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1. 发明申请

WO1996026202A1 PROCESS FOR PRODUCING THIETANONES 审中-公开
标题翻译：用于生产THIETANONEN
公开(公告)号：WO1996026202A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000391
申请日：1996-01-31
申请人： DEGUSSA AKTIENGESELLSCHAFT , KNAUP, Günter , RETZOW, Stefan , WECKBECKER, Christoph
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D331/04
CPC分类号： C07D331/04
摘要： It is known that thietanones of general formula (I), in which R -R have the meanings given in the description, can be produced by the cyclisation, using hydrogen sulphide and a base, of the adducts obtainable by the addition of bromine to the ketones of general formula (III) given in the description. The invention obviates the need for toxic hydrogen sulphide and bromine by cyclising beta -oxosulphenyls of general formula (II), in which R -R have the meanings indicated in the description and X represents Cl, Br or J, in an organic solvent under the influence of a base. The invention also concerns intermediate products for the synthesis of dipeptide sweeteners.
摘要翻译：已知的是，thietanones通式（I）其中R <1> - R的<4>具有说明书中给出的含义，通过加入溴的在说明书中给出的通式的酮获得的加合物的环化（III）以产生硫化氢和碱。根据本发明，所述有毒的硫化氢和溴可以通过β避免-Oxosulfenyle通式（II）其中R <1> - R的<4>是如在说明书中定义如上定义，且X是Cl，Br，J，在一个有机溶剂的基的影响下环化。中间体二肽甜味剂的合成。

2. 发明申请

WO1996026194A1 METHOD OF PRODUCING OXAZOLIDINONES, THE USE THEREOF AND NOVEL OXAZOLIDINONES 审中-公开
标题翻译：用于生产恶唑烷酮的使用和新的恶唑烷酮
公开(公告)号：WO1996026194A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000390
申请日：1996-01-31
申请人： DEGUSSA AKTIENGESELLSCHAFT , DRAUZ, Karlheinz , KNAUP, Günter , RETZOW, Stefan
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D263/18
CPC分类号： C07D263/18 , C07C231/14 , C07C237/22
摘要： The invention concerns a method of producing oxazolidinones of formula (I), wherein R - R have the meanings given in the description, by reacting cyclical anhydrides of formula (II) with carbonyl compounds of general formula (III) at temperatures between ambient temperature and approximately 150 DEG C. The invention also concerns the production of the cyclical anhydrides of formula (II) by reacting N-protected aminodicarboxylic acids of formula (IV) with a dehydrating agent in situ. The invention further concerns the use of oxazolidinones of formula (I) for the alpha -selective production of esters of formula (V) and amides of general formula (VII).
摘要翻译：用于制备式（I）的恶唑烷酮方法，其中R <1> - R的<5>具有说明书中所示的含义; 由式的N-保护的氨基二羧酸反应而制备式（II）的周期性酐（通过在室温下与℃之间约150温度以及式（II）化合物与式（III）的羰基化合物的环状酸酐反应来制备 IV）原位脱水剂。此外，使用式（I）的阿尔法 - 选择性生产或式（V）通式（VII）的酰胺的酯的恶唑烷酮。

3. 发明申请

WO1996026213A1 METHOD OF PRODUCING L-ASPARTYL-D-ALANINE-N-(THIETHANE-3-YL)-AMIDES 审中-公开
标题翻译：法生产L-天冬氨酰-D-丙氨酸-N-（硫杂环丁烷-3-基）酰胺
公开(公告)号：WO1996026213A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000393
申请日：1996-01-31
申请人： DEGUSSA AKTIENGESELLSCHAFT , DRAUZ, Karlheinz , KNAUP, Günter , RETZOW, Stefan , SCHWARM, Michael , WECKBECKER, Christoph
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07K05/06
CPC分类号： C07K5/06113 , Y02P20/55
摘要： The invention concerns a method of producing L-aspartyl-D-alanine-N-(thiethane-3-yl)-amides of general formula (I) by reacting D-alanine-thiethane amides of general formula (II) with oxazolidinone compounds of general formula (III) in an inert organic solvent, wherein R stands for H or a selectively separable protective group, R -R , independently of one another, are identical or different and stand for H or linear or branched C1-C4-alkyl, and R and R , independently of each another, are identical or different and stand for H, linear or branched C1-C4-alkyl, aryl or a group which activates the carbonyl group.
摘要翻译：一种生产L-天冬氨酰-D-丙氨酸-N-（硫杂环丁烷-3-基）通式（I）的酰胺，由D-丙氨酸thietanamiden通式（II）反应，与通式的恶唑烷酮化合物的方法（III），在惰性有机溶剂中，其中，R <1>表示H或选择性地可除去的保护基团R <2> - ，R <5>独立地分支彼此相同或不同的H或C1-C4烷基，直链或且R <6>和R <7>彼此独立地，相同或不同，并且是H，C1-C4烷基，直链或支链的，芳基或羰基活化基团。

4. 发明申请

WO1996026203A1 METHOD OF PRODUCING THIETHANE-3-AMINES BY THE REDUCTIVE AMINATION OF THIETHANE-3-ONES 审中-公开
标题翻译： PROCESS FOR通过的硫杂环丁烷-3-酮的还原胺化PRODUCING硫杂环丁烷胺3
公开(公告)号：WO1996026203A1
公开(公告)日：1996-08-29
申请号：PCT/EP1996000392
申请日：1996-01-31
申请人： DEGUSSA AKTIENGESELLSCHAFT , KNAUP, Günter , RETZOW, Stefan , SCHWARM, Michael , DRAUZ, Karlheinz
发明人： DEGUSSA AKTIENGESELLSCHAFT
IPC分类号： C07D331/04
CPC分类号： C07D331/04
摘要： The invention concerns a method of producing thiethane amines of general formula (I), in which R -R , independently of one another, are identical or different and stand for H, C1-C6-alkyl, C3-C6-cycloalkyl, aryl and arylalkyl, wherein the R -R groups, where possible and acceptable, are linear or branched, halogen-substituted and/or N, O, S hetero atom-substituted, and wherein two of the R -R groups can in each case be attached to form a ring, by condensing thiethane-ones of general formula (II), in which R -R have the meanings given in formula (I), with amine derivatives of general formula (III) NH2-X, in which X stands for OH, O-alkyl, O-aryl, O-acyl or NHR , and R is C1-C4- alkyl, aryl, aralkyl, tosyl, mesyl or acyl, or their salts, such as for example hydrohalides, phosphates, citrates, acetates or sulphates, to form thiethane imines of general formula (IV), in which R -R have the meanings given in formula (I), and X has the meaning given in formula (III) and subsequently reducing the resultant thiethane imine derivatives. The invention is characterized in that condensation is carried out in the autoclave at a temperature of more than 80 DEG C, preferably more than 100 DEG C, in the presence of a salt of an acid whose pK value is between 1 and 4, reduction being carried out with sodium or lithium hydroboron and an activator. The thiethane amines of general formula (I) are used as amide building blocks for sweeteners, imparting extremely good sweetening power thereto.
摘要翻译：一种制备Thietanaminen通式（I）其中R <1> -R <4>独立地相同或不同，为H，C1-C6烷基，C3-C6环烷基，芳基和芳基烷基，其中基团R处理 <1> -R <4>在可能和可允许的直链或支链的，卤素取代的和/或N，O，可以是S-杂原子取代的，并且其中的两个基团R <1> -R <4>被连接以形成一个环能，通过Thietanonen的缩合通式（II）其中R <1> -R <4>如式定义同上，与通式胺衍生物（I）（III）NH 2-X，其中X是OH， O-烷基，O-芳基，O-酰基或NHR <5>和R <5> = C1-C4烷基，芳基，芳烷基，甲苯磺酰基，甲磺酰基或酰基或它们的例如氢卤酸盐，磷酸盐的盐，柠檬酸盐，乙酸盐或硫酸盐，硫杂环丁烷至（IV）其中，R <1> -R <4>如式如上所定义的（I）通式亚胺和X的含义与在式（III），和安格护目镜或减少Thietaniminderivate的获得，其特征在于，在> 80℃的温度，优选> 100℃，在其pK值在1和4之间的酸的盐的存在下，和减少与缩合在高压釜中执行钠或硼氢化锂和活化剂。的硫杂环丁胺通式（I）是甜味剂的Amidbausteine并为他们提供一个极端的甜味。

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