- Compound as protein degradation agent and preparation method and medical application thereof
-
The invention discloses a compound serving as a protein degrading agent and a preparation method and medical application thereof, and particularly discloses a compound represented by the formula (I) and a pharmaceutically acceptable salt thereof, and the
- -
-
-
- Pd-Catalyzed β-C-H Arylation of Aldehydes and Ketones Based on a Transient Directing Group
-
The direct Pd-catalyzed β-C-H arylation of aldehydes and ketones was developed by using 2-amino-N,N′-diisopropylsuccinamide as a novel transient directing group (TDG). The TDG showed good versatility in functionalizing unactivated β-C-H bonds of aldehydes and ketones. It was effective not only for aliphatic aldehydes and ketones but also for aromatic aldehydes and ketones. Besides, it was applicable to o-methylbenzaldehydes.
- Wu, Liang-Fei,Yao, Jian-Wei,Zhang, Xin,Liu, Si-Yuan,Zhuang, Ze-Nian,Wei, Kun
-
supporting information
p. 6237 - 6241
(2021/08/23)
-
- Access to Trisubstituted Fluoroalkenes by Ruthenium-Catalyzed Cross-Metathesis
-
Although the olefin metathesis reaction is a well-known and powerful strategy to get alkenes, this reaction remained highly challenging with fluororalkenes, especially the Cross-Metathesis (CM) process. Our thought was to find an easy accessible, convenient, reactive and post-functionalizable source of fluoroalkene, that we found as the methyl 2-fluoroacrylate. We reported herein the efficient ruthenium-catalyzed CM reaction of various terminal and internal alkenes with methyl 2-fluoroacrylate giving access, for the first time, to trisubstituted fluoroalkenes stereoselectively. Unprecedent TON for CM involving fluoroalkene, up to 175, have been obtained and the reaction proved to be tolerant and effective with a large range of olefin partners giving fair to high yields in metathesis products. (Figure presented.).
- Nouaille, Augustin,Pannecoucke, Xavier,Poisson, Thomas,Couve-Bonnaire, Samuel
-
supporting information
p. 2140 - 2147
(2021/03/06)
-
- Preparation method of pemetrexed acid
-
Belonging to the technical field of organic compound synthesis, the invention in particular relates to a preparation method of pemetrexed acid. The method is characterized by utilizing methyl p-formylbenzoate and malonic acid as the starting materials to synthesize the target product. Compared with the methods for synthesis of the compound reported in previous literatures, the method provided by the invention has the advantages of easily available raw materials, low price and no pollution, greatly reduces the production cost, and is suitable for large-scale industrial production. The method isa brand new synthetic route for the compound.
- -
-
Paragraph 0049; 0050
(2019/05/16)
-
- Chemo- and Regioselective Organo-Photoredox Catalyzed Hydroformylation of Styrenes via a Radical Pathway
-
An unprecedented, chemo- and regioselective, organo-photoredox catalyzed hydroformylation reaction of aryl olefins with diethoxyacetic acid as the formylation reagent is described. In contrast to traditional transition metal promoted ionic hydroformylation reactions, the new process follows a unique photoredox promoted, free radical pathway. In this process, a formyl radical equivalent, produced from diethoxacetic acid through a dye (4CzIPN) photocatalyzed, sequential oxidation-decarboxylation route, regio- and chemoselectively adds to a styrene substrate. Importantly, under the optimized reaction conditions the benzylic radical formed in this manner is reduced by SET from the anion radical of 4CzIPN to generate a benzylic anion. Finally, protonation produces the hydroformylation product. By using the new protocol, aldehydes can be generated regioselectively in up to 90% yield. A broad array of functional groups is tolerated in the process, which takes place under mild, metal-free conditions.
- Huang, He,Yu, Chenguang,Zhang, Yueteng,Zhang, Yongqiang,Mariano, Patrick S.,Wang, Wei
-
supporting information
p. 9799 - 9802
(2017/08/02)
-
- Hydroformylation of olefins and reductive carbonylation of aryl halides with syngas formed ex situ from dehydrogenative decarbonylation of hexane-1,6-diol
-
A variety of primary alcohols have been investigated as convenient substrates for the ex situ delivery of carbon monoxide and molecular hydrogen in a two-chamber reactor. The gaseous mixture is liberated in one chamber by an iridium-catalysed dehydrogenative decarbonylation of the alcohol and then consumed in the other chamber in either a rhodium-catalysed hydroformylation of olefins or a palladium-catalysed reductive carbonylation of aryl halides. Hexane-1,6-diol was found to be the optimum alcohol for both reactions where moderate to excellent yields were obtained of the product aldehydes. A relatively low pressure of 1.5-2.4 bar was measured in the closed system during the two transformations.
- Christensen, Stig Holden,Olsen, Esben P. K.,Rosenbaum, Jascha,Madsen, Robert
-
p. 938 - 945
(2015/02/19)
-
- 3,5-DICHLORO,4-(3,4-(CYCLO-)ALKOXYPHENYL)--2-CARBONYLOXY)ETHYL)PYRIDINE DERIVATIVES AS PDE-4 INHIBITORS
-
The invention relates to novel 3,5-dichloro,4-(3,4-(cyclo-) alkoxyphenyl)--2-carbonyloxy)ethyl)pyridine compounds which are inhibitors of the phosphodiesterase 4 (PDE4) enzyme and muscarinic M3 receptor antagonists, methods of preparing such compounds, co
- -
-
Page/Page column 30-31
(2015/12/24)
-
- Palladium-catalyzed γ-selective arylation of zincated Boc-allylamines
-
The regio- and diastereoselective arylation of Boc-protected allylamines was performed via a one-pot lithiation/transmetalation to zinc/cross-coupling sequence, through an appropriate choice of a phosphine ligand. A variety of γ-arylated products were obtained in moderate to good yield, and the products could be directly transformed into valuable γ-arylamines and β-aryl aldehydes.
- Millet, Anthony,Baudoin, Olivier
-
supporting information
p. 3998 - 4000
(2014/08/18)
-
- A novel consecutive three-component Heck-isomerization-Wittig sequence by way of in situ generated aldehydes
-
A novel consecutive three-component four step synthesis of 5-(hetero)arylpent-2-enoates has been disclosed. Various (hetero)aryl iodides can be coupled with allyl alcohol under Heck conditions to give 3-(hetero)arylpropionaldehyde intermediates, which were transformed without isolation with in situ generated stabilized phosphorus ylides to furnish 5-(hetero)arylpent-2-enoates in moderate to excellent yield. This one-pot procedure circumvents the isolation of sensitive aldehydes and phosphorus ylides as intermediates and finally gives the product isomers with good to excellent E/Z and β/α selectivity. ARKAT-USA, Inc.
- Panther, Jesco,Roehrich, Adalbert,Mueller, Thomas J. J.
-
p. 297 - 311
(2013/09/24)
-
- Double arylation of allyl alcohol via a one-pot heck arylation- isomerization-acylation cascade
-
A one-pot, two-step catalytic protocol has been developed. A regioselective Heck coupling between aryl bromides and allyl alcohol leads to the generation of arylated allyl alcohols that in situ isomerize to give aldehydes, which then undergo an acylation reaction with a second aryl bromide. A variety of aryl bromides can be employed in both the initial Heck reaction and the acylation, providing easy access to a wide variety of substituted dihydrochalcones.
- Colbon, Paul,Ruan, Jiwu,Purdie, Mark,Mulholland, Keith,Xiao, Jianliang
-
supporting information; experimental part
p. 5456 - 5459
(2011/12/05)
-
- Methods for the use of inhibitors of cytosolic phospholipase A2 in the treatment of thrombosis
-
This invention provides methods for the use of substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof. The invention provides methods for the use of the compounds in the treating or preventing thrombosis in a mammal, or preventing progression of symptoms of thrombosis.
- -
-
Page/Page column 19
(2010/11/29)
-
- Nornicotine-organocatalyzed aqueous reduction of α,β-unsaturated aldehydes
-
Nornicotine, a native component of tobacco and minor nicotine metabolite, was found to catalyze the chemoselective reduction of α,β-unsaturated aldehydes under homogeneous aqueous conditions. The Royal Society of Chemistry.
- Brogan, Andrew P.,Dickerson, Tobin J.,Janda, Kim D.
-
p. 4952 - 4954
(2008/09/17)
-
- INHIBITORS OF CYTOSOLIC PHOSPHOLIPASE A2
-
This invention provides chemical inhibitors of the activity of various phospholipase enzymes, particularly cytosolic phospholipase A2 enzymes (cPLA2), more particularly including inhibitors of cytosolic phospholipase A2 alpha enzymes (cPLAα). In some embodiments, the inhibitors have the Formula I: wherein the constituent variables are as defined herein.
- -
-
Page/Page column 33-34
(2008/06/13)
-
- INHIBITORS OF HISTONE DEACETYLASE
-
The invention relates to a series of compounds useful for inhibiting histone deacetylase (HDAC) enzymatic activity. The invention also provides a method for inhibiting histone descetylase in a cell using said compounds as well as a method for treating cell proliferative diseases and conditions using said HDAC inhibitors. Further, the invention provides pharmaceutical compositions comprising the HDAC inhibiting compounds and a pharmaceutically acceptable carrier.
- -
-
Page/Page column 93-94
(2010/02/14)
-
- Process for making an aldehyde
-
A process for making an aromatic aldehyde in which a sulfoxide is reacted with a dihalogenated aromatic compound in the absence of an effective amount of an activating reagent. The aldehyde may then be used to make other compounds, such as a compound that acts as a cPLA inhibitor.
- -
-
-
- Nickel-Catalyzed Arylation of Acrolein Diethyl Acetal: A Substitute to the 1,4-Addition of Arylhalides to Acrolein
-
(Equation presented) In the presence of catalytic amount of NIBr 2 as catalyst precursor, organic halides are reductively coupled at 70°C with acrolein diethyl acetal to give (Z)- and (E)-enolethers by allylic deplacement of an alkoxy group. Subsequent hydrolysis affords β-arylated aldehydes.
- Condon,Dupre,Nedelec
-
p. 4701 - 4703
(2007/10/03)
-
- Inhibitors of cytosolic phospholipase A2
-
This invention provides substituted indole compounds of the general formula: and pharmaceutically acceptable salt forms thereof, and methods for using the compounds as inhibitors of the activity of various phospholipase enzymes, particularly phospholipase A2 enzymes, and for the medical treatment, prevention and inhibition of pain and inflammation.
- -
-
-
- Synthesis and biological activity of new 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitors: 2-oxetanones with a side chain mimicking the folded structure of 1233A.
-
To mimic the folded side chain conformation of 1233A (1), which is a 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) synthase inhibitor, 1233A analogs with aromatic rings in the side chain were synthesized. The 2-oxetanone moiety was kept intact. Among 1233A and its synthetic analogs, trans-3-hydroxymethyl-4-[2-(7-methoxycarbonyl-1-naphthyl)ethyl]-2-oxe tanone (23) showed the highest HMG-CoA synthase inhibitory activity in vitro. The structure-activity relationship at the side chain is discussed.
- Hashizume,Ito,Yamada,Nagashima,Kanao,Tomoda,Sunazuka,Kumagai,Omura
-
p. 512 - 520
(2007/10/02)
-
- Novel 5-Desmethylene Analogues of 5,10-Dideaza-5,6,7,8-tetrahydrofolic Acid as Potential Anticancer Agents
-
The synthesis and biological activity of novel 5-desmethylene analogues of 5,10-dideaza-5,6,7,8-tetrahydrofolic acid (DDATHF), a potent antitumor agent presently undergoing clinical trials, are described.These compounds are representative of a new series
- Taylor, Edward C.,Gillespie, Paul,Patel, Mona
-
p. 3218 - 3225
(2007/10/02)
-
- Alkenoic acid derivatives
-
An alkenoic acid derivative of the formula STR1 in which X and Y are identical or different and represent sulfur, sulfoxide, sulfone, an alkylene chain, --SCH2 --, or oxygen or a direct bond, W represents --CH=CH-- or --CH2 --CH2 --, o represents a number 1 to 5, A and B are identical or different and represent carboxyl, carboxymethylene, tetrazolyl or tetrazolylmethylene, or --CO2 R9 or --CH2 CO2 R9 or --CONR10 R11 or nitrile n represents a number 1 to 10, m represents a number 0 to 7, T and Z are identical or different and represent oxygen or a direct bond and R2, R3, R8 are identical or different and represent hydrogen, alkyl, alkoxy, halogen, trifluoromethyl, trifluoromethoxy, cyano or nitro and R9 is lower alkyl and R10 and R11 are hydrogen, lower alkyl, alkylsulfonyl or arylsulfonyl or together are an alkylene chain to form a ring and pharmaceutically acceptable salts thereof. Such alkenoic acid derivatives are useful as leucotriene disease antagonists.
- -
-
-
- Certain arylalkyl or pyridylalkyl hydroxamates useful for treating allergies and asthma
-
Arylhydroxamates are provided having the structure STR1 wherein R1 is hydrogen, lower alkyl, aryl, lower alkenyl, cycloalkyl, or aralkyl; R2 is hydrogen, lower alkyl, aryl, cycloalkyl, alkanoyl or aroyl; m is 2 to 8; and STR2 wherein R3 is OH, COOH STR3 These compounds are useful as inhibitors of Δ5 -lipoxygenase and as such are useful as antiallergy agents.
- -
-
-
