIDA boronate complex HCú·CB[(OCOCH₂)₂NMe-N,O,O’] (2a) reacts with substituted N-pivaloyloxybenzamides giving R-1(2H)-isoquinolinone-substituted MIDA boronate RC₉H₅N(1-O)-3-B[(OCOCH₂)₂NMe-N,O,O’] (3a–q, R = H, 6-Me, 6-^tBu, 6-Ph, 6-OMe, 6-halo, 6-CF₃, 6-CN, 6-CO₂Me, 6-NO₂, 7-Me, 7-CF₃, 7-I, 7-OMe); annelated furan, thiophene and indole derivatives were also prepared The annelation is catalyzed by rhodium half-sandwich dimer [Rh₂Cp^*₂(¦Ì-Cl)₂Cl₂] in the presence of a base, CsOPiv and copper acetate cocatalyst. Taking advantage of Rh(III)-catalyzed C-H activation reactions, we have developed a mild, short, and efficient method for the synthesis of bench-stable 3-isoquinolone MIDA boronates. The reaction is practical and scalable. The product formed has been applied in the Suzuki-Miyaura reaction with high efficiency. This strategy has also been successfully expanded to the synthesis of MIDA boronate functionalized heterocycles such as isoquinoline, pyrrole, and indole.

Journal of the American Chemical Society published new progress about 1293990-73-4. 1293990-73-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is O-Pivaloylhydroxylamine trifluoromethanesulfonate, and the molecular formula is C37H30ClIrOP2, Recommanded Product: O-Pivaloylhydroxylamine trifluoromethanesulfonate.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Brunner, Otto published the artcileSynthesis of 1-methyl-2-ethyl- and 1-ethyl-2-methylnaphthalene, Application of 2-Methyl-4-phenylbutanoic acid, the publication is Monatshefte fuer Chemie (1934), 76-9, database is CAplus.

PhCH₂CH₂Br and EtCH(CO₂H)₂ with Na in PhMe give di-Et (¦Â-phenylethyl)ethylmalonate, b₁₁ 186-7¡ã; hydrolysis and removal of CO₂ gives ¦Ã-phenyl-¦Á-ethylbutyric acid, b₁₁ 172-3¡ã; concentrated H₂SO₄ gives 2-ethyl-1-keto-1,2,3,4-tetrahydronaphthalene, b₁₁ 140-5¡ã; MeMgI gives 1-methyl-2-ethyl-¦¤¹-dihydronaphthalene, b₁₁ 135-45¡ã; heating with S at 260-90¡ã for 1 hr. gives 1-methyl-2-ethylnaphthalene, b₁₁ 140-5¡ã (picrate, orange, m. 97¡ã; styphnate, yellow, m. 114¡ã). ¦Ã-Phenyl-¦Á-methylbutyric acid, b₁₁ 155-65¡ã; concentrated H₂SO₄ gives 2-methyl-1-keto-1,2,3,4-tetrahydronaphthalene, b11 140-50¡ã, which yields with EtMgBr, as above, 1-ethyl-2-methylnaphthalene, b₁₁ 135-45¡ã (picrate, golden yellow, m. 110-1¡ã; styphnate, yellow, m. 141¡ã).

Monatshefte fuer Chemie published new progress about 1949-41-3. 1949-41-3 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene, name is 2-Methyl-4-phenylbutanoic acid, and the molecular formula is C11H14O2, Application of 2-Methyl-4-phenylbutanoic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Rowles, Ian published the artcileEngineering of phenylalanine ammonia lyase from Rhodotorula graminis for the enhanced synthesis of unnatural L-amino acids, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid, the publication is Tetrahedron (2016), 72(46), 7343-7347, database is CAplus.

Phenylalanine ammonia lyase (PAL) catalyzes the reversible non-oxidative deamination of phenylalanine to trans-cinnamic acid and ammonia. Analogs of L-phenylalanine are incorporated as pharmacophores in several peptidomimetic drug mols. and are therefore of particular interest to the fine chem. industry. PAL from Rhodotorula graminis (RgrPAL) has shown an ability to accept analogs of L-phenylalanine. Our aim was to increase enzymic activity with directed evolution towards a specific non-natural substrate through the cloning and over-production of PAL in Escherichia coli. The identified variants of RgrPAL with significantly showed more catalytic efficient compared to the wild-type enzyme. These variants were used in a preparative scale biotransformation resulting in a 94% conversion to L-4-Br-phenylalanine (>99% ee).

Tetrahedron published new progress about 1772-76-5. 1772-76-5 belongs to catalysis-chemistry, auxiliary class Benzenes, name is (E)-3-(3-Nitrophenyl)acrylic acid, and the molecular formula is C9H7NO4, Recommanded Product: (E)-3-(3-Nitrophenyl)acrylic acid.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Shostenko, A. G. published the artcileRadiation-initiated reaction of ethylene with carboxylic acids, Product Details of C10H20O2, the publication is Khimiya Vysokikh Energii (1976), 10(4), 371-3, database is CAplus.

In the radiochem. telomerization of C2H4 with RCO2H (R = C1-7 n-alkyl) the activation energy of chain isomerization was greater than the activation energies of chain growth and chain transfer, which were equal. A steric effect was observed as the chain grew.

Khimiya Vysokikh Energii published new progress about 3115-28-4. 3115-28-4 belongs to catalysis-chemistry, auxiliary class Aliphatic Chain, name is 2-Butylhexanoic acid, and the molecular formula is C10H16O2, Product Details of C10H20O2.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia

Linkova, Elena I. published the artcileThe study of the reaction paths of 4-aryl-4-oxobutanoic acids with terminal aliphatic N,N-diamines, HPLC of Formula: 2051-95-8, the publication is Arabian Journal of Chemistry (2021), 14(10), 103350, database is CAplus.

Bicyclic pyrroloimidazolones and pyrrolopyrimidinones were synthesized by reacting aryl-substituted 4-oxobutanoic acids with aliphatic binucleophiles with different alkyl chain lengths using a sealed vessels reactor (SVR). By varying the synthesis conditions, the reaction path was studied and formed intermediates were isolated. The structures of the obtained compounds were proved using a set of FTIR, ¹H, ¹³C NMR spectroscopy methods and X-ray diffraction data. Temperature and pressure changes data collected during the syntheses were analyzed and assigned to the processes which occurred inside the vials. It was shown that the reaction of 4-aryl-4-oxobutanoic acids with terminal aliphatic N,N-diamines starts from the formation of corresponded (AlkN₂)²⁺An^2- salts followed by two subsequent dehydration processes giving rise to the corresponding amides and, finally, heterocycles of pyrroloimidazolone and pyrrolopyrimidinone series.

Arabian Journal of Chemistry published new progress about 2051-95-8. 2051-95-8 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ketone, name is 3-Benzoylpropionicacid, and the molecular formula is C10H10O3, HPLC of Formula: 2051-95-8.

Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia