4,5-Dimethyl-2,5-Dihydro-Thiazole置于sulfur体系中,化学反应生成 4,5-二甲基噻唑 参考文献:Asinger,F. Et Al.,Justus Liebigs Annalen Der Chemie,1961,Vol. 648,P. 83-95 标题:Asinger,F. Et Al.,Justus Liebigs Annalen Der Chemie,1961,Vol. 648,P. 83-95
专利信息
专利号:US-9475814-B2 优先权日:2011-10-03 标题:Chiral N-acyl-5,6,7(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines as selective NK-3 receptor antagonists, pharmaceutical composition, methods for use in NK-3 receptor mediated disorders and chiral synthesis thereof 发明人:HOVEYDA HAMID R; DUTHEUIL GUILLAUME; FRASER GRAEME L; ROY MARIE-ODILE; EL BOUSMAQUI MOHAMED; BATT FREDERIC 权利人:EUROSCREEN SA 摘要:The present invention relates to novel compounds of Formula I and their use in therapeutic treatments. The invention further relates to a novel chiral synthesis of 5,6,7,(8-substituted)-tetrahydro-[1,2,4]triazolo[4,3-a]pyrazines using N-sp3 protective groups. The invention also provides intermediates for use in the synthesis of compounds of Formula I.
专利号:US-RE29669-E 优先权日:1973-04-23 标 题:Production of 4-hydroxy-1,2-benzothiazine-3-carboxamides 摘要:A process for the synthesis of N-aryl-3,4-dihydro-2-alkyl-4-oxo-2H-1,2-benzothiazine-3-carboxamide 1,1-dioxides by treatment of N-aryl-N'-alkyl-N'-(2'-alkoxycarbonylbenzenesulfonyl)glycineamides, useful intermediates for said process, with an alkali or alkaline earth metal hydride in a reaction-inert solvent at 50°-150° C., said products being antiinflammatory agents.
专利号:US-5215997-A 优先权日:1985-09-11 标题:Synthesis of beta-lactam compounds 发明人:HUNGERBUEHLER ERNST; KALVODA JAROSLAV 权利人:CIBA GEIGY CORP 摘要:The invention relates to an improved process for the preparation of compounds of formula ##STR1## or salts thereof, starting from compounds of formulae ##STR2## via compounds of formulae ##STR3## in which compounds R 1 is hydrogen or lower alkyl, R 2 is an organic radical which may carry a functional group which may be protected by a customary protective group R 2 o , R 3 is hydrogen or a customary carboxyl protective group R 3 o , W is a group which can be replaced by a thiocarboxylic acid radical of formula III, and Z is oxygen or sulfur.
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-3558614-A 优先权日:1967-09-05 标题:Synthesis of tetranuclear dyes 发明人:JENKINS PHILIP W 权利人:EASTMAN KODAK CO 摘要:TETRANUCLEAR DYES DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE AND A 2-IMIDAZOLIN-4-SELENONE ARE PREPARED IN GOOD YIELDS BY CONDENSING A QUATERNIZED MEROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4-THIONE OR A 2-IMIDAZOLIN4-SELENONE WITH (1) A DIALKOXYALKYL ESTER OF AN ORGANIC ACID, (2) A TRIALKOXY ALKANE OR ARYL COMPOUND, (3) A 3,3-DIALKOZY-1ALKOXYPROPENE, (4) A 1-ANILINO-5-PHENYLIMINO-1,3-PENTADIENE OR (5) A SECOND QUATERNIZED MROCYANINE DYE DERIVED FROM A 2-IMIDAZOLIN-4-ONE, A 2-IMIDAZOLIN-4THIONE OR A 2-IMIDAZOLIN-4-SELENONE, EACH HAVING SUBSTITUTED ON THE CARBON IN THE 2-POSITION A GROUP SUCH AS A B-ACETANILIDOVINYL GROUP, A 4-ACETANILIDO-1,3-BUTADIENYL GROUP, AND A 6-ACETANILIDO-1,3,5-HEXADIENYL GROUP.
专利号:US-6506902-B2 优先权日:2000-03-29 标题:Synthesis of thiazolium compounds 发明人:WAGLE DILIP 权利人:ALTEON INC 摘要:Provided is a method of synthesizing a compound of formula I, n comprising: n (a) reacting a compound of formula II n wherein R 1 and R 2 are independently hydrogen, hydroxy(C 1 -C 2 )alkyl, or (C 1 -C 2 )alkyl with, n a compound of formula III n wherein n R 3 , R 4 , and R 5 are each independently of each other hydrogen, (C 1 -C 3 )alkyl, (C 1 -C 3 )alkoxy, or halogen; and n X is a leaving group, n in a solvent having a dielectric constant at 20° C. of at least 30 but no more than 40; and n (b) obtaining the compound I.
参考标题:Synthesis Of 4-Substituted Chlorophthalazines, Dihydrobenzoazepinediones, 2-Pyrazolylbenzoic Acid, And 2-Pyrazolylbenzohydrazide Via 3-Substituted 3-Hydroxyisoindolin-1-Ones 作者:Hanh Nho Nguyen,Victor J. Cee,Holly L. Deak,Bingfan Du,Kathleen Panter Faber,Hakan Gunaydin,Brian L. Hodous,Steven L. Hollis,Paul H. Krolikowski,Philip R. Olivieri,Vinod F. Patel,Karina Romero,Laurie B. Schenkel,Stephanie D. Geuns-Meyer |发布日期:2012.4.20 摘要:Hydrazine, Followed By Chlorination With Pocl3. We Have Also Discovered Two Novel Transformations Of 3-Vinyl- And 3-Alkynyl-3-Hydroxyisoindolinones. Addition Of Vinyl Organometallic Reagents To N,N-Dimethylaminophthalimide (8A) Provided Dihydrobenzoazepinediones 15A-15C Via The Proposed Ring Expansion Of 3-Vinyl-3-Hydroxyisoindolinone Intermediates. 3-Alkynyl-3-Hydroxyisoindolinones React With Hydrazine And
合成参考文献
摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 337. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 350. 摘要:Koutentis, P. A.; Ioannidou, H. A., Science of Synthesis Knowledge Updates, (2010) 1, 341. 摘要:Yan, G.; Zhang, Y.; Wang, Jianbo, Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 2, 542. 摘要:Yeung, C. S.; Borduas, N.; Dong, V. M., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 796.