- Convergent total synthesis of corallocin A
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The first total synthesis of corallocin A is described herein. The Suzuki coupling reaction as a key step proceeded with high stereoselectivity and in good yield. Robust transformations, including Vilsmeier-Haack formylation and Wittig reaction, allowed for effective access to corallocin A.
- Mashiko, Tomoya,Nakazato, Yuta,Katsumura, Yuta,Kasamatsu, Akihiko,Adachi, Shinya,Kamo, Shogo,Matsuzawa, Akinobu,Sugita, Kazuyuki
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supporting information
p. 5127 - 5132
(2021/06/21)
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- SMTP GROUP OR SMTP-7 PRODUCTION INTERMEDIATE AND CHEMICAL PRODUCTION METHOD THEREOF
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PROBLEM TO BE SOLVED: To provide a compound having a dihydropyran structure that can be a useful intermediate in chemically producing a group of Pre-SMTP, SMTP. SOLUTION: The present invention provides a compound having a dihydropyran structure represente
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Paragraph 0038; 0039
(2020/06/06)
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- CHEMICAL METHOD OF PRODUCING SMTP GROUPS OR SMTP-7 AND INTERMEDIATES USED IN THE METHOD
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The present invention provides a compound having a dihydropyran structure, a method of producing a compound having a dihydropyran structure, a method of producing Pre-SMTP, a method of producing a group of SMTPs, and a pharmaceutical composition. The comp
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Paragraph 0024-0026
(2020/05/29)
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- Synthesis of novel resveratrol-phthalide hybrid compounds and evaluation of their inhibitory activities of nitric oxide production
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Four types of novel resveratrol-phthalide hybrid compounds were designed and synthesized systematically by Suzuki-Miyaura cross-coupling reaction. These hybrid compounds were evaluated upon an inhibitory effect of the LPS-stimulated NO production in murine macrophage cell line, RAW264.7. As a result, two of them showed stronger inhibitory activity than the original resveratrol.
- Kimachi, Tetsutaro,Ogata, Tokutaro,Doe, Misae,Sakanaka, Mariko,Nishiuchi, Arisa,Aomatsu, Mio,Tanaka, Manami,Shimizu, Maki,Yoshioka, Natsuko,Kubota, Kurumi,Teraoka, Yui,Nakajima, Chikako,Takahashi, Satoru
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p. 534 - 548
(2019/08/01)
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- Aminopyrimidine compound
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The invention discloses an aminopyrimidine compound. The structural general formula of the compounds is shown as a formula I in the specification. In the formula I, R1 is one of alkyl with a carbon atom total number of 1-6, cycloalkyl with a carbon atom total number of 3-6, halogen substituted alkyl with a carbon atom total number of 1-6 and halogen substituted cycloalkyl with a carbon atom totalnumber of 3-6, R2 is alkoxy with a carbon atom total number of 1-6, halogen substituted alkoxy with a carbon atom total number of 1-6, cycloalkyl with a carbon atom total number of 3-6 and halogen substituted cycloalkyl with a carbon atom total number of 3-6, and X is F, Br or Cl. The compound has a remarkable antibacterial effect and a good drug forming property.
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Paragraph 0091; 0094; 0096; 0097; 0098
(2019/08/12)
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- Synthesis of chiral isoindolinones via asymmetric propargylation/lactamization cascade
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A Zn-mediated propargylation/lactamization cascade reaction with chiral 2-formylbenzoate derived N-tert-butanesulfinyl imines was realized, which provided a practical and efficient method for the synthesis of chiral isoindolinones. High diastereoselectivities (up to 97:3 dr) and good reaction yields were observed for most examined cases.
- Meng, Jiao-Long,Jiao, Tang-Qian,Chen, Ya-Heng,Fu, Rui,Zhang, Shu-Sheng,Zhao, Qian,Feng, Chen-Guo,Lin, Guo-Qiang
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p. 1564 - 1567
(2018/03/23)
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- A general catalytic route to isoindolinones and tetrahydroisoquinolines: Application in the synthesis of (±)-crispine A
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An unprecedented highly efficient Lewis acid catalyzed one-pot cascade has been demonstrated as a general catalytic system for the synthesis of diversely substituted isoindolinones and tetrahydroisoquinolines. The cascade effects one C-C and two C-N bond-
- Dhanasekaran, Sivasankaran,Bisai, Vishnumaya,Unhale, Rajshekhar A.,Suneja, Arun,Singh, Vinod K.
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supporting information
p. 6068 - 6071
(2015/01/09)
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- Synthesis of chiral 3-substituted phthalides by a sequential organocatalytic enantioselective aldol-lactonization reaction. Three-step synthesis of (S)-(-)-3-butylphthalide
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(Chemical Equation Presented) The development of efficient methods for the facile construction of important molecular frameworks is an important goal in organic synthesis. Chiral 3-substituted phthalides are widely distributed in a large collection of natural products with broad, potent, and potentially path-pointing biological activities. In this investigation, we have uncovered an unprecedented organocatalytic asymmetric aldol-lactonization reaction of 2-formylbenzoic esters with ketones/aldehydes for convenient construction of the enantioenriched "privileged" scaffold. As a result of the sensitive nature of substrate structures of an organocatalytic enantioselective aldol reaction, after extensive optimization of reaction conditions, catalyst L-prolinamide alcohol IV is identified as the best promoter. Interestingly, it is found that in this reaction, addition of an acid additive PhCO2H can significantly enhance reaction efficiency with use of only as low as 2.5 mol % IV for the process. Moreover, due to the sensitivity of reaction conditions toward a sequential aldol-lactonization process without affecting enantioselectivity and racemization, it is essential to remove the catalyst for the subsequent facile lactonization reaction in the presence of K 2CO3. The aldol-lactonization processes serve as a powerful approach to the preparation of synthetically and biologically important 3-substitued phthalides with a high level of enantioselectivities. A 3-step catalytic asymmetric synthesis of the natural product of 3-butylphthalide is reported.
- Zhang, Haoyi,Zhang, Shilei,Liu, Lu,Luo, Guangshun,Duan, Wenhu,Wang, Wei
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supporting information; scheme or table
p. 368 - 374
(2010/03/30)
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- Synthesis of diverse analogues of Oenostacin and their antibacterial activities
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Several diverse analogues of Oenostacin, a naturally occurring potent antibacterial phenolic acid derivative, have been synthesized. A small library with more than forty analogues having different aromatic rings and varied side chains has been achieved through solution phase synthesis. Some of these analogues, that is, 22, 23 and 42, possessed potent antibacterial activities against Staphylococcus epidermidis and Staphylococcus aureus having EC50 ranging from 0.49 to 0.67 μM as compared to Oenostacin (EC50 = 0.12 μM).
- Srivastava, Vandana,Darokar, Mahendra P.,Fatima, Atiya,Kumar,Chowdhury, Chinmay,Saxena, Hari Om,Dwivedi, Gaurav R.,Shrivastava, Kunal,Gupta, Vivek,Chattopadhyay,Luqman, Suaib,Gupta,Negi, Arvind S.,Khanuja, Suman P.S.
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p. 518 - 525
(2008/03/12)
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- Synthesis of unnatural hydroxyanthraquinones : Experiments towards total synthesis of pradimicinone
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The phthalide sulfone 5 has been prepared from readily available ester 6 in four steps on multigram scales. This has been utilized in anionic [4 + 2] cycloaddition with a few cyclohexenones (12-14) to obtain anthraquinones (18-26) in good yields, compound
- Murty,Hazra,Datta,Mal
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p. 126 - 132
(2007/10/03)
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- Syntheses of Methyl Ether of Anaphatol and Three Other Natural Phthalides
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Syntheses of the methyl ether (V) of a natural phthalide anaphatol (II) (5-hydroxy-7-O-3'-methylbut-2'-enylphthalide), two other natural phthalides, viz., 5,7-dihydroxyphthalide (I) and 5-methoxy-7-hydroxyphthalide (III) occuring in Anaphalis contorta and of 5,7-dimethoxyphthalide (IV) reported from Helychrysum arenarium have been accomplished.The assigned structures of the above natural phthalides are thus confirmed. 4,6-Diacetoxyphthalide (VI) has also been synthesized.
- Talapatra, Bani,Roy, Monoj K.,Talapatra, Sunil K.
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p. 1169 - 1171
(2007/10/02)
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