专利号:US-5532147-A 优先权日:1991-08-06 标题:Enzymatic method for synthesis of carbohydrates 发明人:NILSSON KURT 摘要:A synthetic method in which is included at least one process, which is characterized by that a glycosidase (EC 3.2) is used to catalyse a reaction between a partially protected galactose derivative, or a partially protected glucose derivative, and a glycosyl doner, which is an oligosaccharide or a monosaccharide glycoside, is described. The process is suitable for synthesis of carbohydrate derivatives or for synthesis of partially protected carbohydrate intermediates which are suitable for further synthesis e.g. of blood group determinants A and B, or other carbohydrates.
专利号:WO-9407900-A1 优先权日:1992-09-25 标 题 :Synthesis of n-glycosylated compounds with the use of a mild, iodine-catalyzed reaction 发明人:KOREEDA MASATO; HOUSTON TODD A 权利人:UNIV MICHIGAN 摘要:The invention concerns N-glycosylated derivatives of nitrogen nucleophile compounds. The invention also concerns a mild, cost effective, stereoselective, regioselective, and generally applicable method for the preparation of N-glycosides by N-glycosylation of azide and amide nucleophile compounds. The method employs iodine in a catalytic amount that uniquely does not pose an environmental hazard. The invention provides efficient access to key intermediates for the synthesis inter alia of analogs of AZT and DDI and for the synthesis of conventional N-nucleoside antibiotic drugs and their novel N-glycosylated analogs.
专利号:US-4384998-A 优先权日:1981-03-30 标题:Synthesis of thienamycin from D-glucose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-4448976-A 优先权日:1981-03-30 标题 :Chiral synthesis of thienamycin from D-gluocose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
专利号:US-7102023-B2 优先权日:1999-11-24 标 题:Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 发明人:BUCHWALD STEPHEN L; PLANTE OBADIAH J; SEEBERGER PETER H 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.
专利号:US-4544502-A 优先权日:1981-03-30 标 题 :Chiral synthesis of thienamycin from D-glucose 发明人:DURETTE PHILIPPE L 权利人:MERCK & CO INC 摘要:Disclosed is a chiral, total synthesis of thienamycin from D-glucose which proceeds via intermediates I, II and III to known aldehyde IV which is known to be useful in the total synthesis of thienamycin (V): ##STR1## wherein: R is lower alkyl having 1-6 carbon atoms or bi-valent alkyl having 2-6 carbon atoms which joins the two sulfur atoms; R 1 is lower alkyl or aralkyl, such as benzyl and the like; and R 2 is hydrogen or a removable protecting group, such as triorganosilyl wherein the organo groups are independently selected from lower alkyl, phenyl and phenylloweralkyl.
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