专利号:US-2024409495-A1 优先权日:2021-10-20 标 题 :Process for the preparation of 2,7-dihydroxy-9-fluorenone useful for the synthesis of tilorone and its salts 发明人:JAISANKAR PARASURAMAN; DEB INDUBHUSAN; BHATTACHARJEE PINAKI 权利人:COUNCIL SCIENT IND RES 摘要:Methods involving preparation of building blocks of 2,7-dihydroxy-9-fluorenone toward the synthesis of tilorone dihydrochloride salt and other salts (bromide, iodide, fluoride, citrate, oxalate, maleate, phosphate, tartrate, triflate, trifluoroacetate, tetrafluoroborate) of tilorone, and an efficient, safe, cost effective method for the preparation of 2,7-bis-[2-(diethylamino)ethoxy]-fluorenone-9 and its various salts are developed. The methods involve oxygenation of fluorene, nitration of fluorenone, followed by reduction and diazotization toward the formation of 2,7-dihydroxy-9-fluorenone, which is the key intermediate for the formation of 2,7-bis-[2-(diethylamino)ethoxy]-9-fluorenone-dihydrochloride (Tilorone dihydrochloride) and other tilorone salts. The synthesis method has relatively simple operation, mild reaction conditions, high yield, and simple process with yields of 80-97%. Subsequent product purification of this method uses filtration and crystallization methods, avoiding the existing methods of column chromatography. Therefore, the research of its synthetic method being with a wide range of applications from the drug development and material synthesis point of view.
专利号:US-9376461-B2 优先权日:2011-06-06 标 题:Non-enzymatic synthesis of O-acetyl-ADP-ribose and analogues thereof 发明人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B 权利人:KOPPETSCH KARSTEN; SZCZEPANKIEWICZ BRUCE G; PERNI ROBERT B; GLAXOSMITHKLINE LLC 摘要:Provided herein is a simple, one-step, non-enzymatic synthesis of O-Acetyl-ADP-ribose (OAADPR) from NAD and sodium acetate in acetic acid. The extension of this reaction to other carboxylic acids, demonstrates that the reaction between NAD, and NAD analogs produces mixtures of the corresponding 2′- and 3′-carboxylic esters. Included are O-carboxyl-ADP-ribose compounds and corresponding methods of synthesis (e.g., O-propionyl-ADP-ribose, O-succinyl-ADP-ribose, O-malonyl-ADP-ribose), as well as non-adenosine nucleoside compounds.
专利号:US-10662452-B2 优先权日:2016-09-05 标 题 :Strain of meyerozyma guilliermondii and its use in methods of catalytic synthesis of 2,5-dihydroxymethylfuran 发明人:LI NING; LI YANMEI; ZONG MINHUA 权利人:UNIV SOUTH CHINA TECH 摘要:A yeast strain and a method for the synthesis of 2,5-dihydroxymethylfuran using this strain are disclosed. The yeast strain is Meyerozyma guilliermondii SC 1103, which has been maintained in the China Center for Type Culture Collection (CCTCC, Wuhan, P.R. China) with an access No. of M2016144. The method for the synthesis of 2,5-dihydroxymethylfuran using this strain is described as follows: after pre-cultivation and cultivation, Meyerozyma guilliermondii SC 1103 cells are added into the buffer solutions containing 5-hydroxymethylfurfural and glucose; the biocatalytic reaction is conducted under designated conditions, thus affording 2,5-dihydroxymethylfuran. This disclosure has many advantages such as good selectivity, mild reaction conditions, environmental friendliness, high efficiency, and good yield.
专利号:US-2010087658-A1 优先权日:1996-08-06 标 题 :Methods and intermediates for synthesis of selective dpp-iv inhibitors 发明人:CAMPBELL DAVID ALAN; LEITAO EMILIA P T; WU ZHEN-PING; WANG PENG 权利人:PHENOMIX CORP 摘要:Methods and intermediates for the synthesis of selective inhibitors of dipeptidyl peptidase IV (DPP-IV) are provided. Coupling of a carboxylate salt with a boro-proline derivative provides a protected form of a DPP-IV inhibitor, which may be deblocked to yield the medicinal compound. The carboxylate salt can be a crystalline form of a sodium salt or a dicyclohexylammonium salt. The inhibitor can be used in the treatment of diabetes.
专利号:US-2024239737-A1 优先权日:2023-01-13 标题 :Synthesis of Triisoamyl Citrate (Triisopentanol) and its Applications as a Solvent, Plastizer and Component of Cosmetic and Aerosol Formulations 发明人:SATO SETSUO 权利人:BRASIL BIO FUELS S A 摘要:The present invention is based on the synthesis of triisoamyl citrate (triisopentanol citrate) and its applications as a plasticizer for polyvinyl chloride polymers, natural and synthetic rubbers, industrial solvents, replacing petrochemical-based products such as Phthalates (Dioctyl Phthalate, Diisononyl Phthalate, Dibutyl Phthalate), Acetylated tributylcitrate, epoxidized fatty esters, isoparaffins. It is a 100% renewable, high-performance, non-toxic, biodegradable product with an extremely competitive cost. With the increase in corn alcohol production in Brazil, this technology and product adds value to the fusel oil co-product generated in corn alcohol plants.
专利号:US-4029768-A 优先权日:1971-03-16 标 题 :Composition for application to the animal brain for synthesis of brain components involved in the learning process, and method 发明人:PENN NATHAR W 权利人:PENN NATHAR W 摘要:A composition for application to the animal brain (this term is used to include both humans and lower animals) for synthesis of brain components involved in the learning process, thereby facilitating learning. The composition comprising brain deoxyribonucleic acid containing 5-hydroxymethyloytosine ranging from about 8 to 15% of the total cytosines present. The invention includes dosage and method of preparation.
摘要:Resch, V.; Hanefeld, U., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 276. 参考文献:10.1021/bi030213b 摘要:Huang J, Lipscomb WN. Aspartate Transcarbamylase (ATCase) of Escherichia coli: A New Crystalline R-State Bound to PALA, or to Product Analogues Citrate and Phosphate,. Biochemistry. 2004 May 06;43(21):6415–21. doi: 10.1021/bi030213b. 参考文献:10.1074/jbc.m111.242362 摘要:Kocher O, Birrane G, Yesilaltay A, Shechter S, Pal R, Daniels K, Krieger M. Identification of the PDZ3 Domain of the Adaptor Protein PDZK1 as a Second, Physiologically Functional Binding Site for the C Terminus of the High Density Lipoprotein Receptor Scavenger Receptor Class B Type I. Journal of Biological Chemistry. 2011 Jul;286(28):25171–86. doi: 10.1074/jbc.m111.242362. 参考文献:10.1073/pnas.1103187108 摘要:Christoffersen C, Obinata H, Kumaraswamy SB, Galvani S, Ahnström J, Sevvana M, Egerer-Sieber C, Muller YA, Hla T, Nielsen LB, Dahlbäck B. Endothelium-protective sphingosine-1-phosphate provided by HDL-associated apolipoprotein M. Proc Natl Acad Sci U S A. 2011 Jun 07;108(23):9613–8. 参考文献:10.1038/cr.2012.177 摘要:Zhang Q, Qi S, Xu M, Yu L, Tao Y, Deng Z, Wu W, Li J, Chen Z, Wong J. Structure-function analysis reveals a novel mechanism for regulation of histone demethylase LSD2/AOF1/KDM1b. Cell Res. 2013 Feb;23(2):225–41.