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-6133409-A 优先权日:1996-12-19 标 题:Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and αβ-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARM PROD INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and alpha , beta -unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-5068360-A 优先权日:1990-01-25 标题 :Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno(3,2-C)pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:US-5191090-A 优先权日:1990-01-25 标题:Preparation of 2-(2'-thienyl)ethylamine derivatives and synthesis of thieno[3,2-c]pyridine derivatives therefrom 发明人:DEHOFF BRADLEY S 权利人:SYNTEX INC 摘要:An improved process for the synthesis of 2-(2'-thienyl)ethylamine from suitably functionalized derivatives of 2-(2'-thienyl)ethanol employing ammonia gas in the presence of a metal salt or liquid ammonia and alkyl ketone as a solvent. The 2-(2'-thienyl)ethylamine produced by this process is advantageously converted to ticlopidine.
专利号:EP-0946478-B1 优先权日:1996-12-19 标题 :Process for the solid phase synthesis of aldehydes, ketones and hydroxamic acid compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARMA INC 摘要:This invention is directed to processes for the solid-phase synthesis of aldehydes, ketones, oximes, amines and hydroxamic acid compounds and to polymeric hydroxylamine resin compounds useful therefor.
专利号:US-6710208-B2 优先权日:1996-12-19 标题 :Process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds 发明人:SALVINO JOSEPH M; MORTON GEORGE C; MASON HELEN J; LABAUDINIERE RICHARD F 权利人:AVENTIS PHARMA INC 摘要:This invention is directed to a process for the solid phase synthesis of aldehyde, ketone, oxime, amine, hydroxamic acid and α,β-unsaturated carboxylic acid and aldehyde compounds and to polymeric hydroxylamine resin compounds useful therefor.
[参考文献]: William L Scott, Et Al. Distributed Drug Discovery, Part 2: Global Rehearsal Of Alkylating Agents For The Synthesis Of Resin-Bound Unnatural Amino Acids And Virtual D(3) Catalog Construction. J Comb Chem. 2009 Jan-Feb;11(1):14-33. [参考文献]: William L Scott, Et Al. Distributed Drug Discovery, Part 3: Using D(3) Methodology To Synthesize Analogs Of An Anti-Melanoma Compound. J Comb Chem. 2009 Jan-Feb;11(1):34-43.
合成参考文献
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