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-5763681-A 优先权日:1989-09-06 标 题 :Synthesis of stable, water-soluble chemiluminescent 1,2-dioxetanes and intermediates therefor 发明人:EDWARDS BROOKS; JUO RHOU-RONG 权利人:TROPIX INC 摘要:A novel synthesis of compound having the formula: ##STR1## wherein T is a stabilizing spiro-linked polycycloalkylidene group, R 3 is a C 1 -C 20 alkyl, aralkyl or heteroatom containing group, Y is an aromatic fluorescent chromophore, and Z is a cleavable group which, when cleaved, induces decomposition of the dioxetane ring and emission of optically detectable light, is disclosed. A tertiary phosphorous acid alkyl ester of the formula: n n (R.sup.1 O).sub.3 P n n wherein R 1 is a lower alkyl group, is reacted with an aryl dialkyl acetal produced by reacting a corresponding aryl aldehyde with an alcohol of the formula: n n R.sup.3 OH n n wherein R 3 is as defined above, to produce a 1-alkoxy-1-aryl-methane phosphonate ester of the formula: ##STR2## reacting the phosphonate with base to produce a phosphonate-stabilized carbanion, reacting the carbanion with a ketone of the formula: ##STR3## wherein T is as defined above, to produce an enol ether of the formula: ##STR4## then oxygenating the double bond in the enol ether to give the corresponding 1,2-dioxetane compound.
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:US-6469065-B1 优先权日:1996-02-02 标 题:Nitrosated and nitrosylated α-adrenergic receptor antagonist, compositions and methods of use 发明人:GARVEY DAVID S; SCHROEDER JOSEPH D; DE TEJADA INIGO SAENEZ; GASTON RICKY D; SHELEKHIN TATIANA E; WANG TIANSHENG 权利人:NITROMED INC 摘要:The present invention describes novel nitrosated and/or nitrosylated α-adrenergic receptor antagonists, and novel compositions containing at least one nitrosated and/or nitrosylated α-adrenergic receptor antagonist, and, optionally, one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or are a substrate for nitric oxide synthase, and/or one or more vasoactive agents. The present invention also provides novel compositions containing at least one α-adrenergic receptor antagonist, and one or more compounds that donate, transfer or release nitric oxide, elevate endogenous levels of endothelium-derived relaxing factor, stimulate endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or one or more vasoactive agents. The present invention also provides methods for treating or preventing sexual dysfunctions in males and females, for enhancing sexual responses in males and females, and for treating or preventing benign prostatic hyperplasia, hypertension, congestive heart failure, variant (Printzmetal) angina, glaucoma, neurodegenerative disorders, vasospastic diseases, cognitive disorders, urge incontinence, or overactive bladder, and for reversing the state of anesthesia.
专利号:US-7947701-B2 优先权日:2003-11-14 标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof 发明人:CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN 权利人:SANOFI AVENTIS 摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.
参考标题:Continuous-Flow Retro-Diels-Alder Reaction: A Process Window For Designing Heterocyclic Scaffolds 作者:Imane Nekkaa,Márta Palkó,István M. Mándity,Ferenc Miklós,Ferenc Fülöp |发布日期:2018.8.31 摘要:An Approach Based On A Highly Controlled Continuous‐flow (Cf) Retro‐diels-Alder Reaction Was Developed For The Synthesis Of New Compounds. Using This Approach, We Were Able To Rapidly Screen Reaction Conditions To Obtain The Desired Pyrimidinone Moieties In Short Reaction Times And High Yields. We Also Present An Alternative Route For The Synthesis Of Intermediates By Cf Cyclization.
合成参考文献
参考文献:10.1007/s00216-011-5196-8 摘要:Azam MG, Shibata T, Kabashima T, Kai M. Alkaline phosphatase-labeled macromolecular probe for sensitive chemiluminescence detection of proteins on a solid-phase membrane. Analytical and Bioanalytical Chemistry. 2011 Jul 15;401(4):1211. doi: 10.1007/s00216-011-5196-8.