专利号:WO-0027627-A1 优先权日:1998-11-12 标题 :Aryloxime linkers in the solid-phase synthesis of 3-aminobenzisoxazoles 发明人:WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 权利人:LILLY CO ELI; WILEY MICHAEL ROBERT; LEPORE SALVATORE DONATO 摘要:In its first aspect, the invention is directed to a solid support mediated method for the synthesis of diverse polycyclic heterocycles according to general formula (V). A second aspect of the invention is directed to a solid support bound intermediate compound that optionally can be derivatized before a cyclization and displacement procedure provides a product. The intermediate is preferably stable to a wide range of chemical conditions thus allowing, if desired, for the chemical derivatization of the intermediate. A third aspect of the invention is directed to a library of polycyclic heterocycle compounds where said library contains a plurality of diverse library compounds of general formula (V). A fourth aspect of the invention is directed to a method for the synthesis of a library of diverse polycyclic heterocycles by the general method described. A fifth aspect of the invention is directed to an assay kit for the identification of lead compounds of the library described therein.
专利号:US-9073900-B2 优先权日:2013-10-02 标题:Dihydroquinone derivatives of piperidine and piperazine 发明人:ULLAH NISAR 权利人:UNIV KING FAHD PET & MINERALS; KING ABDULAZIZ CITY SCI & TECH 摘要:The dihydroquinone derivatives of piperidine and piperazine are 7-piperazinyl and 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones that exhibit D 2 and 5-HT 1A receptor binding affinities, making them suitable for use as the active ingredient of pharmaceuticals for the treatment of schizophrenia. The derivatives have the general formula: n nwhere X is carbon or nitrogen and R is a group selected from a through f having the formula:n n nor a pharmaceutically acceptable salt thereof. The piperazine compounds are prepared by condensing 4-bromo-2-nitro-benzonitrile with 1-Boc-piperazine (1-tert-butoxycarbonyl-piperazine) to form an intermediate that is converted to a piperazinyl-3,4-dihydroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperadinyl-3,4-dihydroquinazolin-2(1H)-ones. The piperadinyl compounds are prepared from tert-butyl-4-(2-oxo-1,2,3,4-tetradihydroquinazolin-7-yl)piperidine-1-carboxylate, which is converted to 7-(piperidin-4-yl)-3,4-dihyroquinazolin-2(1H)-one. Subsequent reductive amination with the biarylaldehydes a through f completes the synthesis of the 7-piperidinyl-3,4-dihydroquinazolin-2(1H)-ones.
专利号:WO-2023098592-A1 优先权日:2021-11-30 标题:Preparation method for carbon-loaded iron-based catalyst and use thereof in synthesis of intermediates of anti-cancer inhibitors
专利号:US-4476315-A 优先权日:1982-04-30 标 题:Nucleophilic substitution process 发明人:STAHLY G PATRICK; STAHLY BARBARA C 权利人:ETHYL CORP 摘要:Nitroarylacetic acid esters are prepared by reacting a nitroaromatic compound which is devoid of halogen on the aromatic ring carrying a nitro group with an alpha,alpha-disubstituted acetic acid ester in an inert solvent and in the presence of a base so that the ester undergoes a nucleophilic substitution on an unsubstituted ring carbon of the nitroaromatic compound during which an alpha-substituent functions as a leaving group. Nitrobenzene acetic acids and their esters are useful intermediates for the synthesis of pharmaceuticals.
专利号:US-4818753-A 优先权日:1987-09-18 标题 :Synthesis and method of use for 2, 4 diaminoquinazoline 发明人:COLWELL WILLIAM T; DEGRAW JOSEPH I 权利人:STANFORD RES INST INT 摘要:Compounds of the formula ##STR1## wherein R 1 is H, methyl, ethyl, or chloro and R 2 is hydrocarbyl of 1-12 C are useful as antifungal agents. Compounds of this series wherein R 2 is 7-12 C are novel. A new synthetic method for the compounds is also described.
专利号:DE-102011014082-A1 优先权日:2010-04-26 标题 :Synthesis of tetrazole derivatives
摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 381. 摘要:Rudzinski, D. M.; Leadbeater, N. E., Science of Synthesis Knowledge Updates, (2012) 1, 384. 摘要:Asano, Y., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 258. 摘要:Ouali, A.; Taillefer, M., Science of Synthesis: C-1 Building Blocks in Organic Synthesis, (2013) 2, 119. 摘要:Li, D.-D.; Wang, G.-W., Science of Synthesis: Catalytic Transformations via CH Activation, (2015) 2, 344.