Month: October 2022

Cao, Qingxiang; Luo, Jie; Zhao, Xiaodan published the artcile< Chiral Sulfide Catalysis for Desymmetrizing Enantioselective Chlorination>, Recommanded Product: (2,6-Dibromophenyl)methanol, the main research area is chiral sulfide catalyzed desymmetrizing enantioselective chlorination aryl olefin; tetralin enantioselective diastereoselective synthesis; tricyclic hexahydrophenalene enantioselective diastereoselective synthesis; spiro nitrogen heterocycle synthesis; Lewis base catalysis; chlorination; cyclizations; olefins; synthetic methods.

An unprecedented chiral sulfide catalyzed desymmetrizing enantioselective chlorination is disclosed. Various aryl-tethered diolefins and diaryl-tethered olefins afforded tetralins and tricyclic hexahydrophenalene derivatives, resp., bearing multiple stereogenic centers in high yields with excellent enantio- and diastereoselectivities [e.g., I → II (91%, 93% ee, 31:1 d.r.) in presence of sulfide III, DCDMH as Cl+ reagent and Tf2NH as acid in CH2Cl2]. In contrast, the tertiary amine catalyst (DHQD)2PHAL led to a diastereomeric product. The products could be transformed into a variety of compounds, such as spiro-N-heterocycles.

Angewandte Chemie, International Edition published new progress about Alkadienes Role: RCT (Reactant), SPN (Synthetic Preparation), RACT (Reactant or Reagent), PREP (Preparation) (aryl-tethered diolefins). 1013031-65-6 belongs to class bromides-buliding-blocks, and the molecular formula is C7H6Br2O, Recommanded Product: (2,6-Dibromophenyl)methanol.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Zhou, Sha; Zhou, Shaa; Xie, Yong-Tao; Jin, Ru-Yi; Meng, Xiang-De; Zhang, Dong-Kai; Hua, Xue-Wen; Liu, Ming; Wu, Chang-Chun; Xiong, Li-Xia; Zhao, Yu; Li, Zheng-Ming published the artcile< The exploration of chiral N-cyano sulfiliminyl dicarboxamides on insecticidal activities>, Computed Properties of 82-73-5, the main research area is chiral cyano sulfiliminyl dicarboxamide preparation insecticide Pseudaletia larva.

Due to new mechanism of action and ecofriendly characteristics, dicarboxamide insecticides have attracted more and more attentions in modern pest management. A series of 20 dual chiral N-cyano sulfilimines containing two centers (carbon and sulfur) were designed and synthesized. All title compounds were determined by 1H NMR, high-resolution mass spectrometry (HRMS) and optical polarimeter. The preliminary results indicated that some of them exhibited favorable insecticidal activities against oriental armyworm (Pseudaletia separata Walker). These isomers exhibited different impact on activity following the sequence as (Sc, Ss) ≥ (Sc, Rs), and the rule of title compounds’ activity against oriental armyworm was 3-CF3 ≥ 2-CH3-4-Cl >2, 3, 4-trifluro in the anilide moiety. The results indicated that these groups such as 3-CF3, 2-CH3-4-Cl or 2, 3, 4-trifluro were inefficient to replace heptafluoroisopropyl group for high larvicidal activity, which provided some guidance for the further modifications of sulfiliminyl dicarboxamides.

Chinese Chemical Letters published new progress about Insecticides. 82-73-5 belongs to class bromides-buliding-blocks, and the molecular formula is C8H3BrO3, Computed Properties of 82-73-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Vechorkin, Oleg; Godinat, Aurelien; Scopelliti, Rosario; Hu, Xile published the artcile< Cross-Coupling of Nonactivated Alkyl Halides with Alkynyl Grignard Reagents: A Nickel Pincer Complex as the Catalyst>, Application In Synthesis of 639520-70-0, the main research area is alkyl halide alkynyl Grignard cross coupling nickel catalysis.

Alkynes containing nonactivated alkyl groups, especially those with β-hydrogen atoms, are difficult to synthesize. In this paper, we have disclosed the first general nickel-catalyzed cross-coupling of nonactivated alkyl halides with alkynyl Grignard reagents. The wide scope and high functional group tolerance makes the method attractive for the streamlined preparation of alkynes containing nonactivated alkyl groups. At this moment, only primary alkyl halides can be coupled. Methods to couple secondary alkyl halides are currently being developed in our laboratory

Angewandte Chemie, International Edition published new progress about Cross-coupling reaction. 639520-70-0 belongs to class bromides-buliding-blocks, and the molecular formula is C12H16BrNO2, Application In Synthesis of 639520-70-0.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Hu, Penghui; Tan, Mingxi; Cheng, Lu; Zhao, Hongyuan; Feng, Rui; Gu, Wei-Jin; Han, Wei published the artcile< Bio-inspired iron-catalyzed oxidation of alkylarenes enables late-stage oxidation of complex methylarenes to arylaldehydes>, HPLC of Formula: 188813-04-9, the main research area is alkylarene polymethylhydrosiloxane promoter iron catalyst selective aerobic oxidation; aryl carbonyl compound preparation.

A bio-inspired iron-catalyzed polymethylhydrosiloxane-promoted aerobic oxidation of methylarenes to arylaldehydes with high yields and selectivities was reported. Notably, this method can tolerate oxidation-labile and reactive boronic acid group, which is normally required to be transformed immediately after its introduction and represents a significant advance in the area of the chem. of organoboronic acids, including the ability to incorporate both aldehyde and ketone functionalities into unprotected arylboronic acids, a class that can be difficult to access by current means. The robustness of this protocol was demonstrated on the late-stage oxidation of complex bioactive mols., including dehydroabietic acid, Gemfibrozil, Tocopherol nicotinate, a complex polyol structure and structurally complex arylboronic acids.

Nature Communications published new progress about Air. 188813-04-9 belongs to class bromides-buliding-blocks, and the molecular formula is C8H7BrO, HPLC of Formula: 188813-04-9.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Yu, Bin; Zhao, Bin; Hao, Zesheng; Chen, Lei; Cao, Lixin; Guo, Xiaofeng; Zhang, Nailou; Yang, Dongyan; Tang, Liangfu; Fan, Zhijin published the artcile< Design, synthesis and biological evaluation of pyrazole-aromatic containing carboxamides as potent SDH inhibitors>, Related Products of 5751-83-7, the main research area is pyrazole thiazole aryl carboxamide preparation antifungal SDH inhibitor SAR; Antifungal activity; Molecular docking; Structure-activity relationships; Succinate dehydrogenase inhibitors.

To continue studies on discovery of new potent antifungal leads, 43 novel pyrazole-aromatic containing carboxamides were rationally designed and synthesized. Bioassays indicated that most target compounds displayed good in vitro antifungal activities against Botrytis cinerea, Rhizoctonia cerealis and Sclerotinia sclerotiorum and in vivo antifungal activity against R. solani. Compound I exhibited the most significant in vitro activity against R. cerealis (EC50 = 0.93μg/mL) with about 2-fold more potent than a previously reported lead compound N-(3-bromophenyl)-2-[3-(difluoromethyl)-1-methyl-1H-pyrazol-4-yl]-4-thiazolecarboxamide (EC50 = 2.01μg/mL), and about 11-fold more potent than the pos. control/com. succinate dehydrogenase inhibitor thifluzamide (EC50 = 23.09μg/mL). Structure-activity relationship anal. and mol. docking simulations indicated that the presence of difluoromethyl pyrazole-(m-benzene)carboxamide scaffold obviously increased the antifungal activity. The further enzymic bioassay showed that both thifluzamide and compound I displayed excellent SDH inhibitory effects, and fluorescence quenching anal. suggested that they may share the same target SDH.

European Journal of Medicinal Chemistry published new progress about Amides Role: PAC (Pharmacological Activity), SPN (Synthetic Preparation), THU (Therapeutic Use), BIOL (Biological Study), PREP (Preparation), USES (Uses). 5751-83-7 belongs to class bromides-buliding-blocks, and the molecular formula is C7H7BrO2S, Related Products of 5751-83-7.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Jiang, Zhiwei; Toffano, Martial; Vo-Thanh, Giang; Bournaud, Chloee published the artcile< Bifunctional N-Heterocyclic Carbene-Catalyzed Highly Enantioselective Trans-Cyclopentannulation of Enals and Enones via Homoenolate>, Computed Properties of 3893-18-3, the main research area is cyclopentene preparation enantioselective diastereoselective; enal enone trans cyclopentannulation bifunctional heterocyclic carbene catalyst.

An efficient and flexible synthesis of a new class of chiral bifunctional NHC catalysts I [R = i-Pr, i-Bu, Bn, cyclohexyl; Ar = Ph, 3,5-bis(trifluoromethyl)phenyl, pentafluorophenyl, 2-methoxyphenyl; X = S, O] has been reported. These new imidazolylidene NHCs I, bearing a (thio)urea function as a hydrogen bond donor promoted efficiently highly diastereoselective trans-cyclopentannulation of enals R1CH=CHCHO (R1 = n-Pr, Ph, naphthalen-2-yl, furan-2-yl, etc.) and enones R2CH=CHC(O)R3 (R2 = methoxycarbonyl, Ph, thiophen-2-yl, etc.; R3 = Ph, 2-phenylethenyl, thiophen-2-yl, etc.) in moderate to good yields (up to 69% yield) along with excellent enantioselectivity (up to 96% ee). This methodol. could be applied to a large variety of substrates (30 examples).

ChemCatChem published new progress about Amino alcohols, chiral Role: RCT (Reactant), RACT (Reactant or Reagent). 3893-18-3 belongs to class bromides-buliding-blocks, and the molecular formula is C9H7BrO, Computed Properties of 3893-18-3.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Du, Yufeng; Huang, Linyu; Wang, Neng; Li, Xiaohuan; Zhou, Xian-Li; Zhang, Lan; Huang, Shuai; Walsh, Patrick J.; Gao, Feng published the artcile< Rhodium-Catalyzed Direct Arylation of Furopyridine: Synthesis and the Cardiac Effects of Dictamnine Derivatives>, SDS of cas: 401-78-5, the main research area is aryl furopyridine preparation chemoselective; furopyridine aryl bromide arylation rhodium catalyst; furoquinoline preparation chemoselective; dictamnine aryl bromide arylation rhodium catalyst.

Synthesis of Rh2(OAc)4/IMes·HCl system promotes the chemoselective installation of aryl groups at the 2-position of furo[2,3-b]pyridines I (R = Ph, naphthalen-1-yl, 2,3-dihydro-1,4-benzodioxin-6-yl, etc.) (53-94% yields). The method is applicable to the direct modification of the natural furoquinoline alkaloid dictamnine. The cardiac effects of the fluorinated analogs II were improved, and compared to dictamnine at 160μg/mL. Preliminary mechanism of action studies indicate that the effects might be related to epinephrine αreceptors, M-receptor and calcium channel receptor.

Advanced Synthesis & Catalysis 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, SDS of cas: 401-78-5.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary

Huan, Leitao; Shu, Xiaomin; Zu, Weisai; Zhong, De; Huo, Haohua published the artcile< Asymmetric benzylic C(sp3)-H acylation via dual nickel and photoredox catalysis>, Electric Literature of 2725-82-8, the main research area is alpha aryl ketone enantioselective preparation photochem; alkylarene carboxylic acid benzylic carbon hydrogen acylation nickel photocatalyst; photochem alpha aryl ester enantioselective preparation; phenyl chloroformate alkylarene coupling nickel photocatalyst.

An asym. benzylic C-H acylation of alkylarenes employing carboxylic acids as acyl surrogates for synthesis of α-aryl ketones I [R1 = Me, 2-thienyl, 2-naphthyl, etc.; R2 = Me, Et, CH2CH2OAc, etc.; Ar = 3-thienyl, 4-FC6H4, 1,1′-biphenyl, etc.] via nickel and photoredox dual catalysis was reported. This mild yet straightforward protocol transformed a diverse array of feedstock carboxylic acids and simple alkyl benzenes into highly valuable α-aryl ketones with high enantioselectivities. The utility of this method was showcased in gram-scale synthesis and late-stage modification of medicinally relevant mols. Mechanistic studies suggested a photocatalytically generated bromine radical could perform benzylic C-H cleavage to activate alkylarenes as nucleophilic coupling partners which could then engage in a nickel-catalyzed asym. acyl cross-coupling reaction. This bromine-radical-mediated C-H activation strategy could be also applied to enantioselective coupling of alkylarenes with chloroformate for synthesis of chiral α-aryl esters, e.g., II.

Nature Communications published new progress about Acylation catalysts (stereoselective). 2725-82-8 belongs to class bromides-buliding-blocks, and the molecular formula is C8H9Br, Electric Literature of 2725-82-8.

Referemce:
Bromide – Wikipedia,
bromide – Wiktionary