专利号:US-6251689-B1 优先权日:1998-05-14 标 题:Methods for the solid phase synthesis of combinatorial libraries of benzimidazoles benzoxazoles benzothiazoles and derivatives thereof 发明人:LABORDE EDGARDO; MATSUMOTO YUKIHARU 权利人:TELIK INC 摘要:The present invention provides an efficient and versatile method for the synthesis and screening of combinatorial libraries of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof. In order to expedite the synthesis of large arrays of compounds possessing these core structures, a general methodology for solid phase synthesis of these derivatives is provided. Arrays of benzimidazoles, benzoxazoles, benzothiazoles, and derivatives thereof useful as peptidomimetics and for the identification of agents having antifungal, antiviral, antimicrobial, anticoagulant, and antiulcer activity, or use in the treatment of inflammation, hypertension, cancer, and other conditions can be prepared by this method.
专利号:US-5175302-A 优先权日:1987-07-13 标 题 :Nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4837327-A 优先权日:1987-07-13 标 题 :Process for nucleophilic fluoroalkylation of aldehydes 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:US-4999429-A 优先权日:1989-01-09 标 题 :Process for the preparation of α,α,β-1-trifluoro-1-olefinic derivatives 发明人:STAHLY G PATRICK 权利人:ETHYL CORP 摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.
专利号:WO-2004050654-A1 优先权日:2002-11-29 标 题 :Synthesis of pyrrolidine compound and salt thereof 发明人:KAWANISHI YASUYUKI; UENAKA MASAAKI; IDE YUTAKA; SHINOMOTO SHOJI; OKUNO TAKAYUKI 权利人:SHIONOGI & CO; KAWANISHI YASUYUKI; UENAKA MASAAKI; IDE YUTAKA; SHINOMOTO SHOJI; OKUNO TAKAYUKI 摘要:A p-toluenesulfonate, sulfate, or hydrochloride of the compound represented by the formula (I): (I) a solvate of any of these, or crystals of any of these; and processes for producing these.
专利号:US-5877296-A 优先权日:1994-06-03 标题:Process for preparing conjugates of methyltrithio antitumor agents 发明人:HAMANN PHILIP ROSS; HINMAN LOIS; HOLLANDER IRWIN 权利人:AMERICAN CYANAMID CO 摘要:This invention describes carrier-drug conjugates prepared from disulfide analogs of the calicheamicin family of potent antitumor antibiotics and their derivatives, as well as similar analogs from related antitumor antibiotics such as the esperamicins. The carrier can be an antibody, growth factor, or steroid which targets an undesired population of cells, such as those of a tumor. Whole protein carriers as well as their antigen-recognizing fragments and their chemically or genetically manipulated counterparts are useful for the targeting portion of the conjugates. This invention includes compounds required for the synthesis of these conjugates, appropriate pharmaceutical compositions of the carrier-drug conjugates, and their method of use.