专利号:US-9085518-B2 优先权日:2011-10-14 标题 :Method for the synthesis of 18F-labelled molecules 发明人:NAIRNE ROBERT JAMES DOMETT; BHALLA RAJIV; KHAN IMTIAZ; BROWN JANE; WILSON ANTHONY; BLACK ANDRES 权利人:GE HEALTHCARE LTD 摘要:The present invention provides a method for the synthesis of 18F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, in a preferred embodiment, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.
专利号:US-6417380-B1 优先权日:1987-12-31 标 题 :Synthesis of 1,2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 摘要:Compounds having the formula: n wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., n m-phenylene), produced by reacting a compound having the formula: n with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: n are produced by reacting a compound having the formula: n with n wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula n are produced by reacting a compound of the formula n with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:US-4237054-A 优先权日:1979-05-18 标 题 :Total synthesis of (1RS,4SR,5RS)-4-(4,8-dimethyl-5-hydroxy-7-nonenyl)-4-methyl-3,8-dioxabicyclo[3.2.1] octane-1-acetic acid 发明人:CHEN ROBERT H K 权利人:ORTHO PHARMA CORP 摘要:A method for the total synthesis of (1RS,4SR,5RS)-4-(4,8-dimethyl-5-hydroxy-7-nonenyl)-4-methyl-3,8-dioxabicyclo [3.2.1] octane-1-acetic acid is described. The compound is active as a utero-evacuant agent.
专利号:US-9125954-B2 优先权日:2011-10-14 标 题 :Method for the synthesis of 18F-labelled biomolecules 发明人:BHALLA RAJIV; WILSON ANTHONY; KHAN IMTIAZ; BROWN JANNE 权利人:GE HEALTHCARE LTD 摘要:The present invention provides a method for the synthesis of 18 F-labelled biomolecules, which is amenable to automation. The present invention also provides a cassette for automating the method of the invention. The method of the present invention provides numerous advantages over the prior art methods. One less purification step is required as compared with known methods. Also, one less reagent is required as a particular reagent is employed in two different steps. The chemistry process is thereby simplified, the cost of goods is reduced and the burden of validation and documentation of reagents required for GMP clinical production is minimized.
专利号:US-5777133-A 优先权日:1987-12-31 标 题:Synthesis of 1, 2-dioxetanes and intermediates therefor 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 权利人:TROPIX INC 摘要:Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (eg., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
专利号:US-4956477-A 优先权日:1987-12-31 标 题:Synthesis of 1,2-dioxetanes 发明人:BRONSTEIN IRENA Y; EDWARDS BROOKS 权利人:TROPIX INC 摘要:Compounds having the formula: ##STR1## wherein T is a polycycloalkylidene group (e.g., adamant-2-ylidene); R is a C 1-20 alkyl, aralkyl or cycloalkyl group; and Y is a fluorescent chromophore (e.g., m-phenylene), produced by reacting a compound having the formula: ##STR2## with an R-ylating agent (e.g., R 2 SO 4 ) in the presence of an alkali metal alkoxide in a polar aprotic solvent. Also, compounds having the formula: ##STR3## are produced by reacting a compound having the formula: ##STR4## wherein X is an electronegative leaving group (e.g., a halogen anion such as chloride ion) in the presence of a Lewis base (e.g., a trialkyl-amine) dissolved in an aprotic organic solvent (e.g., benzene or toluene). Also, compounds having the formula ##STR5## are produced by reacting a compound of the formula ##STR6## with a tetra-O-acylated-O-hexopyranoside halide, then hydrolyzing off the protective acyl groups. The aforementioned compounds and procedures are useful in the synthesis of enzyme-cleavable 1,2-dioxetane ring systems that can serve as members of a binding pair employed, for example, in chemiluminescent immunoassays, DNA probe assays, and direct assays for an enzyme.
参考标题:Synthesis Of Difunctional Oxyethylene-Based Compounds 摘要:A Method Of Reacting A Toluenesulfonyl-Terminated Polyoxyethylene Compound Having The Formula Ch 3 -C 6 H 4 -So 2 -(O-Ch 2 -Ch 2 ) N -O-R 1 With An Ammonium Salt Having The Formula Nr 2 4 X To Form A Compound Having The Formula X-Ch 2 -Ch 2 -(O-Ch 2 -Ch 2 ) N-1 -R 3 . The Value N Is A Positive Integer. X Is A Halogen, Cyanide, Cyanate, Thiocyanate, Or Azide. R 1 Is A Terminating Group. Each R 2 Is Hydrogen Or An Alkyl Group. -R 3 Is -O-R 1 Or -X.
合成参考文献
摘要:Eilbracht, P., Science of Synthesis, (2009) 48, 394. 摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 38. 摘要:Weast, R.C. (ed.). Handbook of Chemistry and Physics. 60th ed. Boca Raton, Florida: CRC Press Inc., 1979., p. C-530 摘要:GENE-TOX Program: Current Status of Bioassay in Genetic Toxicology. U.S. Environmental Protection Agency, Washington, DC. Office of Toxic Substances and Pesticides. (For program information, contact Environmental Mutagen Information Center, Oak Ridge National Laboratory, Post Office Box Y, Oak Ridge, Tennessee 37830. Telephone (615) 574-7871) 摘要:Budavari, S. (ed.). The Merck Index - Encyclopedia of Chemicals, Drugs and Biologicals. Rahway, NJ: Merck and Co., Inc., 1989., p. 605