- Selective Electrochemical Oxygenation of Alkylarenes to Carbonyls
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An efficient electrochemical method for benzylic C(sp3)-H bond oxidation has been developed. A variety of methylarenes, methylheteroarenes, and benzylic (hetero)methylenes could be converted into the desired aryl aldehydes and aryl ketones in moderate to excellent yields in an undivided cell, using O2 as the oxygen source and lutidinium perchlorate as an electrolyte. On the basis of cyclic voltammetry studies, 18O labeling experiments, and radical trapping experiments, a possible single-electron transfer mechanism has been proposed for the electrooxidation reaction.
- Li, Xue,Bai, Fang,Liu, Chaogan,Ma, Xiaowei,Gu, Chengzhi,Dai, Bin
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supporting information
p. 7445 - 7449
(2021/10/02)
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- Volatiles from the xylarialean fungus Hypoxylon invadens
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The volatiles emitted by agar plate cultures of the xylarialean fungus Hypoxylon invadens were investigated by use of a closed loop stripping apparatus in combination with GC-MS. Several aromatic compounds were found that could only be identified by comparison to all possible constitutional isomers with different ring substitution patterns. For the set of identified compounds a plausible biosynthetic scheme was suggested that gives further support for the assigned structures.
- Dickschat, Jeroen S.,Wang, Tao,Stadler, Marc
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p. 734 - 746
(2018/04/16)
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- Selective Aerobic Oxidation of Methylarenes to Benzaldehydes Catalyzed by N-Hydroxyphthalimide and Cobalt(II) Acetate in Hexafluoropropan-2-ol
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Efficient and highly selective catalytic conditions for the aerobic autoxidation of methylarenes to benzaldehydes, based on N-hydroxyphthalimide (NHPI) and cobalt(II) acetate in 1,1,1,3,3,3-hexafluoropropan-2-ol (HFIP), were developed. The sustainable conditions enable a multigram scale preparation of benzaldehyde derivatives in high efficiency and with excellent chemoselectivity (up to 99 % conversion and 98 % selectivity).
- Gaster, Eden,Kozuch, Sebastian,Pappo, Doron
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supporting information
p. 5912 - 5915
(2017/05/12)
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- HETEROCYCLIC CARBOXYLIC ACIDS AS ACTIVATORS OF SOLUBLE GUANYLATE CYCLASE
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The present invention relates to compounds of formula I: and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R5, R6, R7, R8, R9, B, V, W, X, Y, Z and m are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
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- ALKOXY PYRAZOLES AS SOLUBLE GUANYLATE CYCLASE ACTIVATORS
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The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6 and R7 are as defined herein. The inventi
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- AROMATIC RING COMPOUND
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Provided is an aromatic ring compound having a GPR40 agonist activity. A compound represented by the formula (I): wherein each symbol is as described in the DESCRIPTION, or a salt thereof has a GPR40 agonist activity, and is useful as an agent for the prophylaxis or treatment of diabetes and the like.
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Paragraph 0420
(2015/01/18)
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- Roles of the synergistic reductive O-methyltransferase GilM and of O-methyltransferase GilMT in the gilvocarcin biosynthetic pathway
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Two enzymes of the gilvocarcin biosynthetic pathway, GilMT and GilM, with unclear functions were investigated by in vitro studies using purified, recombinant enzymes along with synthetically prepared intermediates. The studies revealed GilMT as a typical
- Tibrewal, Nidhi,Downey, Theresa E.,Van Lanen, Steven G.,Ul Sharif, Ehesan,O'Doherty, George A.,Rohr, Juergen
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p. 12402 - 12405
(2012/09/05)
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- Efficient discovery of potent anti-HIV agents targeting the Tyr181Cys variant of HIV reverse transcriptase
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Non-nucleoside reverse transcriptase inhibitors (NNRTIs) that interfere with the replication of human immunodeficiency virus (HIV) are being pursued with guidance from molecular modeling including free-energy perturbation (FEP) calculations for protein-in
- Jorgensen, William L.,Bollini, Mariela,Thakur, Vinay V.,Domaoal, Robert A.,Spasov, Krasimir A.,Anderson, Karen S.
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p. 15686 - 15696
(2011/12/03)
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- An oxidation of benzyl methyl ethers with NBS that selectively affords either aromatic aldehydes or aromatic methyl esters
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Either mono- or dibromination of benzyl methyl ethers can be achieved by controlling the amount of NBS and the temperature. Elimination of methyl bromide from the monobrominated intermediates produces aromatic aldehydes, whereas hydrolysis of the dibrominated intermediates affords aromatic methyl esters in good yields.
- Mayhoub, Abdelrahman S.,Talukdar, Arindam,Cushman, Mark
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experimental part
p. 3507 - 3510
(2010/08/06)
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- The first total synthesis of (±)-γ-herbertenol, a herbertene isolated from a non-herbertus source
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The structure of the aromatic sesquiterpene, (±)-γ- herbertenol, the first herbertane to be isolated from a non-herbertus source, was confirmed by a total synthesis, employing a Claisen rearrangement and ring-closing metathesis. Georg Thieme Verlag Stuttg
- Srikrishna,Ravikumar
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- Synthesis of benzo[b]phenanthridines and related naturally occurring 2-aryl-1,4-naphthoquinones by palladium- and copper-catalyzed coupling of organostannanes with bromoquinones
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Syntheses of phenanthroviridone, gilvocarcin BE-12406X2, antibiotic WS 5995B, and a key intermediate for the synthesis of jadomycin are described, based on palladium- and copper-catalyzed coupling reactions of sterically hindered arylstannanes
- De Frutos, Oscar,Atienza, Carmen,Echavarren, Antonio M.
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p. 163 - 171
(2007/10/03)
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- N-(4- carbamimidoyl-phenyl) -glycine derivatives
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The invention is concerned with novel N-(4-carbamimidoyl-phenyl)-glycine derivatives of the formula: wherein R1, E, X1 to X4 and G1 and G2 are as defined in the description and the claims, as well as hydrates or solvates and physiologically usable salts thereof.
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- Total syntheses of O4,O9-dimethylstealthins A and C
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O12-Acetyl-O4,O9-dimethylstealthin A (2-acetoxymethyl-11-amino-5-hydroxy-4,9-dimethoxybenzo[b]-fluoren-10-one and O4,O9-dimethylstealthin C (11-amino-5-hydroxy-4,9-dimethoxy-2-methylbenzo-[6]fluoren-10-one), methylated derivatives of potent radical scavengers produced by Streptomyces viridochromogenes, have been synthesized using Suzuki coupling as a key step.
- Koyama, Hiroya,Kamikawa, Tadao
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p. 203 - 209
(2007/10/03)
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- Total syntheses of O4,9-dimethyl stealthins A and C
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O4,9-dimethylstealthin A (11-amino-5-hydroxy-2-hydroxymethyl-4,9-dimethoxybenzo[b]fluoren-10-on e) and O4,9-dimethylstealthin C (11-amino-5-hydroxy-4,9-dimethoxy-2-methyl-benzo[b]fluoren-10-one), methylated derivatives of radical scavengers produced by Streptomyces viridochromogenes, were synthesized using the Suzuki coupling reactions as a key step.
- Koyama, Hiroya,Kamikawa, Tadao
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p. 3973 - 3976
(2007/10/03)
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- Syntheses of fenanthroviridone, gilvocarcin BE-12406X2, and antibiotic WS 599B based on the palladium and copper catalyzed coupling of organostannanes with bromoquinones
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A total synthesis of fenanthroviridone, gilvocarcin BE-12406X2, antibiotic WS 5995B is described based on the palladium and copper catalyzed coupling reaction of sterically hindered aryl stannanes with a 2-bromonaphthoquinone. Copyright (C) 199
- De Frutos, Oscar,Echavarren, Antonio M.
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p. 8953 - 8956
(2007/10/03)
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- Benzoannelated Centropolyquinanes, 4. - Steric Effects in Multiply Substituted Triptindans (9H,10H-4b,9a-(Benzenomethano)indenoindenes)
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Upon cyclodehydration of-indanones 11, 12, and 14, the steric interactions of three substituents in the endo positions 4, 5, and 15 of triptindan (6) allow only one methyl group to be introduced into the molecular cavity.In accordance with DNMR measurements and molecular mechanical calculations of triptindans 1-5, this regioselectivity is caused by the considerably increased compression due to a second endo-methyl group in the triptindan rotamers A and A'.
- Paisdor, Bernd,Gruetzmacher, Hans-Friedrich,Kuck, Dietmar
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p. 1307 - 1314
(2007/10/02)
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