专利号:US-5442065-A 优先权日:1993-09-09 标 题:Synthesis of tetrahydroquinoline enediyne core analogs of dynemicin 发明人:MAGNUS PHILIP D; ILIADIS THEODORE; EISENBEIS SHANE A; FAIRHURST ROBIN A 权利人:UNIV TEXAS 摘要:A process is described for the preparation of the core azobicyclo[7.3.1]tridecaenediyne moiety of the antitumor antibiotic dynemicin. The synthesis allows efficient production of the enediyne as a stable, compound in good yield from the adamantyl N-protected azabicyclo[7.3.1]tridecadiyne. The adamantyl protecting group is employed in the starting material, N-adamantyl dihydroquinoline or N-adamantyl 6-methoxy quinoline. Also disclosed are process for the synthesis of 3-hydroxy-6-methoxyquinoline and several N-substituted derivatives of azobicyclo[7.3.1]tridecaenediyne. Solid tumor and leukemia assays were performed on the analogs of dynemicin. The results suggest a method that these compounds will useful in treating certain types of leukemias and solid tumors. The disclosed synthesis provides a route to new dynemicin intermediates and analogs which will allow development of second and third generation dynemicins.
专利号:EP-0310950-B1 优先权日:1983-11-18 标题 :Quinoline intermediates for the synthesis of 1H-imidazo[4,5-c]quinolines and 1H-imidazo[4,5-c]quinolin-4-amimes 摘要:Compounds of the types (I) and (II) are disclosed, wherein each R5 is independently selected from the group consisting of alkyl of one to about four carbon atoms, alkoxy of one to about four carbon atoms and halogen, and n is an integer from 0 to 2, with the proviso that if n is 2, then said R5 substituents together contain no more than 6 carbon atoms; R6 is selected from the group consisting of hydroxyalkyl of one to about six carbon atoms and cyclohexylmethyl; and R7 is selected from the group consisting of alkyl of one to about four carbon atoms and hydrogen. These compounds may be used as intermediates for the synthesis of 1H-imidazo[4,5-c]quinoline derivatives.
专利号:US-2013225819-A1 优先权日:2010-08-18 标 题:Use of azides in synthesis 发明人:JAMISON TIMOTHY F; PALDE PRAKASH B 权利人:JAMISON TIMOTHY F; PALDE PRAKASH B; MASSACHUSETTS INST TECHNOLOGY 摘要:Described herein are inventive methods for synthesis of tetrazoles. In some embodiments, the method involves the use of a flow reactor. The methods provided herein are capable at being carried out in short reaction times, with high yields, with minimal side reactions, and/or with minimal chance of explosions caused by the presence of azides.
专利号:US-3943142-A 优先权日:1969-01-24 标 题:Dye intermediates and their preparation and use in the synthesis of methine dyes 发明人:OWEN JOHN R 权利人:EASTMAN KODAK CO 摘要:Compositions of matter are provided comprising a stable, non-vaporous monomeric methylene base selected from a 2-methylenethiazoline; a 2-methylenebenzothiazoline; a 2-methylenenaphthothiazoline; a 2-methylenebenzoselenazoline; and a 2-methylenenaphthoselenazoline. The compositions of the invention are prepared by reacting the parent 2-methyl quaternary salt with a non-hydroxylic base which removes a proton of the heterocyclic salt together with a proton acceptor which inhibits build-up of the hydro salt of the non-hydroxylic base, the reaction being conducted under anhydrous conditions in a non-hydroxylic liquid in which the heterocyclic quaternary salt is sufficiently insoluble to inhibit dimer formation. The compositions of the invention are employed in the preparation of methine dyes.
专利号:US-5656634-A 优先权日:1991-03-21 标题 :N-aryl and N-heteroarylamide and urea derivatives as inhibitors of acyl coenzyme A: cholesterol acyl transferase (ACAT) 发明人:CHANG GEORGE; HAMANAKA ERNEST S; MCCARTHY PETER A; TRUONG THIEN V; WALKER FREDERICK J 权利人:PFIZER 摘要:Compounds of the formula ##STR1## the pharmaceutically acceptable salts thereof, wherein Q and R 1 are as defined below, and novel carboxylic acid and acid halide intermediates used in the synthesis of such compounds. The compounds of formula I are inhibitors of acyl coenzyme A: cholesterol acyltransferase (ACAT) and are useful as hypolipidemic and antiatherosclerosis agents.
专利号:WO-2009117985-A1 优先权日:2008-06-12 标题 :Pirinixic acid derivatives as prostglandin e2 synthesis inhibitors for treating inflammatory diseases 发明人:WERZ OLIVER; KOEBERLE ANDREAS; SCHUBERT-ZSILAVECZ MANFRED; POPESCU LAURA; SYHA YVONNE 权利人:MEDEON PHARMACEUTICALS GMBH; UNIV TUEBINGEN; WERZ OLIVER; KOEBERLE ANDREAS; SCHUBERT-ZSILAVECZ MANFRED; POPESCU LAURA; SYHA YVONNE 摘要:The invention relates to pirinixic acid derivatives, especially a-substituted pirinixic acids and pirinixic acid esters, and the structural derivatives thereof with the following structural formula. The pirinixic acid derivatives inhibit the PGE2 synthesis, especially that of the mPGES-1. The invention also relates to the use of said pirinixic acid derivatives for producing a medicament for treating prostaglandin E2-mediated diseases, especially inflammatory diseases, painful and feverish conditions, cardiovascular events and cancerous diseases associated with an increased inducible microsomal prostaglandin E2 synthesis-1 (mPGES-1) activity or increased prostaglandin E2 synthesis.
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合成参考文献
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