CAS: 4049-33-6; (2S,3R,4S,5R)-Tetrahydro-2H-Pyran-2,3,4,5-Tetrayl Tetraacetate

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专利信息

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:WO-9839347-A3
优先权日:1997-03-05
标题:Synthesis of l-ribose and 2-deoxy l-ribose
发明人：JUNG MICHAEL E; XU YUE
权利人:UNIV CALIFORNIA; JUNG MICHAEL E; XU YUE
摘要:A method for synthesizing L-ribose (1) and 2-deoxy L-ribose (12) from inexpensive D-ribose (2) is provided. The 5-O-trityl ribose (3) (prepared in 70 % yield from D-ribose) is reduced with borohydride to give the tetrol (4), which is then peracetylated to the tetraacetate (5). Hydrolysis of the trityl ether followed by Swern oxidation affords the aldehyde (7) via the alcohol (6). This aldehyde is a protected form of L-ribose, being L-ribose 2,3,4,5,-tetraacetate. Mild basic hydrolysis of the acetate affords L-ribose itself (1), thus ending an efficient six-step synthesis of (1) from (2) which proceeds in 39 % overall yield. In a second aspect of the invention, L-ribose is converted into the β-selenophenyl ribofuranoside (10) via the tetraester (9) in 71 % isolated yield for the four steps. Treatment of (10) with tributylstannane and AIBN furnishes in 84 % yield the tribenzoyl 2-deoxy-L-ribofuranoside (11) which, on basic hydrolysis, gives 2-deoxy L-ribose (12) in high yield. In a third aspect of the invention, L-arabinose (13) is converted into 2-deoxy L-ribose (12) via the arabinopyranosyl bromide (14), via similar reductive rearrangement with tributylstannane to give the 2-deoxy ribopyranose tribenzoate (16). Hydrolysis yields 2-deoxy L-ribose. In a third aspect of the invention, L-arabinose is converted into 2-deoxy L-ribose by an alternate route.

专利号:WO-02085848-A8
优先权日:2001-04-18
标 题 :Synthesis of pancratistatin prodrugs
发明人：PETIT GEORGE R; ORR BRIAN; DUCKI SYLVIE
权利人:UNIV ARIZONA STATE; PETIT GEORGE R; ORR BRIAN; DUCKI SYLVIE
摘要:A new and efficient synthesis of the (+)-pancratistatin phosphate prodrug 2a has been accomplished. Selective protection (tetraacetate 4) of (+)-pancratistatin (1a) was followed by phosphorylation (to 5) with dibenzyl chlorophosphite (prepared in situ from dibenzyl phosphite). Cleavage of the acetate (with sodium methoxide) and benzyl (by hydrogenolysis) protecting groups followed by concomitant reaction with two equivalents of sodium methoxide afforded good yield of disodium (+)-pancratistatin phosphate (2a). Further increases in yields of the prodrug (2a) were realized by avoiding heat in the final purification steps. Fourteen (2b-o) additional metal and ammonium derived phosphate prodrugs were also synthesized.

专利号:US-8333952-B2
优先权日:2009-09-23
标 题:Dose synthesis module for biomarker generator system
发明人：NUTT RONALD; GIAMIS ANTHONY M; MCFARLAND AARON
权利人:NUTT RONALD; GIAMIS ANTHONY M; MCFARLAND AARON; ABT MOLECULAR IMAGING INC
摘要:A microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, one (1) unit dose of a radiopharmaceutical biomarker for use in positron emission tomography (PET). The radiopharmaceutical production system includes a reaction vessel that receives a radioisotope from an accelerator or other radioisotope generator. Organic and aqueous reagents are introduced into the reaction vessel, and the mixture is heated to synthesize a solution of a pre-selected radiopharmaceutical. The radiopharmaceutical solution is purified by passing the solution through a solid phase extraction column and a filter. The synthesis process produces per run a quantity of radiopharmaceutical approximately equal to, but not less than, one (1) unit dose of a radiopharmaceutical, reducing waste and allowing for the production of radiopharmaceutical on an as-needed basis. The synthesis process allows for the production of biomarker radiopharmaceuticals on site and close to the location where the unit dose will be administered to the patient. On-site, as-needed production of radiopharmaceuticals in small doses reduces the time between the synthesis of the radiopharmaceutical and the administration of that radiopharmaceutical, thereby minimizing the loss of active isotopes through decay and allowing the production of lesser amounts of radioisotopes overall.

专利号:US-10109385-B2
优先权日:2009-09-23
标题:Dose synthesis card for use with automated biomarker production system
发明人：MCFARLAND AARON; ANZELLOTTI ATILIO; HILLESHEIM DANIEL; BROWN-PROCTOR CLIVE; KHACHATURIAN MARK HAIG; LAND ANDREW
权利人:ABT MOLECULAR IMAGING INC
摘要:Microfluidic radiopharmaceutical production system and process for synthesizing per run approximately, but not less than, ten (10) unit doses of radiopharmaceutical biomarker for use in positron emission tomography (PET). A radioisotope from an accelerator or other radioisotope generator is introduced into a reaction vessel, along with organic and aqueous reagents, and the mixture heated to synthesize a solution of a pre-selected radiopharmaceutical. The solution is purified by passing through a combination of solid phase extraction purification components, trap and release components, and a filter. The synthesis process reduces waste and allows for production of biomarker radiopharmaceuticals on site and close to the location where the unit dose will be administered to the patient. On-site, as-needed production of radiopharmaceuticals in small doses reduces the time between synthesis of the radiopharmaceutical and administration of that radiopharmaceutical, minimizing loss of active isotopes through decay and allowing production of lesser amounts of radioisotopes overall.

专利号:US-8987430-B2
优先权日:2009-10-30
标 题:Efficient and scalable process for the manufacture of fondaparinux sodium
发明人：PATEL PAYAL PARTH; MA CHUN; OHRR KEVIN K; NADJI SOURENA
权利人:PATEL PAYAL PARTH; MA CHUN; OHRR KEVIN K; NADJI SOURENA; RELIABLE BIOPHARMACEUTICAL CORP
摘要:The present invention relates to a process for the synthesis of the Factor Xa anticoagulent Fondaparinux and related compounds. The invention relates, in addition, to efficient and scalable processes for the synthesis of various intermediates useful in the synthesis of Fondaparinux and related compounds.