非那西丁置于硫酸,氢溴酸,砷酸,原砷酸体系中,化学反应生成 6-羟基喹啉 参考文献:Fujita Et Al.,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1954,Vol. 74,P. 206 标题:Fujita Et Al.,Yakugaku Zasshi/journal Of The Pharmaceutical Society Of Japan,1954,Vol. 74,P. 206
专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
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-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.
专利号:EP-2173747-B1 优先权日:2007-06-26 标 题:A regioselective metal catalyzed synthesis of annelated benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARE MARC; R KYEN OMAR; URMANN MATHIAS; HALLAND NIS 权利人:SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, wherein R1; R2; R3; R4; J1; J2; J3; J4 and G have the meanings indicated in the claims. The present invention provides a direct metal, e.g. palladium or copper, catalyzed, regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-10927135-B2 优先权日:2017-08-03 标 题:Metal-free direct arylation of dialkyl phosphonates for the synthesis of mixed alkyl aryl phosphonates 发明人:KANG JUN YONG; HUANG HAI 权利人:THE BOARD OF REGENTS OF THE NEVADA SYSTEM OF HIGHER EDUCATION ON BEHALF OF THE UNIV OF NEVADA LAS VE 摘要:Provided herein are phosphates, thiophosphates, phosphonates, and phosphinates, methods of making same, and methods of using these compounds and methods for the generation of pharmaceutically relevant phosphate, phosphonate, and phosphinate analogs. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.
[参考文献]: G Bott, Et Al. Microbial Metabolism Of Quinoline And Related Compounds. Ix. Degradation Of 6-Hydroxyquinoline And Quinoline By Pseudomonas Diminuta 31/1 Fa1 And Bacillus Circulans 31/2 A1. Biol Chem Hoppe Seyler. 1991 Jun;372(6):381-3. [参考文献]: Junhong Qian, Et Al. Excited State Proton Transfer In The Cinchona Alkaloid Cupreidine. Phys Chem Chem Phys. 2010 Oct 21;12(39):12562-9. [参考文献]: Katharigatta Narayanaswamy Venugopala, Et Al. Synthesis And Antimosquito Properties Of 2,6-Substituted Benzo[参考文献]: M S Mehata, Et Al. Fluorescence Characteristics Of Protonated Form Of 6-Hydroxyquinoline In Nafion Film. Spectrochim Acta A Mol Biomol Spectrosc. 2003 Feb;59(3):559-67. [参考文献]: Mohan Singh Mehata, Et Al. Proton Translocation And Electronic Relaxation Along A Hydrogen-Bonded Molecular Wire In A 6-Hydroxyquinoline/acetic Acid Complex. J Phys Chem B. 2008 Jul 17;112(28):8383-6.
合成参考文献
摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 73. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 310. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 247. 摘要:Harsanyi, A.; Sandford, G., Science of Synthesis Knowledge Updates, (2015) 1, 172. 摘要:Huang, J.; Ma, D., Science of Synthesis: Special Topics, (2022) 1, 19.