专利号:US-2009198084-A1 优先权日:2006-05-02 标题:Process for the deprotection of protected amines 发明人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 权利人:ALSTERS PAULUS LAMBERTUS; VERKADE JORGE MERIJN MATHIEU; QUAEDFLIEG PETER JAN LEONARD MARIO; RUTJES FLORIS PETRUS JOHANNES 摘要:The present invention relates to a process for the deprotection of protected amine compounds, wherein the protected amine compound is contacted with an electrophilic oxidating agent that is optionally formed in situ, said electrophilic oxidating agent being selected from the group of I 2 , Br 2 , Cl 2 and compounds comprising a halogen atom having a formal oxidation state of 1+, 3+, 5+ or 7+, provided that the electrophilic oxidating agent is not iodobenzene diacetate. The process can be conveniently employed in the synthesis of 1,3-amino alcohols, β-amino acids and heterocyclic compounds, in particular β-amino acids.
专利号:US-4117234-A 优先权日:1972-08-17 标题:Intermediate in the synthesis of estrone 发明人:JOHNSON WILLIAM S; BARTLETT PAUL A 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Estrogenic steroids are synthesized by combining under conditions favoring the formation of a trans-olefin, a γ-arylpropanal with a 5,5,8,8-tetraalkoxy Wittig reagent. After hydrolysis of the gem-diethers, the resulting dioxo is internally condensed to form a cyclopentenone. The ketone is reduced to an oxy group and the resulting 2-(6'-arylhex-3'-enyl-1)cyclopent-2-en-1-ol or derivative thereof is cyclized to the Δ 13 ,17 -estrene, preferably 17-alkyl-Δ 13 ,17 -estrene with the A ring aromatized. After epoxidation, the 17-alkyl derivative is rearranged to form the 13-alkyl-1,3,5(10)-estratien-17-one. New compounds are provided as intermediates and final products.
专利号:US-8697032-B2 优先权日:2003-05-02 标题:Prosthetic groups attached to stannyl polymer in the synthesis of radiopharmaceuticals 发明人:HUNTER DUNCAN; GAGNON M KAREN J 权利人:UNIV WESTERN ONTARIO 摘要:The present invention relates to compositions and methods for preparing radiopharmaceutical compounds in high chemical-purity and isotopic-purity. The present invention provides polymer-bound precursors to radiopharmaceutical compounds that can be converted to radiopharmaceutical compounds in one step. In a preferred embodiment, a radiopharmaceutical precursor is bound to a polymeric support via a prosthetic group comprising an alkenyl-tin bond. The radiopharmaceutical precursor is converted to a radiopharmaceutical compound in one step involving cleavage of the alkenyl-tin bond and incorporation of a radioisotope to form the radiopharmaceutical compound. Importantly, the polymeric support containing the toxic tin by-product can be easily removed from the radiopharmaceutical compound by filtration. The present invention can be used to install a large number of different radioisotopes. In a preferred embodiment, the radioisotope is 211 At, 123 I, or 131 I.
专利号:US-2008312459-A1 优先权日:2007-06-01 标 题 :Method for the synthesis of phospholipid ethers
专利号:US-4293495-A 优先权日:1980-04-07 标 题:Symmetrical azetidinone aldehyde disulfides and process 发明人:KUKOLJA STJEPAN; PFEIL JANICE L 权利人:LILLY CO ELI 摘要:4R,4'R bis[1-(2-N-3-methyl-4-al-Z-but-2-ene-oate)-2-oxo-3S-acylamino azetidine]disulfide compounds are prepared by reacting the corresponding 7α-acylamino-2α-alkoxy-3-methyl-3-cephem-4-carboxylates first with an N-chloro halogenating agent, e.g., N-chlorosuccinimide, then with an aqueous suspension of mercury dichloride and cadmium carbonate. The disulfide compounds produced in this invention are intermediates in the synthesis of the biologically active 7β-acylamino-7α-alkoxy-3-methyl 1-oxa β-lactam antibiotic compounds.
专利号:CA-2524466-C 优先权日:2003-05-02 标题 :Prosthetic groups useful in the synthesis of radiopharmaceutical compounds
1: Nakai JS, Poon R, Lecavalier P, Chu I, Yagminas A, Valli VE. Effects of subchronic exposure of rats to dichloramine and trichloramine in drinking water. Regul Toxicol Pharmacol. 2000 Apr;31(2 Pt 1):200-9. 15: Cullen GE, Taylor HD. RELATIVE IRRITANT PROPERTIES OF THE CHLORINE GROUP OF ANTISEPTICS. J Exp Med. 1918 Nov 30;28(6):681-99. 16: Baker HW. The Treatment of Infected Wounds with Dichloramine-T with special Reference to its Advantages over the Carrol-Dakin Method. Can Med Assoc J. 1918 Sep;8(9):805-23.
合成参考文献
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