专利号:US-10995049-B2 优先权日:2019-07-19 标 题 :Total synthesis of prostaglandin J natural products and their intermediates 发明人:LI JIAMING; XU CHEN; AHMED TONIA S; GRUBBS ROBERT H; STOLTZ BRIAN M 权利人:CALIFORNIA INST OF TECHN 摘要:The present disclosure is directed to methods of preparing prostaglandin J natural products by stereoretentive metatheses reactions and intermediates used in the synthesis of these natural products, including the use of intermediates of Formula (I-A), where R 1 is defined in the specification
专利号:US-7939679-B2 优先权日:2006-01-19 标题:Method for synthesis of ciguatoxin CTX1B and compounds useful for the synthesis of ciguatoxin CTX1B 发明人:HIRAMA MASAHIRO; INOUE MASAYUKI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:Disclosed is a method for total synthesis of CTX1B, which is developed for the synthesis of a ciguatoxin analogue such as CTX3C and enables the more efficient application of an established reaction to the total synthesis of CTC1B. More specifically, disclosed is a method for total synthesis of CTX1B comprising; an O.S-acetal formation for synthesizing a novel compound (3); a radical cyclization reaction for constructing a 9-membered ring formation reaction including a novel compound (6) through a novel compound (8) and yielding a compound (D); and a deprotection for yielding CTX1B. Also disclosed are novel compounds (1) to (8) which are particularly useful for synthesis of CTX1B and can be used for the synthesis of a ciguatoxin analogue.
专利号:US-11548898-B2 优先权日:2017-07-06 标题 :Synthesis of halichondrins 发明人:KISHI YOSHITO; AI YANRAN; YE NING; WANG QIAOYI; YAHATA KENZO; ISO Kentaro; NAINI SANTHOSH REDDY; YAMASHITA SHUJI; LEE JIHOON; OHASHI ISAO; FUKUYAMA TAKASHI 权利人:HARVARD COLLEGE; EISAI R&D MAN CO LTD 摘要:The present invention provides methods for the synthesis of ketones involving a Ni/Zr-mediated coupling reaction. The Ni/Zr-mediated ketolization reactions can be used in the synthesis of halichondrins (e.g., halichondrin A, B, C; homohalichondrin A, B, C; norhalichondrin A, B, C), and analogs thereof. Therefore, the present invention also provides synthetic methods useful for the synthesis of halichondrins, and analogs thereof. Also provided herein are compounds (i.e., intermediates) useful in the synthesis of halichondrins, and analogs thereof. In particular, the present invention provides methods and compounds useful in the synthesis of compound of Formula (H3-A).
专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:US-8318427-B2 优先权日:2005-12-29 标 题 :Use of acid scavengers for the synthesis of standard length and long-mer nucleic acid arrays 发明人:KUIMELIS ROBERT G; MCGALL GLENN H; GOLDBERG MARTIN J; XU GUANGYU 权利人:KUIMELIS ROBERT G; MCGALL GLENN H; GOLDBERG MARTIN J; XU GUANGYU; AFFYMETRIX INC 摘要:Protective groups which may be cleaved with an activatable deprotecting reagents are employed to achieve a highly sensitive, high resolution, combinatorial synthesis of pattern arrays of diverse polymers. In preferred embodiments of the instant invention, the activatable deprotecting reagent is a photoacid generator and the protective groups are DMT for nucleic acids and tBOC for amino acids. This invention has a wide variety of applications and is particularly useful for the solid phase combinatorial synthesis of polymers.
专利号:US-4914220-A 优先权日:1988-05-23 标题 :Process for synthesis of E-2-methyl-α,β-unsaturated aldehydes 发明人:DESMOND RICHARD; MILLS SANDER G; VOLANTE RALPH P; SHINKAI ICHIRO 权利人:MERCK & CO INC 摘要:A process is described for the synthesis of E-2-methyl-α,β-unsaturated aldehydes, which are useful as intermediates in the synthesis of the macrolide structure of the immunosuppressant FK-506. These compounds are also useful as ultraviolet radiation absorbers.
[参考文献]: D Crich, Et Al. Direct Stereoselective Synthesis Of Beta-Thiomannosides. J Org Chem. 2000 Feb 11;65(3):801-5. [参考文献]: Katsumi Kobayashi, Et Al. Gacl(3)-Catalyzed Ortho-Ethynylation Of Phenols. J Am Chem Soc. 2002 Jul 24;124(29):8528-9. [参考文献]: Kou Hiroya, Et Al. Cyclization Reactions Of Homopropargyl Azide Derivatives Catalyzed By Ptcl4 In Ethanol Solution: Synthesis Of Functionalized Pyrrole Derivatives. Org Lett. 2006 Nov 9;8(23):5349-52.
合成参考文献
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