Tag: M.W=200-250

Mu, Binsong; Zhang, Le; Lv, Guanghui; Chen, Kang; Wang, Ting; Chen, Jian; Huang, Tianle; Guo, Li; Yang, Zhongzhen; Wu, Yong published the artcile< Access to Phosphine-Containing Quinazolinones Enabled by Photo-Induced Radical Phosphorylation/Cyclization of Unactivated Alkenes>, Formula: C7H6BrNO2, the main research area is iridium catalyzed phosphorylation photocyclization unactivated alkene phosphine oxide phosphite; quinazolinone phosphine containing preparation.

A mild and facile photo-induced cascade radical addition/cyclization of unactivated alkenes is reported, through which a variety of biol. valuable phosphine-containing quinazolinones could be obtained in moderate to good yields. The protocol was characterized by mild conditions, broad substrate scope, and high at. economy.

Journal of Organic Chemistry published new progress about Alkenes Role: RCT (Reactant), RACT (Reactant or Reagent) (unactivated). 20776-50-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6BrNO2, Formula: C7H6BrNO2.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Liu, Yingpeng; Ho, Thanh C.; Baradwan, Mohammed; Lopez-Alberca, Maria Pascual; Iliopoulos-Tsoutsouvas, Christos; Nikas, Spyros P.; Makriyannis, Alexandros published the artcile< Synthesis of functionalized cannabilactones>, Recommanded Product: Methyl 2-bromo-4-methoxybenzoate, the main research area is cannabilactone Suzuki cross coupling reaction; CB2 selective ligands; Suzuki cross-coupling; cannabilactones; cannabinoids.

A new approach to synthesize cannabilactones using Suzuki cross-coupling reaction followed by one-step demethylation-cyclization is presented. The two key cannabilactone prototypes AM1710 and AM1714 were obtained selectively in high overall yields and in a lesser number of synthetic steps when compared to our earlier synthesis. The new approach expedited the synthesis of cannabilactone analogs with structural modifications at the four potential pharmacophoric regions.

Molecules published new progress about Cyclization. 17100-65-1 belongs to class bromides-buliding-blocks, and the molecular formula is C9H9BrO3, Recommanded Product: Methyl 2-bromo-4-methoxybenzoate.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Chiang, Pei-Chen; Kaeobamrung, Juthanat; Bode, Jeffrey W. published the artcile< Enantioselective, Cyclopentene-Forming Annulations via NHC-Catalyzed Benzoin-Oxy-Cope Reactions>, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde, the main research area is unsaturated aldehyde oxobutenoate chiral triazolium enantioselective benzoin oxy Cope; trisubstituted cyclopentene derivative stereoselective preparation; enantioselective benzoin catalyst chiral nitrogen heterocyclic carbene triazolium; oxy Cope enantioselective catalyst chiral nitrogen heterocyclic carbene triazolium.

Chiral N-heterocyclic carbene catalysts generated from triazolium salts promote the cyclopentene-forming annulation of α,β-unsaturated aldehydes and aryl-4-oxobutenoates with excellent levels of enantioinduction and preference for the cis-1,3,4-trisubstituted cyclopentene diastereomers, e.g., I. Although the observed products could arise by conjugate additions of catalytically generated homoenolates, our mechanistic and stereochem. investigations strongly support a novel reaction manifold featuring an intermol. crossed-benzoin reaction and an NHC-catalyzed oxy-Cope rearrangement.

Journal of the American Chemical Society published new progress about Aldol addition, stereoselective (intramol.). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Recommanded Product: 3-(4-Bromophenyl)acrylaldehyde.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Suchaud, Virginie; Bailly, Fabrice; Lion, Cedric; Calmels, Christina; Andreola, Marie-Line; Christ, Frauke; Debyser, Zeger; Cotelle, Philippe published the artcile< Investigation of a Novel Series of 2-Hydroxyisoquinoline-1,3(2H,4H)-diones as Human Immunodeficiency Virus Type 1 Integrase Inhibitors>, Application In Synthesis of 16426-64-5, the main research area is hydroxyisoquinolinedione preparation inhibition HIV1 integrase; structure hydroxyisoquinolinedione inhibition HIV1 integrase RNase H toxicity; mol docking hydroxyisoquinolinedione HIV1 integrase; physicochem property toxicity inhibition hERG CYP isoform hydroxyisoquinolinedione.

Hydroxyisoquinolinediones such as I (R = MeO, O2N, H2N, F, Cl, Br, F3C, NC, AcNH, PhCONH, 2-pyridinecarbonylamino, PhCH2CONH, 2-thiophenecarbonylamino; R1 = 4-FC6H4CH2, BuCH2CH2, Ph, PhCH2, 4-FC6H4, 4-FC6H4CH2CH2, 4-MeOC6H4CH2) (or their enol forms) were prepared as inhibitors of HIV-1 integrase; their inhibition of HIV-1 integrase, their anti-HIV-1 activities in human cells, their toxicities to human cells, and their inhibitions of RNase H were determined Introduction of electron-withdrawing functional groups such as a nitro moiety at position 7 of the isoquinoline ring led to a noticeable improvement in the antiviral activity of the resultant hydroxyisoquinolinediones with improved therapeutic indexes approaching those of the clin. used raltegravir while retaining potency against a panel of HIV-1 integrase mutants. The solubility, biol. permeability, transport by P-glycoprotein, inhibition of hERG and CYP isoforms, and specific cell toxicity effects of I (R = O2N; R1 = 4-FC6H4CH2) were determined

Journal of Medicinal Chemistry published new progress about Anti-HIV agents. 16426-64-5 belongs to class bromides-buliding-blocks, and the molecular formula is C7H4BrNO4, Application In Synthesis of 16426-64-5.

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

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

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

Hayashi, Yujiro; Hatano, Yutaro; Mori, Naoki published the artcile< Asymmetric Michael Reaction of Malononitrile and α,β-Unsaturated Aldehydes Catalyzed by Diarylprolinol Silyl Ether>, Electric Literature of 3893-18-3, the main research area is diarylprolinol silyl ether preparation; malononitrile unsaturated aldehyde asym Michael.

An asym. Michael reaction of malononitrile and α,β-unsaturated aldehydes catalyzed by a diarylprolinol silyl ether (NC)2CHCH(R)CH2CH(OMe)2 [R = Me, Ph, 2-furyl, etc.] was developed. Michael products were obtained in good yields and with excellent enantioselectivities without the formation of overreaction products. As a malononitrile moiety can be transformed into an alkoxy or amino carbonyl moiety by oxidative transformation, α-chiral esters or amides with all-carbon quaternary centers can be synthesized with excellent enantioselectivities.

Synlett published new progress about Michael reaction. 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Electric Literature of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Gustafson, Jeffrey L.; Lim, Daniel; Miller, Scott J. published the artcile< Dynamic Kinetic Resolution of Biaryl Atropisomers via Peptide-Catalyzed Asymmetric Bromination>, Recommanded Product: Methyl 2-bromo-5-fluorobenzoate, the main research area is dynamics kinetics resolution biaryl atropisomer peptide catalyzed asym bromination.

Despite the widespread use of axially chiral, or atropisomeric, biaryl ligands in modern synthesis and the occurrence of numerous natural products exhibiting axial chirality, few catalytic methods have emerged for the direct asym. preparation of this compound class. Here, the authors present a tripeptide-derived small-mol. catalyst for the dynamic kinetic resolution of racemic biaryl substrates. The reaction proceeds via an atropisomer-selective electrophilic aromatic substitution reaction using simple bromination reagents. The result is an enantioselective synthesis that delivers chiral nonracemic biaryl compounds with excellent optical purity and good isolated chem. yields (in most cases a >95:5 enantiomer ratio and isolated yields of 65 to 87%). A mechanistic model is advanced that accounts for the basis of selectivity observed

Science (Washington, DC, United States) published new progress about Atropisomers. 6942-39-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H6BrFO2, Recommanded Product: Methyl 2-bromo-5-fluorobenzoate.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Peng, Pan; Yan, Xingxiu; Zhang, Ke; Liu, Zhao; Zeng, Li; Chen, Yixuan; Zhang, Heng; Lei, Aiwen published the artcile< Electrochemical C-C bond cleavage of cyclopropanes towards the synthesis of 1,3-difunctionalized molecules>, Application of C7H7BrO2S, the main research area is aryl fluoropropane regioselective chemoselective preparation; aromatic cyclopropane triethylamine trihydrofluoride electrochem bond cleavage fluorination; alc aryl cyclopropane electrochem bond cleavage oxyfluorination; ether aryl cyclopropane electrochem bond cleavage oxyfluorination; methanol aryl cyclopropane electrochem bond cleavage dioxygenation.

An electrochem. C-C bond cleavage and 1,3-difuntionalization of arylcyclopropanes under catalyst-free and external-oxidant-free conditions. It involved 1,3-difluorination, 1,3-oxyfluorination and 1,3-dioxygenation of arylcyclopropanes with a high chemo- and regioselectivity by the strategic choice of nucleophiles. This protocol has good functional groups tolerance and can be scaled up. Mechanistic studies demonstrated that arylcyclopropane radical cation obtained from the anode oxidation and the subsequently generated benzyl carbonium were the key intermediates in this transformation. This development provided a scenario for constructing 1,3-difunctionalized mols.

Nature Communications published new progress about Aryl bromides Role: RCT (Reactant), RACT (Reactant or Reagent). 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Application of C7H7BrO2S.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary