Month: October 2022

Whitmarsh-Everiss, Thomas; Olsen, Asger Hegelund; Laraia, Luca published the artcile< Identification of Inhibitors of Cholesterol Transport Proteins Through the Synthesis of a Diverse, Sterol-Inspired Compound Collection>, Name: 2-Amino-5-bromobenzaldehyde, the main research area is cholesterol transport protein inhibitor sterol synthesis; cholesterol-transport proteins; inhibitors; library synthesis; natural products.

Cholesterol transport proteins regulate a vast array of cellular processes including lipid metabolism, vesicular and non-vesicular trafficking, organelle contact sites, and autophagy. Despite their undoubted importance, the identification of selective modulators of this class of proteins has been challenging due to the structural similarities in the cholesterol-binding site. Herein we report a general strategy for the identification of selective inhibitors of cholesterol transport proteins via the synthesis of a diverse sterol-inspired compound collection. Fusion of a primary sterol fragment to an array of secondary privileged scaffolds led to the identification of potent and selective inhibitors of the cholesterol transport protein Aster-C, which displayed a surprising preference for the unnatural-sterol AB-ring stereochem. and new inhibitors of Aster-A. We propose that this strategy can and should be applied to any therapeutically relevant sterol-binding protein.

Angewandte Chemie, International Edition published new progress about Cell membrane. 29124-57-0 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO, Name: 2-Amino-5-bromobenzaldehyde.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Adachi, Yohei; Arai, Fuka; Yamada, Kohei; Kurihara, Maho; Ohshita, Joji published the artcile< Optical Properties of Boron-Incorporated Analogues of Tetrathienoanthracene>, Related Products of 576-83-0, the main research area is borepin incorporated analog tetrathienoanthracene preparation emission fluorescence DFT; crystal structure borepin incorporated analog tetrathienoanthracene; mol structure borepin incorporated analog tetrathienoanthracene.

B-introduced aromatic systems have caught the interest of materials chemists because of their unique photophys. properties and tunable Lewis acidity. The authors prepared B-incorporated analogs of tetrathienoanthracene (TTA) containing aromatic borepin rings. Despite the low aromaticity of the borepin rings, the bis-borepins showed high chem. stability and no decomposition in air. The bis-borepins exhibited bluish fluorescence at room temperature and bright greenish phosphorescence at a low temperature The specific electronic structure of the B-incorporated analogs of TTA was revealed by comparing the photophys. properties of the bis-borepins with those of TTA and the parent mono-borepin. The electronic structure was further studied by DFT/TD-DFT calculations Titration experiments using cyanide as the anion revealed the high Lewis acidity and the turn-off fluorescence response of the bis-borepins to the addition of cyanide.

Organometallics published new progress about Anthracenes Role: PEP (Physical, Engineering or Chemical Process), PRP (Properties), SPN (Synthetic Preparation), PROC (Process), PREP (Preparation) (borepin-incorporated analogs of tetrathienoanthracene). 576-83-0 belongs to class bromides-buliding-blocks, and the molecular formula is C9H11Br, Related Products of 576-83-0.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Cai, Xinye; Du, Jun; Zhang, Lianglin; Li, Yi; Li, Baozong; Li, Hongkun; Yang, Yonggang published the artcile< Circularly polarized luminescence of single-handed helical tetraphenylethylene-silica nanotubes>, Recommanded Product: 1,2-Bis(4-bromophenyl)-1,2-diphenylethene, the main research area is circularly polarized luminescence helical tetraphenylethylene silica nanotube.

Two single-handed helical tetraphenylethylene-silica nanotubes with circularly polarized luminescence (CPL) properties and enhanced fluorescence efficiency were fabricated through a supramol. templating approach using the self-assemblies of chiral gelators as templates. This work provides a facile strategy for constructing CPL-active organic-inorganic hybrid nanomaterials with single-handed helical morphologies.

Chemical Communications (Cambridge, United Kingdom) published new progress about Circular dichroism. 184239-35-8 belongs to class bromides-buliding-blocks, and the molecular formula is C26H18Br2, Recommanded Product: 1,2-Bis(4-bromophenyl)-1,2-diphenylethene.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Daili, Farah; Ouarti, Abdelhakim; Pinaud, Marine; Kribii, Ibtihal; Sengmany, Stephane; Le Gall, Erwan; Leonel, Eric published the artcile< Nickel-Catalyzed Electrosynthesis of Aryl and Vinyl Phosphinates>, Synthetic Route of 401-78-5, the main research area is nickel catalyst electrochem coupling aryl vinyl bromide phosphinate; aryl vinyl phosphinate preparation.

A mild and useful nickel-catalyzed electrochem. phosphonylation of aryl and vinyl bromides is described. We show that alkyl H-phenylphosphinates can be coupled electrochem. with functionalized aryl and vinyl bromides using very simple conditions (Fe/Ni anode, bench-stable nickel pre-catalyst, undivided cell, galvanostatic electrolysis) to furnish the corresponding aryl and vinyl phosphinates in satisfactory to good yields. Couplings can also be applied to heteroaromatic bromides with some limitations like increased propensity to hydro-dehalogenation.

European Journal of Organic Chemistry published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 401-78-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrF3, Synthetic Route of 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Skotnitzki, Juri; Kremsmair, Alexander; Keefer, Daniel; Gong, Ye; de Vivie-Riedle, Regina; Knochel, Paul published the artcile< Stereoselective Csp3-Csp2 Cross-Couplings of Chiral Secondary Alkylzinc Reagents with Alkenyl and Aryl Halides>, Formula: C7H7BrO2S, the main research area is alkyl iodide dialkylzinc reagent alkenyl halide palladium cross coupling; chiral alkene preparation diastereoselective; cross-coupling; lithium; natural products; palladium; zinc.

The palladium-catalyzed cross-coupling reactions of chiral secondary non-stabilized dialkylzinc reagents, prepared from readily available chiral secondary alkyl iodides, with alkenyl and aryl halides were reported. This method provides α-chiral alkenes and arenes with very high retention of configuration (dr up to 98:2) and satisfactory overall yields (up to 76 % for 3 reaction steps). The configurational stability of these chiral non-stabilized dialkylzinc reagents was determined and exceeded several hours at 25 °C. DFT calculations were performed to rationalize the stereoretention during the catalytic cycle. Furthermore, the cross-coupling reaction was applied in an efficient total synthesis of the sesquiterpenes (S)- and (R)-curcumene with control of the absolute stereochem.

Angewandte Chemie, International Edition published new progress about Alkenes Role: SPN (Synthetic Preparation), PREP (Preparation). 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Formula: C7H7BrO2S.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Lin; Guo, Kai-Xin; Tian, Yu; Yang, Chang-Jiang; Gu, Qiang-Shuai; Li, Zhong-Liang; Ye, Liu; Liu, Xin-Yuan published the artcile< Copper-Catalyzed Intermolecular Enantioselective Radical Oxidative C(sp3)-H/C(sp)-H Cross-Coupling with Rationally Designed Oxazoline-Derived N,N,P(O)-Ligands>, Quality Control of 2725-82-8, the main research area is cycloalkene alkyne copper catalyst regioselective enantioselective oxidative cross coupling; cycloalkenyl alkyne preparation; alkyne aryl alkene copper catalyst enantioselective oxidative cross coupling; aryl alkyne preparation regioselective; alkynylation; anionic N,N,P(O)-ligands; copper catalysis; oxidative cross-coupling; radical asymmetric chemistry.

Here, a copper-catalyzed asym. C(sp3)-C(sp) cross-coupling of (hetero)benzylic and (cyclic)allylic C-H bonds with terminal alkynes that occurs with high to excellent enantioselectivity was reported. Critical to the success is the rational design of chiral oxazoline-derived N,N,P(O)-ligands that not only tolerate the strong oxidative conditions which were requisite for intermol. hydrogen atom abstraction (HAA) processes but also induce the challenging enantiocontrol. Direct access to a range of synthetically useful chiral benzylic alkynes and 1,4-enynes, high site-selectivity among similar C(sp3)-H bonds, and facile synthesis of enantioenriched medicinally relevant compounds make this approach very attractive.

Angewandte Chemie, International Edition published new progress about Aldehydes Role: RCT (Reactant), RACT (Reactant or Reagent). 2725-82-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H9Br, Quality Control of 2725-82-8.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhan, Yizhou; Liu, Tao; Ren, Jun; Wang, Zhongwen published the artcile< Lewis Acid-Catalyzed Intramolecular [3+2] Cross-Cycloaddition of Aziridine 2,2-Diesters with Conjugated Dienes for Construction of Aza-[n.2.1] Skeletons>, Quality Control of 89003-95-2, the main research area is Lewis acid intramol cross cycloaddition aziridine diester conjugate diene; aza skeleton preparation; aziridine; bridged ring; cycloaddition; medium-sized ring; regioselectivity.

A novel Lewis acid-catalyzed [3+2] intramol. cross-cycloaddition (IMCC) between aziridine 2,2-diesters and conjugated dienes has been developed. This is the first regiospecific IMCC of intramol. 1,3-dipolar cycloadditions of azomethine ylides with carbon=carbon double bonds, and supplies a general and efficient strategy for construction of structurally complex and diverse aza-[n.2.1] skeletons, e.g. I. The [3+2]IMCC could be carried out under mild conditions and in gram scale. More importantly, 3-alkyl-substituted aziridines were also successful. The excellent structural diversity, the facile operation and the versatile post-modifications will support the applications of the [3+2]IMCC in natural products synthesis and drugs discovery.

Chemistry – A European Journal published new progress about Aziridines Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation). 89003-95-2 belongs to class bromides-buliding-blocks, and the molecular formula is C8H4BrNO, Quality Control of 89003-95-2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Rabal, Obdulia; Sanchez-Arias, Juan A.; Cuadrado-Tejedor, Mar; de Miguel, Irene; Perez-Gonzalez, Marta; Garcia-Barroso, Carolina; Ugarte, Ana; Estella-Hermoso de Mendoza, Ander; Saez, Elena; Espelosin, Maria; Ursua, Susana; Tan, Haizhong; Wu, Wei; Xu, Musheng; Pineda-Lucena, Antonio; Garcia-Osta, Ana; Oyarzabal, Julen published the artcile< Multitarget Approach for the Treatment of Alzheimer's Disease: Inhibition of Phosphodiesterase 9 (PDE9) and Histone Deacetylases (HDACs) Covering Diverse Selectivity Profiles>, Name: Ethyl 5-bromothiophene-2-carboxylate, the main research area is Alzheimer’s disease HDAC inhibition PDE9 inhibition HDAC6 dual inhibitors; Alzheimer’s disease; HDAC6; dual inhibitors; histone deacetylase inhibition; phosphodiesterase 9 inhibition.

Here, we present a series of dual-target phosphodiesterase 9 (PDE9) and histone deacetylase (HDAC) inhibitors devised as pharmacol. tool compounds for assessing the implications of these two targets in Alzheimer’s disease (AD). These novel inhibitors were designed taking into account the key pharmacophoric features of known selective PDE9 inhibitors as well as privileged chem. structures, bearing zinc binding groups (hydroxamic acids and ortho-amino anilides) that hit HDAC targets. These substituents were selected according to rational criteria and previous knowledge from our group to explore diverse HDAC selectivity profiles (pan-HDAC, HDAC6 selective, and class I selective) that were confirmed in biochem. screens. Their functional response in inducing acetylation of histone and tubulin and phosphorylation of cAMP response element binding (CREB) was measured as a requisite for further progression into complete in vitro absorption, distribution, metabolism and excretion (ADME) and in vivo brain penetration profiling. Compound 31b, a selective HDAC6 inhibitor with acceptable brain permeability, was chosen for assessing in vivo efficacy of these first-in-class inhibitors, as well as studying their mode of action (MoA).

ACS Chemical Neuroscience published new progress about Alzheimer disease. 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Name: Ethyl 5-bromothiophene-2-carboxylate.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary