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公开(公告)号：US5470969A
公开(公告)日：1995-11-28
申请号：US237947
申请日：1994-05-02
摘要： Sucrose is mono-acylated in the 6-position by reacting sucrose with a carboxylic acid anhydride such as acetic or benzoic anhydride in a reaction mixture containing a polar aprotic solvent and a catalytic quantity of a 1,3-diacyloxy-1,1,3,3-tetra(hydrocarbyl)distannoxane, for a period of time and at a temperature sufficient to produce a sucrose-6-ester.
摘要翻译： 蔗糖通过蔗糖与羧酸酐如乙酸或苯甲酸酐在含有极性非质子溶剂和催化量的1,3-二酰氧基-1,1,3,3-四氢呋喃的反应混合物中在6-位上单酰化 ，3-四（烃基）二锡氧烷，持续一段时间并在足以产生蔗糖-6-酯的温度下进行。
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公开(公告)号：US4977254A
公开(公告)日：1990-12-11
申请号：US388657
申请日：1989-08-02
摘要： Sugars and partly protected sugar derivatives are chlorinated by reaction of unprotected hydroxyl groups with thionyl chloride to form a persulphite followed by decomposition of the sulphite groups to form chlorosulphites, displacement of the chlorosulphite groups and insertion of chlorine atoms at one or more positions, characterised in that formation and displacement of the chlorosulphite groups and insertion of chlorine atoms is effected by reaction with thionyl chloride in an inert solvent in the presence of a quaternary salt of the general formula:N.sup.+ R.sup.1 R.sup.2 R.sup.3 R.sup.4 Cl.sup.- (I)wherein R.sup.1, R.sup.2 and R.sup.3, which may be the same or different, each represent a lower alkyl group, and R.sup.4 represents a hydrocarbon group with at least seven carbon atoms; and, when the sugar or partly protected sugar derivative has more than three unprotected hydroxyl groups, the process comprises the following stages:(a) reaction of the sugar or partly protected sugar derivative with thionyl chloride in the presence of pyridine to form a persulphite;(b) isolation of the polysulphite to remove free pyridine; and(c) reaction of the isolated polysulphite with thionyl chloride in an inert solvent or suspension medium in the presence of a quaternary salt of the general formula (I).
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3.发明授权.alpha.-(Hydroxy and alkoxy substituted)phenyl-.alpha.-(2-piperidinyl)-methanols 失效{60-（羟基和烷氧基取代的）苯基 - {60-（2-哌啶基） - 甲醇
公开(公告)号：US3941796A
公开(公告)日：1976-03-02
申请号：US487661
申请日：1974-07-11
IPC分类号： C07D211/22 , C07D213/30 , C07D213/50
CPC分类号： C07D213/30 , C07D211/22 , C07D213/50 , Y10S514/826
摘要： .alpha.-(Hydroxy and alkoxy substituted)phenyl-.alpha.-(2-piperidinyl)methanols of the formula ##SPC1##Where R is hydrogen or lower alkyl, R.sup.1 is hydrogen, hydroxy or lower alkoxy, and R.sup.2 is phenyl, phenyl-lower alkyl, diphenyl-lower alkyl, phenoxy-lower alkyl or diphenoxy-lower alkyl, and the non-toxic pharmaceutically acceptable acid-addition and quaternary ammonium salts thereof.
摘要翻译： 式WHERE R是氢或低级烷基，R 1是氢，羟基或低级烷氧基的α-（羟基和烷氧基取代的）苯基-α-（2-哌啶基）甲醇，R 2是苯基，苯基 - 低级烷基， 低级烷基，苯氧基 - 低级烷基或二苯氧基 - 低级烷基，及其无毒的药学上可接受的酸加成盐和季铵盐。
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公开(公告)号：US4920207A
公开(公告)日：1990-04-24
申请号：US98023
申请日：1987-09-17
申请人： George H. Sankey , Nigel J. Homer
发明人： George H. Sankey , Nigel J. Homer
CPC分类号： C07H13/04
摘要： 2,3,4,3',4'-penta-O-acetyl sucrose (4-PAS), a key intermediate in the preparation of sucralose, is prepared by the selective removal of trityl groups from 6,1', 6'-tri-O-trityl-penta-O-acetyl sucrose (TRISPA) in which a catalytic amount of an aralkyl chloride or hydrogen chloride is added to a solution of TRISPA is an inert organic solvent is hydrogenated in the presence of a hydrogenolysis catalyst such a platinum or palladium.
摘要翻译： 2,3,4,3'，4'-五-O-乙酰基蔗糖（4-PAS）是制备三氯蔗糖的关键中间体，通过选择性地从6,1'，6' - 三 - 三 - 三乙基 - 乙酰基蔗糖（TRISPA），其中将催化量的芳烷基氯或氯化氢加入到TRISPA的溶液中是惰性有机溶剂，在氢解催化剂 铂或钯。
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公开(公告)号：US5136031A
公开(公告)日：1992-08-04
申请号：US474314
申请日：1990-07-09
摘要： A process for the chlorination of sucrose or a derivative thereof, comprises reaction of the sucrose or derivative thereof with thionyl chloride and a nitrogen base at a ratio of about 1 molar equivalent (ME) of thionyl chloride and about 1 ME of base for every ME of free hydroxyl, in a non-reactive moderately polar solvent. The process is particularly suitable for the preparation of sucralose.
摘要翻译： 蔗糖或其衍生物的氯化方法包括将蔗糖或其衍生物与亚硫酰氯和氮碱按每摩尔约1摩尔当量（ME）亚硫酰氯和约1ME碱的比例反应 的游离羟基，在非反应性中等极性溶剂中。 该方法特别适用于制备三氯蔗糖。
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公开(公告)号：US5449772A
公开(公告)日：1995-09-12
申请号：US64852
申请日：1993-05-20
申请人： George H. Sankey
发明人： George H. Sankey
摘要： A method is provided for the preparation of a sucrose 6-ester by: (i) reacting a solution of sucrose in an inert organic solvent with a reagent selected from the group consisting of a trialkyl orthoester and a ketene acetal, in the presence of an acid catalyst to provide a sucrose alkyl 4,6-orthoester, (ii) treating the sucrose alkyl 4,6-orthoester under mild aqueous acidic conditions to provide a mixture of sucrose 4- and 6-monoesters, (iii) treating the mixture of esters with a base to convert the sucrose 4-ester into sucrose 6-ester, and (iv) neutralizing the solution and isolating the sucrose 6-ester, in which stage (i) is effected in a continuous manner by passing the solution of sucrose and reagent through a strong acid macroreticular ion exchange resin at ambient temperature. Sucralose is prepared by chlorinating the sucrose 6-esters obtained.
摘要翻译： 提供了通过以下步骤制备蔗糖6酯的方法：（i）在惰性有机溶剂中的蔗糖溶液与选自三烷基原酸酯和乙烯酮缩醛的试剂在 酸催化剂以提供蔗糖烷基4,6-原酸酯，（ii）在温和的酸性水溶液条件下处理蔗糖烷基4,6-原酸酯以提供蔗糖4-和6-单酯的混合物，（iii） 酯与酯，将蔗糖4-酯转化成蔗糖6-酯，和（iv）中和溶液并分离蔗糖6酯，其中阶段（i）以连续方式通过蔗糖溶液 和试剂通过强酸大网络离子交换树脂在环境温度下。 通过氯化得到的蔗糖6酯制备三氯蔗糖。
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