专利号:US-2024294462-A1 优先权日:2023-02-15 标题:Method for the Synthesis of Ionizable Lipids Using a Doubly Alkylated Intermediate 发明人:SAADATI FARIBA; TRAN HUY; CIUFOLINI MARCO; ATMURI N D PRASAD 权利人:NANOVATION THERAPEUTICS INC 摘要:Provided herein is a method for the preparation of ionizable, cationic amino lipids using a doubly alkylated nucleophilic intermediate to produce a ketone. The ketone, or a corresponding alcohol, is subjected to one or more synthesis steps to add an ionizable moiety thereto. The method can be advantageously employed for the synthesis of unsymmetrical analogues of the above lipids that would be considerably more difficult to make by alternative strategies. The method can also be used to prepare symmetrical ionizable, cationic amino lipids with fewer steps and/or with the use of fewer hazardous chemicals than known synthesis methods.
专利号:US-10730904-B2 优先权日:2012-11-14 标 题:Method for liquid-phase synthesis of nucleic acid 发明人:NONOGAWA MITSURU; NAGATA TOSHIAKI; SAITO HIDEKI; YASUMA TSUNEO 权利人:TAKEDA PHARMACEUTICALS CO 摘要:In this method, an oligonucleotide represented by formula (II) [wherein Y 1 , Q, Base, r and r′ are each as defined in claim 1 ] is prepared by using, as a synthesis unit, a novel nucleoside monomer compound represented by formula (I) [wherein X, R 1 , Y, Base, Z, Ar, R 2 , R 3 and n are each as defined in claim 1 ]. The novel nucleoside monomer compound is a nucleoside, the base moiety of which is substituted with an aromatic-hydrocarbon-ring-carbonyl or -thiocarbonyl group having at least one hydrophobic group. The method can dispense with column-chromatographic purification in every reaction, and enables base elongation not only in the 3′-direction but also in the 5′-direction, thus attaining efficient liquid-phase mass synthesis of an oligonucleotide.
专利号:US-10751285-B1 优先权日:2019-05-14 标题 :Synthesis of C resorcinarene based novel amphiphilic supramolecular macrocycle as nano-scale drug loading system 发明人:SHAH MUHAMMAD RAZA; ALI IMDAD; ALI HEYAM SAAD; EL-HAJ BABIKER M; IMRAN MUHAMMAD 权利人:SHAH MUHAMMAD RAZA; ALI IMDAD; ALI HEYAM SAAD; EL-HAJ BABIKER M; IMRAN MUHAMMAD 摘要:A drug delivery system comprising the synthesis of resorcinarene based novel amphiphilic supramolecular macrocycle that is capable of self-assembling in nano-scale vesicles upon its contact with aqueous medium and its use as nano-drug loading vehicle when mixed with cholesterol (2:1 ratio w/w).
专利号:WO-2025109557-A1 优先权日:2023-11-24 标题:Process for the synthesis of monoesters of ethylenediaminetetraacetic acid 发明人:TERAZONO YUICHI 权利人:NUTRIEN AG SOLUTIONS CANADA INC 摘要:A process for the synthesis of a compound of Formula (I) is provided. (I) wherein R is selected from the group consisting of alkyl, alkenyl, alkynyl, and steroidyl. The process comprises reacting a compound of Formula (IIa), Formula (IIb) or a mixture thereof with a compound of Formula R-X, to obtain a compound of Formula (IIIa), a compound of Formula (IIIb) or a mixture thereof, wherein A+ is a cesium cation, a quaternary ammonium cation or a quaternary phosphonium cation, and X is a leaving group; and reacting the compound of Formula (IIIa), compound of Formula (IIIb) or mixture thereof with an acid to obtain a reaction product which comprises the compound of Formula (I). (IIa) (IIb) (IIIa) (IIIb)
专利号:US-4594426-A 优先权日:1980-01-17 标题 :Benzoxazole derivative intermediates for synthesis of dye releasing redox compounds 发明人:FUJITA SHINSAKU; KOYAMA KOICHI; INAGAKI YOSHIO 权利人:FUJI PHOTO FILM CO LTD 摘要:Benzoxazole derivatives represented by general formula (I) which are intermediates for synthesis of o-sulfonamidophenol derivatives useful as dye releasing redox compounds in a color diffusion transfer color image forming process: ##STR1## wherein R 1 and R 2 , which may be the same as or different from each other, each represents an alkyl group or an aryl group or they may combine and form a ring; R 3 represents a hydrogen atom, an alkyl group or an aryl group; R 4 represents an alkyl group or an aryl group; R 5 represents an alkyl group, an alkoxy group, an alkylthio group, an arylthio group, a halogen atom or an acylamino group, or --CR 1 R 2 R 3 and R 5 may combine and form the nucleus ##STR2## which is condensed at the 6- and the 7-positions of the benzoxazole nucleus; and n is 0, 1 or 2.
专利号:US-8153615-B2 优先权日:2005-06-10 标 题:Synthesis of glycerolipid carbamates and dicarbamates and their use as an antitumor compounds 发明人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 权利人:BITTMAN ROBERT; BYUN HOE-SUP; ARTHUR GILBERT 摘要:The syntheses and in vitro antitumor properties of carbamate-containing, dicarbamate-containing, and ureido-containing phospholipid compounds that have an ether linkage at the C-1 position of a glycerol backbone, a carbamate, dicarbamate, or ureido moiety at the C-2 position of the glycerol backbone, and a phosphocholine, phosphonocholine, or glycoside moiety at the C-3 position of the glycerol backbone are described. The synthesis and antiproliferative activity of ether lipids with a naphthol moiety at the C-1 position are also described. These compounds were shown to be potent inhibitors of cancer cell growth. These compounds are useful for killing cancer cells and treating cancer.
[参考文献]: Agustín Molina-Ontoria, Et Al. Preparation And Characterization Of Soluble Carbon Nano-Onions By Covalent Functionalization, Employing A Na-K Alloy. Chem Commun (Camb). 2013 Mar 25;49(24):2406-8. [参考文献]: Andreas Hkansson, Et Al. A Method For Estimating Effective Coalescence Rates During Emulsification From Oil Transfer Experiments. J Colloid Interface Sci. 2012 May 15;374(1):25-33. [参考文献]: Bhowmira Rathore, Et Al. Cationic Lipid-Conjugated Hydrocortisone As Selective Antitumor Agent. Eur J Med Chem. 2016 Jan 27:108:309-321. [参考文献]: Christiaan Ridings, Et Al. Change Of Surface Structure Upon Foam Film Formation. Chemphyschem. 2015 Mar 16;16(4):733-8. [参考文献]: Julfikar Hassan Mondal, Et Al. Dual Self-Sorting By Cucurbit[8]Uril To Transform A Mixed Micelle To Vesicle. Langmuir. 2014 Oct 7;30(39):11528-34.
合成参考文献
摘要:Haino, T.; Iwamoto, H., Science of Synthesis, (2010) 45, 1233. 摘要:Haino, T.; Iwamoto, H., Science of Synthesis, (2010) 45, 1210. 摘要:Haino, T.; Iwamoto, H., Science of Synthesis, (2010) 45, 1240. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 87. 摘要:Braun, M., Science of Synthesis Knowledge Updates, (2017) 1, 448.