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-2023242581-A1 优先权日:2020-06-17 标题:Synthesis of a guanylate cyclase agonist by fragments based approach 发明人:SAMBASIVAM GANESH; KASTURCHAND GODHA ATUL; VENKATA BHAGYARAJ ARETI; ANNADURAI SATHYA; VEERANJANEYULU AVULA; VASANTRAO GADAKH AMOL; S JADHAV DIPAK 权利人:ANTHEM BIOSCIENCES PRIVATE LTD 摘要:The present invention provides a process for the synthesis of Plecanatide, a guanylate cyclase agonist. The process involves convergent synthesis with compounds, i.e., fragment of peptides followed by cyclization. The method provides high yield of Plecanatide with less impurities.
专利号:US-5139940-A 优先权日:1989-10-26 标题 :Activation compounds and methods of synthesis of activation compounds 发明人:ISAACS STEPHEN T; CIMINO GEORGE D; METCHETTE KENNETH C; TESSMAN JOHN W 权利人:ISAACS STEPHEN T; CIMINO GOERGE D; METCHETTE KENNETH C; TESSMAN JOHN W 摘要:The invention is directed to isopsoralen compound compositions that contain a variety of substitutions which yet permit their binding to nucleic acid polymers. Reaction conditions that activate these bound isopsoralens results in covalent crosslinking to the nucleic acid polymers. The resultant complex is inhibited from being a template for the template-directed enzymatic synthesis of a complementary nucleic acid polymer. Beside the isopsoralens compositions, the invention includes their synthesis, the nucleic acid complex production and detection, and the above inhibitory method of use of the isopsoralens.
专利号:US-12410140-B2 优先权日:2020-06-19 标题:Method for synthesis of roxadustat and intermediate thereof, and intermediate thereof 发明人:ZHANG YONG; WANG GUO; YANG FEI; LIU FENGWEI; ZHOU CHUNDONG; ZHANG ZITONG 权利人:JUMPCAN SHANGHAI MEDICAL TECH CO LTD 摘要:Disclosed are a method for the synthesis of roxadustat and an intermediate thereof, and an intermediate thereof. In particular, disclosed is a method for the synthesis of compound M1, the method comprising the following steps: carrying out a reaction as shown below between compound SM and compound SM-A under the action of an oxidizing agent. The method of the present invention uses cheap and easily available raw materials, has short reaction steps, produces a high yield, has simple and convenient post-treatment procedures, and is suitable for industrial production.
专利号:US-4849513-A 优先权日:1983-12-20 标 题 :Deoxyribonucleoside phosphoramidites in which an aliphatic amino group is attached to the sugar ring and their use for the preparation of oligonucleotides containing aliphatic amino groups 发明人:SMITH LLOYD M; FUNG STEVEN; KAISER ROBERT J 权利人:CALIFORNIA INST OF TECHN 摘要:The invention consists of compounds and methods for the synthesis of oligonucleotides which contain one or more free aliphatic amino groups attached to the sugar moieties of the nucleoside subunits. The synthetic method is versatile and general, permitting amino groups to be selectively placed at any position on oligonucleotides of any composition or length which is attainable by current DNA synthetic methods. Fluorescent dyes or other detectable moieties may be covalently attached to the amino groups to yield the corresponding modified oligonucleotide.
专利号:US-11945957-B2 优先权日:2017-10-17 标题 :Aqueous composition and a method of producing durable and extremely efficient water repelling superhydrophobic materials at ambient condition thereof 发明人:THALAPPIL PRADEEP; BAIDYA AVIJIT; GANAYEE MOHD AZHARDIN; RAVINDRAN SWATHY JAKKA 权利人:INDIAN INSTITUTE OF TECH MADRAS; INDIAN INST TECH MADRAS 摘要:The present invention relates to a durable and multifunctional superhydrophobic coating composition and water based fabrication method of producing the durable and multifunctional superhydrophobic coating composition via chemical modification and functionalization of hydrophilic material by silanes under room temperature without any organic solvents. Synthesis of chemically modified cellulose nanofibers or clay in water forms excellent water repelling thin films upon coating over various substrates. The super hydrophobic materials are used as additive for paints, pigments, paper, varnish and, textile and used for various industrial applications such as construction of buildings and other super structures.
参考文献:10.1016/s0378-4347(01)00267-5 摘要:Berrueta LA, Fernández-Armentia M, Bakkali A, Gonzalo A, Lucero ML, Orjales A. Matrix solid-phase dispersion technique for the determination of a new antiallergic drug, bilastine, in rat faeces. Journal of Chromatography B: Biomedical Sciences and Applications. 2001 Aug;760(1):185–90. doi: 10.1016/s0378-4347(01)00267-5. 参考文献:10.1093/jaoac/91.1.67 摘要:Sippel J, Sfair LL, Schapoval EES, Steppe M. New High-Performance Liquid Chromatographic Method for Determination of Clopidogrel in Coated Tablets. 2008 Jan 01;91(1):67–72. doi: 10.1093/jaoac/91.1.67. 参考文献:10.1186/1476-511x-10-85 摘要:Inoue N, Nagao K, Sakata K, Yamano N, Gunawardena PER, Han S, Matsui T, Nakamori T, Furuta H, Takamatsu K, Yanagita T. Screening of soy protein-derived hypotriglyceridemic di-peptides in vitro and in vivo. Lipids in Health and Disease. 2011 May 22;10(1):85. doi: 10.1186/1476-511x-10-85. 参考文献:10.1016/s1570-0232(02)00310-0 摘要:Buratti M, Valla C, Xaiz D, Brambilla G, Colombi A. Determination of hexafluoroisopropanol, a sevoflurane urinary metabolite, by 9-fluorenylmethyl chloroformate derivatization. J Chromatogr B Analyt Technol Biomed Life Sci. 2002 Sep 05;776(2):237–43. doi: 10.1016/s1570-0232(02)00310-0.