- Nickel-catalysed cross-electrophile coupling of aryl bromides and primary alkyl bromides
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The structure of primary alkylated arenes plays an important role in the molecular action of drugs and natural products. The nickel/spiro-bidentate-pyox catalysed cross-electrophile coupling of aryl bromides and primary alkyl bromides was developed for th
- Gao, Nanxing,Li, Yanshun,Teng, Dawei
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p. 3569 - 3572
(2022/02/11)
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- Synthesis of Alkyl Indium Reagents by Using Unactivated Alkyl Chlorides and Their Applications in Palladium-Catalyzed Cross-Coupling Reactions with Aryl Halides
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An efficient method for the preparation of alkyl indium reagents by using unactivated and cheap alkyl chlorides as substrates in the presence of indium and LiI was developed. The thus-formed alkyl indium species effectively underwent palladium-catalyzed cross-coupling reactions with aryl halides with wide functional group tolerance.
- Chen, Bing-Zhi,Zhi, Man-Ling,Wang, Chuang-Xin,Chu, Xue-Qiang,Shen, Zhi-Liang,Loh, Teck-Peng
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supporting information
p. 1902 - 1905
(2018/04/16)
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- 1-[4-(3-Phenylalkyl)phenyl]-2-aminopropanes as 5-HT(2A) partial agonists
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Phenylalkylamines such as 1-(4-bromo-2,5-dimethoxyphenyl)-2-aminopropane (DOB; 1a) and its corresponding iodo derivative DOI (2) are commonly used 5-HT2 serotonin agonists. Previous studies have established that the 2,5-dimethoxy substitution p
- Dowd,Herrick-Davis,Egan,DuPre,Smith,Teitler,Glennon
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p. 3074 - 3084
(2007/10/03)
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- Influence of Conformation and Proton-Transfer Dynamics in the Dibenzyl σ-Complex on Regioselectivity in Gattermann-Koch Formylation via Intracomplex Reaction
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The Gattermann-Koch formylations of diphenyl, diphenylmethane, dibenzyl, and 1,3-diphenyl- propane were studied in HF-SbF5, -TaF5, -BF3, -NbF5, and CF3SO3H-SbF5. While usual high para regioselectivity was obtained for diphenyl, diphenylmethane, and 1,3-diphenylpropane, unprecedented ortho regioselectivity was observed for dibenzyl which increased with decreasing the SbF5/dibenzyl molar ratio and with strength of Lewis acids used in HF. A sandwich-like complex for monoprotonated dibenzyl resulting in ortho regioselectivity via the intracomplex reaction was suggested; therefore, the conformations of protonated diphenylmethane, dibenzyl, and 1,3- diphenylpropane and their proton-transfer dynamics were probed by semiempirical calculation (PM3). The calculation predicted that ortho monoprotonation was slightly preferable for dibenzyl, and remarkable preference of dibenzyl over other aromatic compounds was observed in ortho- ortho intramolecular inter-ring proton transfer via a fan-shaped complex rather than a sandwich- like complex. The experimental and theoretical data for dibenzyl are compatible with the intracomplex reaction, whereby CO is protonated by the ortho σ-complex undergoing rapid inter- ring proton transfer to generate formyl cation in the vicinity of the ortho position leading to ortho regioselectivity.
- Tanaka, Mutsuo,Fujiwara, Masahiro,Xu, Qiang,Ando, Hisanori,Raeker, Todd J.
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p. 4408 - 4412
(2007/10/03)
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- Methods of using α-phosphonosulfonate squalene synthetase inhibitors including the treatment of atherosclerosis and hypercholesterolemia
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α-Phosphonosulfonate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula STR1 wherein R2 is OR5 or R5a ; R3 and R5 are independently H, alkyl, arylalkyl, aryl or cycloalkyl; R5a is H, alkyl, arylalkyl or aryl; R4 is H, alkyl, aryl, arylalkyl, or cycloalkyl;, Z is H, halogen, lower alkyl or lower alkenyl; and R1 is a lipophilic group which contains at least 7 carbons and is alkyl, alkenyl, alkynyl, mixed alkenyl-alkynyl, aryl, arylalkyl, cycloalkyl, cycloalkylalkyl, heteroaryl, heteroarylalkyl, cycloheteroalkyl, cycloheteroalkylalkyl; as further defined above; including pharmaceutically acceptable salts and or prodrug esters of the phosphonic (phosphinic) and/or sulfonic acids.
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