专利号:US-7893286-B2 优先权日:2007-06-01 标题 :Method for the synthesis of phospholipid ethers 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:Disclosed are improved methods for the synthesis of phospholipid ether analogs and alkyl phosphocholine analogs. The methods allow greater versatility of the reactants used and greater ease in synthesizing alkyl chains of varying length while affording reaction temperatures at room temperature or below. The methods disclosed herein provide reactants and conditions using alkyl halides and organozinc reagents and do not utilize Gringard reactions thus, allowing greater ease of their separation and purity of products. The PLE compounds synthesized by the methods disclosed herein can also be used for synthesizing high specific activity phospholipid ether (PLE) analogs, for use in treatment and diagnosis of cancer.
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-5565185-A 优先权日:1994-07-20 标 题 :Process for the preparation of radiolabeled meta-halobenzylguanidine 发明人:HUNTER DUNCAN H; GOEL ALOK; FLANAGAN RICHARD J 权利人:MERCK FROSST CANADA INC 摘要:The present invention provides a no-carrier-added synthesis of radiolabeled meta-halobenzylguanidine by halodestannylation which comprises reacting a meta-trialkylstannylbenzylguanidine with a source of radionuclide of a halogen. The present invention also provides meta-trialkylstannylbenzylguanidine as intermediates in the afore-mentioned process.
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-8022235-B2 优先权日:2007-06-01 标 题 :Compositions of phospholipid ether boronic acids and esters and methods for their synthesis and use 发明人:PINCHUK ANATOLY; WEICHERT JAMEY P; LONGINO MARC 权利人:CELLECTAR INC 摘要:The present invention discloses boronic acids and esters of phospholipid ether analogs and methods for their synthesis and use. The boronic acids and esters of phospholipid ether analogs described herein can be used in treating cancer and in particular can be used in conjunction with radiation therapy, such as external beam radiation therapy and neutron capture therapy to specifically target and kill cancer cells.
专利号:US-2008312459-A1 优先权日:2007-06-01 标 题 :Method for the synthesis of phospholipid ethers
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