专利号:WO-2025108921-A1 优先权日:2023-11-22 标 题 :Synthesis of radiopharmaceutical agents 发明人:AUZELOUX PHILIPPE; LEVESQUE SOPHIE; GALMIER MARIE-JOSÈPHE; CHEZAL JEAN-MICHEL 权利人:INST NAT SANTE RECH MED; UNIV CLERMONT AUVERGNE; CENTRE LUTTE CONTRE LE CANCER 摘要:Synthesis of radiopharmaceutical agents It is disclosed a method to synthesize a compound of formula (I), or a pharmaceutically acceptable salt thereof: Formula (I), (I) said process comprising contacting a trialkylstannane precursor of formula (II), or a pharmaceutically acceptable salt thereof: Formula (II), (II) with an alkali metal salt of a radionuclide selected from the group consisting of 123I, 124I, 125I, 131I, 211At, in appropriate acidic conditions and in presence of a peroxide ROOH in an 10 appropriate concentration. Said method is particularly suited for synthesizing [131I]N-(2- diethylaminoethyl)-6-iodoquinoxaline-2-carboxamide, providing a notable reduction in the quantity of side products, allowing a much purer finished product, while making use of reagents which are adapted to the constraints which need to be met when developing a product for clinical use and, more in particular, to the constraints to be met in order to 15 adapt the process for being fully automated.
专利号:US-6509506-B1 优先权日:1997-05-21 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L- α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively, divalent ligands are preferred over monovalent ligands because of their enhanced regio-and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydoxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L- α-amino acid or D- and L-α-amino aldehyde.
专利号:US-6573387-B1 优先权日:1997-03-21 标 题 :Synthesis of α,β-substituted amino amides, esters, and acids 发明人:SHARPLESS K BARRY; RUBIN A ERIK 权利人:SCRIPPS RESEARCH INST 摘要:α,β-Unsaturated amides and esters are converted to α,β-substituted amino amides, esters, and acids. An α,βunsaturated amide or ester is first converted to an α,β-hydroxysulfonamide or hydroxycarbamate amide or ester using an osmium-catalyzed aminohydroxylation. The α,β-hydroxysulfonamide or hydroxycarbamate amides or esters is then cyclodehydrated to produce a α,β-N-sulfonyl- or the α,β-N-carbamoylaziridine amide or ester. The ring of aziridine intermediate is then nucleophilically opened in a regioselective manner with a variety of nucleophiles to give the $g(α,β-substituted amino- amides or esters. Preferred nucleophiles include sulfur, oxygen, carbon, and nitrogen nucleophiles.
专利号:US-5994583-A 优先权日:1996-05-22 标 题 :Two step synthesis of D- and L- α-amino acids and D- and L- α-amino-aldehydes 发明人:SHARPLESS K BARRY; LI GUIGEN 权利人:SCRIPPS RESEARCH INST 摘要:D- and L-α-amino acids and D- and L-α-amino aldehydes are synthesized from olefin substrates in two steps. The first step is a catalyzed asymmetric aminohydroxylation addition reaction to the olefin substrate. The addition reaction is catalyzed by osmium and is co-catalyzed by chiral ligands. The chiral ligands, in addition to being co-catalysts with the osmium, also serve to direct the addition reaction regioselectively and enantioselectively. Divalent ligands are preferred over monovalent ligands because of their enhance regio- and enantio-selectivity. As an oxidant nitrogen source for the addition reaction, either a carbamate or sulfonamide may be employed. If carbamate is employed as an oxidant nitrogen source, the resultant β-hydroxycarbamate is deprotected to yield the corresponding β-hydroxyamine. If sulfonamide is employed as an oxidant nitrogen source, the resultant β-hydroxysulfonamide is deprotected to yield the corresponding β-hydroxyamine. The resultant β-hydroxyamine is then selectively oxidized in a second synthetic step to produce the desired D- and L-α-amino acid or D- and L-α-amino aldehyde.
专利号:US-4107176-A 优先权日:1976-04-23 标题:Mono-N-tosylsulfimides, their preparation and their reaction products 发明人:EVANS DAVID H; GREENWALD RICHARD B 权利人:POLAROID CORP 摘要:This application is directed to cycloalkanes containing the moiety -SO2-CH2-X- wherein X represents +TR wherein R is hydrogen or alkyl and R' is alkyl and to the preparation of these compounds which find utility as silver halide complexing agents. This application is also concerned with cycloalkanes containing the moiety useful as intermediates in the preparation of the aforementioned compounds. Also included within the confines of this disclosure are the 2-thioether-substituted derivatives of certain of the above-identified cycloalkanes and with the synthesis of all of these compounds.
专利号:RU-2536686-C1 优先权日:2013-08-08 标题:Method of regioselective synthesis of monohalogenderivatives of 1,2-, 1,7-, 1,12-dicarba-closo-dodecarboranes(12) with application of ultrasound activation
[参考文献]: Kloth Lc, Et Al. Bactericidal And Cytotoxic Effects Of Chloramine-T On Wound Pathogens And Human Fibroblasts In Vitro. Adv Skin Wound Care. 2007 Jun;20(6):331-45. [参考文献]: Kuklina I, Et Al. Investigation Of Chloramine-T Impact On Crayfish Astacus Leptodactylus (Esch., 1823) Cardiac Activity. Environ Sci Pollut Res Int. 2014 Sep;21(17):10262-9. [参考文献]: Martínez Ma, Et Al. Induction Of Cytochrome P450-Dependent Mixed Function Oxidase Activities And Peroxisome Proliferation By Chloramine-T In Male Rat Liver. Food Chem Toxicol. 2017 Aug;106(Pt A):86-91. [参考文献]: Shim I, Et Al. Inhalation Exposure To Chloramine T Induces Dna Damage And Inflammation In Lung Of Sprague-Dawley Rats. J Toxicol Sci. 2013;38(6):937-46. [参考文献]: F C Greenwood, Et Al. The Preparation Of I-131-Labelled Human Growth Hormone Of High Specific Radioactivity. Biochem J. 1963 Oct;89(1):114-23.
合成参考文献
参考文献:10.1038/srep15194 摘要:Baumann T, Carvalho TS, Lussi A. The effect of enamel proteins on erosion. Scientific Reports. 2015 Oct 15;5(1):15194. doi: 10.1038/srep15194.