- Substituted Fused Heteroaromatic Tricyclic Compounds as Kinase Inhibitors and The Use Thereof
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The disclosure relates to substituted fused heteroaromatic tricyclic compounds and the use thereof. Specifically, the disclosure provides compounds of the following Formula I: or a pharmaceutically acceptable salt or prodrug thereof, wherein A1
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Paragraph 0166; 0203
(2021/05/07)
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- Chiral naphthyl-C2-indole as scaffold for phosphine organocatalysis: Application in asymmetric formal [4 + 2] cycloaddition reactions
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The applications of a newly designed chiral naphthyl-C2-indole bifunctional phosphine organocatalyst in stereoselective formal [4 + 2] cycloaddition reactions were reported. The chiral naphthyl-C2-indole skeleton was introduced to bifunctional phosphine o
- He, Tingting,Peng, Lei,Li, Shan,Hu, Fangli,Xie, Chuandong,Huang, Shengli,Jia, Shiqi,Qin, Wenling,Yan, Hailong
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supporting information
p. 6966 - 6971
(2020/09/15)
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- Synthetic method for optically pure double-helix oligomeric tetra-benzocyclooctene substances
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The invention discloses a synthetic method for optically pure double-helix oligomeric tetra-benzocyclooctene substances. The synthetic method comprises the following steps: (1) carrying out oxidative cross-coupling on diiodo dimethoxy biphenyl (51) and 2,2',6,6'-biphenyl tetrabromide (97) to obtain 1,16-dibromo-8,9-dimethoxy tetra-benzocyclooctene (96); (2) splitting the compound (96), thus obtaining optically pure (S, S)-96 and (R, R)-96; (3) taking the compound (96) as a raw material, synthesizing an intermediate (116) containing 6 benzene rings; (4) splitting the intermediate (116) to obtain (M)-116 and (P)-116; (5) making the optically pure (S, S)-96 and (M)-116 reacted to obtain target products, namely (M) -117, (M)-149 and (M)-150; and/or: making the (R, R)-96 and (P)-116 reacted to obtain target products, namely (P)-117, (P)-149 and (P)-150.
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Paragraph 0033; 0034; 0035
(2017/07/31)
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- TETRAHYDROQUINOLINE COMPOSITIONS AS BET BROMODOMAIN INHIBITORS
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The present invention relates to inhibitors of bromo and extra terminal (BET) bromodomains that are useful for the treatment of cancer, inflammatory diseases, diabetes, and obesity, having Formula (I): wherein W, X, Y, Z, R1, R2, R5, and R8 are as described herein.
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Paragraph 0216
(2015/06/03)
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- Total synthesis of dictyodendrins B and E, and formal synthesis of dictyodendrin C
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A full account of the concise total syntheses of dictyodendrins B and E, and the formal synthesis of dictyodendrin C are described. A palladium-catalysed Larock indole synthesis was used to form the highly substituted indole core, and a palladium-mediated
- Tao, Pengyu,Liang, Jingjing,Jia, Yanxing
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p. 5735 - 5748
(2014/11/07)
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- Total synthesis of indole-3-acetonitrile-4-methoxy-2-C-β-d- glucopyranoside. Proposal for structural revision of the natural product
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Indole-3-acetonitrile-4-methoxy-2-C-β-d-glucopyranoside (1), a novel C-glycoside from Isatis indigotica with important cytotoxic activity, has been prepared in ten steps from ethynyl-β-C-glycoside 3 and 2-iodo-3-nitrophenyl acetate 6. Key steps in the synthesis include a Sonogashira coupling and a CuI-mediated indole formation. NMR spectroscopic data for synthetic 1 differs from that reported for the natural product. A revised structure for the natural product, containing an alternate carbohydrate substituent, is proposed. The Royal Society of Chemistry 2012.
- Yepremyan, Akop,Minehan, Thomas G.
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supporting information; experimental part
p. 5194 - 5196
(2012/08/08)
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- An innovative strategy for the synthesis of a new series of potent aminopeptidase (APN or CD13) inhibitors derived from the oxepin-4-one family
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Derivatives from the aminobenzosuberone family have been recently synthesized and recognized as highly selective inhibitors of aminopeptidase N (APN)/CD13 (EC 3.4.11.2), an important target for cell migration processes involved in particular in tumor inva
- Roux, Lionel,Charrier, Cédric,Salomon, Emmanuel,Ilhan, Meral,Bisseret, Philippe,Tarnus, Céline
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scheme or table
p. 2586 - 2589
(2011/06/21)
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- Enantioselective hydrogenation of α-dehydroamino acid esters catalyzed by rhodium complexes with chiral bisaminophosphine ligands
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A highly efficient strategy for the synthesis of a series of chiral bisaminophosphine ligands was well established with several remarkable features. The synthetic utility of these ligands was explored for rhodium-catalyzed asymmetric hydrogenations of α-d
- Sun, Xianfeng,Li, Wei,Zhou, Le,Zhang, Xumu
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supporting information; experimental part
p. 1150 - 1154
(2010/06/20)
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- A Pd[0]-catalyzed Ullmann cross-coupling/reductive cyclization approach to C-3 mono-alkylated oxindoles and related compounds
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The Pd[0]-catalyzed Ullmann cross-coupling of o-nitrohaloarenes 1a-e with the brominated heterocycles 2a-f delivers the expected products 3a-j in good to excellent yields. The reductive cyclization of such products, as well as N-acyl derivatives 3k, l, and m, has been investigated and provided the C-3 mono-substituted oxindoles 5a-d, f, g, k, and m, the direct reduction products 4i and j or indole 5l.
- Banwell, Martin G.,Jones, Matthew T.,Loong, David T.J.,Lupton, David W.,Pinkerton, David M.,Ray, Jayanta K.,Willis, Anthony C.
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experimental part
p. 9252 - 9262
(2011/01/12)
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- Chiral biphenylamide derivative: An efficient organocatalyst for the enantioselective synthesis of α-hydroxy phosphonates
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The aldol reactions of α-keto phosphonates and aldehydes were facilitated by an axially chiral biphenylprolinamide under mild conditions, affording the synthetically and pharmaceutically useful products in high yields and excellent enantioselectivities.
- Jiang, Jun,Chen, Xiaohong,Wang, Jun,Hui, Yonghai,Liu, Xiaohua,Lin, Lili,Feng, Xiaoming
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supporting information; experimental part
p. 4355 - 4357
(2009/12/25)
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- Axial chirality control by 2,4-pentanediol for the alternative synthesis of c3-tunephos chiral diphosphine ligands and their applications in highly enantioselective ruthenium-catalyzed hydrogenation of β-keto esters
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A highly efficient strategy for the synthesis of a series of C 3*-TunePhos chiral diphosphine ligands was well established with several remarkable features. The synthetic utility of these ligands was explored for the ruthenium-catalyzed asymmetric hydrogenation of β-keto esters. Up to 99% ee values were achieved for the enantioselective synthesis of β-hydroxy acid derivatives, which are very important chiral building blocks for the synthesis of a variety of natural products and biologically active molecules.
- Sun, Xianfeng,Li, Wei,Hou, Guohua,Zhou, Le,Zhang, Xumu
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supporting information; experimental part
p. 2553 - 2557
(2009/12/28)
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- Tuning Rate of the Bergman Cyclization of Benzannelated Enediynes with Ortho Substituents
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matrix presented The Bergman cyclization of benzannelated enediynes is highly sensitive to ortho substitution. This finding opens possibilities for the rational design of conformer-specific and pH-dependent DNA-cleaving agents.
- Alabugin, Igor V.,Manoharan, Mariappan,Kovalenko, Serguei V.
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p. 1119 - 1122
(2007/10/03)
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- Chemistry of aminophenols. Part 3: First synthesis of nitrobenzo[b]furans via a coupling-cyclization approach
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The first synthesis of 4-, 5-, and 6-nitrobenzo[b]furans has been achieved via the Sonogashira cross-coupling reaction of 2-iodonitrophenol acetates prepared from commercially available and inexpensive 2-aminonitrophenols. The obtained 2-alkynylnitropheno
- Dai, Wei-Min,Lai, Kwong Wah
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p. 9377 - 9380
(2007/10/03)
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- Iodination of Thallium(I) salts of Phenols
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The iodination of thallium(I) salts of phenols is examined and the results are compared with those of the selective ortho-iodinating reagent thallium(I) acetate-iodine.
- Gambie, Richard C.,Larsen, David S.,Rutledge, Peter S.,Woodgate, Paul D.
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p. 767 - 769
(2007/10/03)
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- An efficient access to (R)- and (S)-6,6'-dimethoxy-2,2'-diiodo-1,1'-biphenyl
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In a better procedure than the known for (rac)-2a, the diamine (rac)-2b was resolved for the first time with the new resolving agent (R,R)- and (S,S)-2,3-di(phenylaminocarbonyl)tartaric acid (5c) (40-45% weight yields; >99% ee). The diamines (R)- and (S)-2a and 2b were converted with >98% stereochemical retention into the diiodides (R)- and (S)-3a and 3b and subsequently, without loss of optical purity, diphenylphosphinated to the known diphosphines (R)- and (S)-4a and 4b.
- Cereghetti, Marco,Schmid, Rudolf,Schoenholzer, Peter,Rageot, Alain
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p. 5343 - 5346
(2007/10/03)
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