专利号:US-11220513-B2 优先权日:2015-04-30 标题:Chromium-mediated coupling and application to the synthesis of halichondrins 发明人:KISHI YOSHITO; YAN WUMING; LI JINGWEI; LI ZHANJIE; YAHATA KENZO 权利人:HARVARD COLLEGE 摘要:The present invention provides unified synthesis of the C1-C19 building blocks of halichondrins and analogs thereof using selective coupling of poly-halogenated nucleophiles in chromium-mediated coupling reactions. The present invention also provides a practical and efficient synthesis of C20-C38 building blocks of halichondrins and analogs thereof. Also provided herein are general methods of selective activation and coupling of poly-halogenated analogs with an aldehyde. The provided coupling reactions are selective for halo-enone and halo-acetylenic ketal over vinyl halide and halide attached to a sp hybridized carbon. The provided efficient selective coupling reactions can allow easy access to the C1-C19 building blocks and C20-C38 building blocks of halichondrins and analogs thereof with limited or no purification or separation of the intermediates.
专利号:US-2003083352-A1 优先权日:2000-07-31 标 题 :Synthesis of imidazole intermediates 发明人:HELAL CHRISTOPHER J 权利人:PFIZER 摘要:The invention provides a method for synthesis of compounds of formula n n n wherein R 1 and R 19 are as defined. Compounds of formula 12 are useful as intermediates for synthesizing compounds having pharmacological activity inhibiting cdk5, cdk2, and GSK-3.
专利号:US-6087512-A 优先权日:1996-09-18 标题:Process for preparation of glycidyl ether 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; YANAGIMOTO TETSUYA; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of a glycidyl ether which is characrelized in reacting an epoxy compound of the formula ##STR1## wherein X is halogen or sulfonyloxy in the presence of a fluoride salt, with an alcohol. According to the above method, glycigyl ethers or their optically active compounds important as intermediates for synthesis of medicines are easily obtained in good yield and especially the optically active compounds are obtained with highly optical purity.
专利号:US-6057476-A 优先权日:1996-09-18 标题:Process for the preparation of 3-amino-2-hydroxy-1-propyl ethers 发明人:FURUKAWA YOSHIRO; KITAORI KAZUHIRO; MIKAMI MASAFUMI; YOSHIMOTO HIROSHI; OTERA JUNZO 权利人:DAISO CO LTD 摘要:A process for preparation of 3-amino-2-hydroxy-1-propyl ether of the formula ##STR1## wherein R 1 is substituted or unsubstituted alkyl, substituted or unsubstituted aryl, or substituted or unsubstituted heterocyclic ring, R 2 and R 3 are the same or different hydrogen atom, a substituted or unsubstituted alkyl, or may form a ring together with an adjacent nitrogen atom, which ring may be interrupted with nitrogen atom, oxygen atom or sulfur atom, n which is characterized in reacting an epoxy compound of the formula ##STR2## wherein X is halogen, in the presence of a fluoride salt, with an alcohol and then reacting an amine. n According to the above method, an intermediates for synthesis of medicines is obtained in good yield and highly optical purity.
专利号:US-5599520-A 优先权日:1994-11-03 标题:Synthesis of crystalline porous solids in ammonia 发明人:GARCES JUAN M; MILLAR DEAN M; HOWARD KEVIN E 摘要:A process of preparing a crystalline porous solid selected from silicas and metallosilicates, such as, aluminosilicate zeolites or clathrasils. The process involves preparing a reaction mixture containing ammonia; water in a controlled concentration; a (hydrocarbyl)ammonium polysilicate hydrate salt; a mineralizer, such as ammonium fluoride; optionally, a source of a metal oxide, such as aluminum nitride; and optionally, a source of a charge-balancing cation or a structure directing agent; and maintaining the mixture at a temperature and for a time so as to produce the crystalline porous solid. A novel silica which is isostructural with zeolite P1 is prepared. Also prepared are a novel silica which is isostructural with zeolite beta and a novel TMA sodalite having a silica/alumina molar ratio between 12 and about 20.
专利号:US-5648484-A 优先权日:1995-03-07 标 题 :Catalytic enantioselective synthesis of a spriofused azetidinone 发明人:WU GUANG-ZHONG 权利人:SCHERING CORP 摘要:A process for producing a compound of the formula ##STR1## comprises the following sequence of steps: ##STR2## wherein the various radicals are as defined in the specification.