相似化合物
88189-03-1 52093-30-8 139177-62-1欧盟法规
C&L通报专利信息
专利号:US-12221452-B2
优先权日:2017-10-04
标题:Synthesis of cantharidin
发明人:DAVIDSON MATTHEW GENE; EKLOV BRIAN MATTHEW; WUTS PETER; LOERTSCHER BRAD MELVIN; SCHOW STEVEN R
权利人:VERRICA PHARMACEUTICALS INC
摘要:The invention provides synthetic methods for the preparation of cantharidin and analogs thereof. In one aspect, the invention provides an improved Diels-Alder cycloaddition to generate a key intermediate en route to cantharidin and analogs thereof. In certain embodiments, the new Diels-Alder reaction involves reacting Compound (2) in the presence of furan, and in the absence of acid or increased pressure, in an aprotic polar solvent with slight warming, to yield Compound (1) in favorable yield and exo-endo ratio. In another aspect, the invention also provides a new Diels-Alder reaction between compounds of Formula (III) and furan to yield compounds of Formula (IV), which can then be transformed into cantharidin or analogs thereof. In yet another aspect, the invention describes a new palladium-mediated carbonylation providing another key intermediate en route to cantharidin and analogs thereof. In addition to synthetic methods, present invention also provides compounds (i.e., intermediates) useful in the synthesis of cantharidin and analogs thereof. Compounds provided herein may have biological activity, and therefore may be used in the treatment of diseases or conditions (e.g., infectious diseases and skin conditions).
专利号:US-5948693-A
优先权日:1994-09-01
标题:Solid phase synthesis of immunosuppressive agents
发明人:RICH DANIEL H; RAMAN PRAKASH; ANGELL YVONNE M
权利人:WISCONSIN ALUMNI RES FOUND
摘要:The present invention relates generally to cyclosporin analogs, and more paritcularly to methods for the solid-phase synthesis and on-resin cyclization of cyclosporin analogs. Methods are described for the on-resin cyclization of sterically hindered compounds synthesized through solid phase synthesis techniques. The methods utilize solvent, temperature, and washing conditions that allow the efficient on-resin cyclization of compounds like analogs of cyclosporin A.
专利号:WO-2004047990-A1
优先权日:2002-11-27
标题:Catalyst for the preparation of carboxylic esters and process for the preparation of carboxylic esters with the same
发明人:WATANABE YOSHIHIRO; KURODA YASUSHI
权利人:SHOWA DENKO KK; WATANABE YOSHIHIRO; KURODA YASUSHI
摘要:The invention provides a catalyst for the synthesis of carboxylic esters from aldehydes through Tishchenko reaction or the like which can dispense with a special cooling unit, permits the synthesis at temperatures above ordinary temperature, and exhibits high selectivity and a long lifetime. A catalyst for the preparation of carboxylic esters by dimerization of aldehydes, which consists of an aluminum alkoxide and at least one compound selected from among sulfonic acids and salts thereof with Groups 4 to 14 metals of the periodic table; preparation of carboxylic esters by dimerization of aldehydes with the catalyst; and a process for the preparation of carboxylic esters, in which the synthesis is conducted at a reaction temperature controlled within the range of 30 to 100°C.
专利号:US-9045462-B2
优先权日:2012-08-17
标 题 :Synthesis of an antiviral compound
发明人:EVANS JARED WAYNE; FUJIMORI SHINJI; HUYNH GRACE M; LIU QI; TERESK MARTIN GERALD
权利人:GILEAD SCIENCES INC
摘要:The present disclosure provides processes for the preparation of a compound of Formula I: n nwhich is useful as an antiviral agent. The disclosure also provides compounds that are synthetic intermediates to compounds of formula.
专利号:US-6544952-B1
优先权日:1994-03-15
标 题:Synthesis of glycoconjugates of the globo-H epitope and uses thereof
发明人:DANISHEFSKY SAMUEL J; LIVINGSTON PHILIP O; RAGUPATHI GOVINDASWAMI; KIM IN JONG; SCHER HOWARD; SLOVIN SUSAN
权利人:SLOAN KETTERING INST CANCER
摘要:The present invention provides a method of synthesizing a compound having the structure:as well as other related glycoconjugates useful as vaccines for inducing antibodies to epithelial cancer cells in an adjuvant therapy therefore, and in a method for preventing recurrence of epithelial cancer. The present invention also provides a vaccine comprising an amount of the compound described above effective to prevent the recurrence of cancer in a subject.
专利号:US-2017121258-A1
优先权日:2014-04-10
标题 :Synthesis of r-glucosides, sugar alcohols, reduced sugar alcohols, and furan derivatives of reduced sugar alcohols
发明人:SANBORN ALEXANDRA; BINDER THOMAS P
权利人:ARCHER DANIELS MIDLAND CO
摘要:Disclosed herein are methods for synthesizing 1,2,5,6-hexanetetrol (HTO), 1,6 hexanediol (HDO) and other reduced polyols from C5 and C6 sugar alcohols or R glycosides. The methods include contacting the sugar alcohol or R-glycoside with a copper catalyst, most desirably a Raney copper catalyst with hydrogen for a time, temperature and pressure sufficient to form reduced polyols having 2 to 3 fewer hydoxy groups than the starting material. When the starting compound is a C6 sugar alcohol such as sorbitol or R-glycoside of a C6 sugar such as methyl glucoside, the predominant product is HTO. The same catalyst can be used to further reduce the HTO to HDO.