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公开(公告)号：US5270460A
公开(公告)日：1993-12-14
申请号：US893407
申请日：1992-06-03
摘要： Sucrose or derivatives thereof such as esters are acylated at the 4'- and/or the 6- position by reaction with a donor acyl ester, e.g. a reactive ester of an alkanoic acid or benzoic acid, in the presence of lipase. Sucrose 6,4' so produced can be chlorinated and deacylated to produce the sweetener sucralose.
摘要翻译： 蔗糖或其衍生物如酯通过与供体酰基酯反应而在4'-和/或6-位上被酰化。 在脂肪酶存在下的链烷酸或苯甲酸的反应性酯。 如此生产的蔗糖6,4'可以被氯化和脱酰基化以产生甜味剂三氯蔗糖。
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12.发明授权Process for the preparation of 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose (TGS) 失效制备4,1'，6'-三氯-4,1'，6'-三脱氧半乳糖（TGS）的方法
公开(公告)号：US4380476A
公开(公告)日：1983-04-19
申请号：US275593
申请日：1981-06-19
申请人： Khizar S. Mufti , Riaz A. Khan
发明人： Khizar S. Mufti , Riaz A. Khan
CPC分类号： C07H5/02
摘要： A process for the preparation of 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose (TGS) comprising the steps of:(a) reacting sucrose with an acylating reagent under conditions to provide a mixture of acylated sucrose derivatives containing a major proportion of 6-monoacylated material;(b) optionally separating 6-monoacylated sucrose derivative from other acylated derivatives before step (c);(c) reacting the monoacylated sucrose derivative with a chlorinating reagent capable of chlorinating at positions 1', 4 and 6' of a sucrose 6- acylate; and(d) deacylating and separating (in either order) the 4,1',6'-trichloro-4,1',6'-trideoxygalactosucrose material formed.
摘要翻译： 制备4,1'，6'-三氯-4,1'，6'-三脱氧半乳糖蔗糖（TGS）的方法，包括以下步骤：（a）在酰化试剂的条件下使蔗糖与酰化试剂反应，得到酰化的 含有主要比例的6-单酰化物质的蔗糖衍生物; （b）在步骤（c）之前任选地将6-单酰化蔗糖衍生物与其它酰化衍生物分离; （c）使单酰化蔗糖衍生物与能够在蔗糖6-酰化物的1'，4'和6'位置进行氯化的氯化试剂反应; 和（d）形成的4,1'，6'-三氯-4,1'，6'-三脱氧半乳蔗糖材料的脱酰和分离（以任何顺序）。
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公开(公告)号：US5440026A
公开(公告)日：1995-08-08
申请号：US886633
申请日：1992-05-21
申请人： Riaz A. Khan , Keith Smith , Andrew Pelter , Jin Zhao
发明人： Riaz A. Khan , Keith Smith , Andrew Pelter , Jin Zhao
CPC分类号： C07H13/04
摘要： A method for the preparation of a sucrose 6-ester comprises:(i) reacting sucrose with a ketene acetal in the presence of an acid catalyst in an inert organic solvent to form a sucrose alkyl 4, 6-orthoester;(ii) subjecting the sucrose alkyl 4, 6-orthoester to mild acidic hydrolysis to provide a mixture of 4- and 6-monoesters of sucrose; and(iii) treating the mixture of sucrose monoesters with a base to convert the sucrose 4-ester into sucrose 6-ester. Sucralose may be prepared by chlorination of sucrose 6-esters prepared according to the invention.
摘要翻译： 蔗糖-6-酯的制备方法包括：（i）在酸催化剂存在下，在惰性有机溶剂中使蔗糖与乙烯酮缩醛反应，形成蔗糖烷基4,6-起始酯; （ii）使蔗糖烷基酯4,6-起始酯进行温和的酸性水解以提供蔗糖的4-和6-单酯的混合物; 和（iii）用碱处理蔗糖单酯的混合物以将蔗糖4-酯转化成蔗糖6-酯。 三氯蔗糖可以通过根据本发明制备的蔗糖6-酯的氯化来制备。
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公开(公告)号：US5128248A
公开(公告)日：1992-07-07
申请号：US412904
申请日：1989-09-26
摘要： Sucrose or derivatives thereof such as esters are acylated at the 4'- and/or the 6-position by reaction with a donor acyl ester, e.g. a reactive ester of an alkanoic acid or benzoic acid, in the presence of lipase. Sucrose 6,4'-diesters so produced can be chlorinated and deacylated to produce the sweetener sucralose.
摘要翻译： 蔗糖或其衍生物如酯通过与供体酰基酯反应而在4'-和/或6-位被酰化。 在脂肪酶存在下的链烷酸或苯甲酸的反应性酯。 如此生产的蔗糖6,4'-二酯可以被氯化和脱酰基化以产生甜味剂三氯蔗糖。
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公开(公告)号：US4826962A
公开(公告)日：1989-05-02
申请号：US921370
申请日：1986-10-20
申请人： Elner B. Rathbone , Khizar S. Mufti , Riaz A. Khan , Peter S. J. Cheetham , Andrew J. Hacking , Jonathan S. Dordick
发明人： Elner B. Rathbone , Khizar S. Mufti , Riaz A. Khan , Peter S. J. Cheetham , Andrew J. Hacking , Jonathan S. Dordick
IPC分类号： A23G3/38 , A23G3/34 , C07H1/00 , C07H3/04 , C07H5/02 , C12P19/00 , C12P19/14 , C12P19/20 , C12R1/645 , C12R1/685
CPC分类号： C07H5/02
摘要： The novel chlorinated sugar O-.alpha.-D-6-chloro-6-deoxygalactopyranosyl-(1.fwdarw.6)-.alpha.-D-4-chloro-4-deoxygalactopyranosyl-(1.fwdarw.2)-.beta.-D-1, 6-dichloro-1, 6-dideoxyfructofuranoside (TCR) can be used to prepare sucralose by incubating the TCR in solution in the presence of an enzyme serving to remove the 6-chloro-6-deoxygalactosyl moiety from the 6-position, especially an enzyme derived from a strain of Mortierella vinacea, Circinella muscae or Aspergillus niger. TCR is prepared by treating raffinose with thionyl chloride in the presence of triphenylphosphine oxide.
摘要翻译： 新型氯化糖O-α-D-6-氯-6-脱氧半乳糖吡喃糖基 - （1-> 6）-α-D-4-氯-4-脱氧半乳糖吡喃糖基 - （1-> 2）-β-D-1， 6-二氯-1,6-二脱氧呋喃果糖苷（TCR）可用于制备三氯蔗糖，通过在用于从6-位除去6-氯-6-脱氧半乳糖基部分的酶存在下，在溶液中温育TCR，特别是 衍生自高山被孢霉菌株，，蛇科或黑曲霉的酶。 通过在三苯基氧化膦存在下用亚硫酰氯处理棉子糖来制备TCR。
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公开(公告)号：US4225590A
公开(公告)日：1980-09-30
申请号：US886531
申请日：1978-03-14
CPC分类号： A61K31/7004 , C07H5/02 , Y10S514/841
摘要： A male fertility-inhibiting composition in unit dosage form, contains as an active ingredient a 6-chlorodeoxy-saccharide containing a pyranose or furanose ring of the formula ##STR1## where A represents the remainder of the pyranose or furanose ring, and has the formula C.sub.4 H.sub.7 O.sub.4 X (where X represents a hydrogen atom or another pyranose or furanose ring) in association with a physiologically acceptable carrier or excipient. The saccharide preferably contains a pyranose ring or furanose ring of the formula ##STR2## Also a method of controlling fertility in men or male animals comprises administering thereto a 6-chlorodeoxy-saccharide as defined above.
摘要翻译： 单位剂型中的雄性生育抑制组合物含有含有式（I）的吡喃糖或呋喃糖环的6-氯脱氧糖的活性成分，其中A代表吡喃糖或呋喃糖环的剩余部分，和 具有与生理学上可接受的载体或赋形剂相关的式C4H7O4X（其中X表示氢原子或另一种吡喃糖或呋喃糖环）。 糖类优选含有下式的吡喃糖环或呋喃糖环。另外，一种在男性或雄性动物中控制生育力的方法包括向其施用如上定义的6-氯脱氧糖。
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