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公开(公告)号：US06739059B2
公开(公告)日：2004-05-25
申请号：US10078110
申请日：2002-02-20
申请人： Heinrich Bollinger , Max Keller
发明人： Heinrich Bollinger , Max Keller
IPC分类号： B26B700
CPC分类号： B26B7/00
摘要： A cutting tool with a linear oscillating drive has a handle body (1) and a knife (3, 4) which is guided therein and is displaceable in an oscillating manner in the longitudinal direction, the knife (3, 4), by means of a knife holder (4), being detachably connected via a clamping member to a transmission element, arranged in the handle body (1), of the linear oscillating drive. Since the knife holder (4) is cohesively connected, in particular sealed, together with a knife shaft (31), the cutting tool complies with the hygiene regulations for use in the foodstuffs sector.
摘要翻译： 具有线性摆动驱动器的切割工具具有把手主体（1）和一个被引导到其中的刀具（3,4），并且可沿纵向以摆动方式移动刀具（3,4），通过 刀架（4），其经由夹紧构件可拆卸地连接到设置在手柄主体（1）中的传动元件的线性摆动驱动器。 由于刀架（4）与刀轴（31）一起被内联地连接（特别是密封的），所以切割工具符合用于食品领域的卫生规定。
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公开(公告)号：US06194600B1
公开(公告)日：2001-02-27
申请号：US09475265
申请日：1999-08-26
IPC分类号： C07C25500
CPC分类号： C07C253/30 , C07C255/28
摘要： With the present method, a process which can be employed industrially can be used for the first time for the direct production of aminocyanoacetamide. The method is based on the reaction of cyanoacetamide with nitrites to form nitrosocyanoacetamide at a pH of around 2 and on the subsequent catalytic hydrogenation of nitrosocyanoacetamide to form aminocyanoacetamide.
摘要翻译： 采用本发明的方法，可以在工业上应用的方法首次用于直接生产氨基氰乙酰胺。 该方法是基于氰基乙酰胺与亚硝酸盐反应形成亚硝基氰基乙酰胺，pH值约为2，随后催化氢化亚硝基氰乙酰胺，形成氨基氰乙酰胺。
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公开(公告)号：US6140507A
公开(公告)日：2000-10-31
申请号：US381907
申请日：1999-12-13
IPC分类号： C07D495/04
CPC分类号： C07D495/04
摘要： The present invention relates to a novel process for the selective debenzylation of dibenzylbiotin, which is formed as an intermediate in the synthesis of biotin, but is usually not isolated.
摘要翻译： PCT No.PCT / EP98 / 01545 Sec。 371 1999年12月13日第 102（e）1999年12月13日PCT PCT 1998年3月17日PCT公布。 第WO98 / 43979号公报 日期1998年10月8日本发明涉及二苄基生物素的选择性脱苄基化的新方法，其在生物素的合成中形成中间体，但通常不分离。
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公开(公告)号：US20050014943A1
公开(公告)日：2005-01-20
申请号：US10838986
申请日：2004-05-04
申请人： Alvin Glasky , Heinrich Bollinger , Hans Muller
发明人： Alvin Glasky , Heinrich Bollinger , Hans Muller
IPC分类号： A61P25/28 , C07D233/88 , C07D233/90 , C07D473/30 , C07D473/10
CPC分类号： C07D233/90 , C07D473/30
摘要： An improved method of synthesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of aminocyanacetamide; (2) forming a compound having a reactive amino group on a hydrocarbyl moiety, the hydrocarbyl moiety being linked through an amide group to a physiologically active moiety or an esterified derivative of a physiologically active moiety including therein an esterified benzoyl group; (3) reacting the imidoester with the compound having the reactive amino group on the hydrocarbyl moiety to form a derivative of 5-aminoimidazole-4-carboxamide substituted at the 1-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; (4) forming the six-membered heterocyclic ring of the purine moiety of the hypoxanthine by reacting the derivative of 5-aminoimidazole-4-carboxamide formed in step (3) with triethyl orthoformate to form a 9-substituted hypoxanthine compound substituted at the 9-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; and (5) hydrolyzing the ester of the optionally esterified benzoyl group if present.
摘要翻译： 合成9-取代的次黄嘌呤衍生物的改进方法包括以下步骤：（1）使氨基异氰酸乙酰胺与原甲酸三乙酯反应形成氨基异氰酸乙酰胺的酰亚胺酯衍生物; （2）在烃基部分上形成具有反应性氨基的化合物，烃基部分通过酰胺基与生理活性部分或生理活性部分的酯化衍生物连接，其中包括酯化苯甲酰基; （3）使亚氨酯与在烃基部分上具有反应性氨基的化合物反应，以形成在1-位被取代的5-氨基咪唑-4-甲酰胺的衍生物，其中烃基部分通过酰胺基连接到生理活性部分 其中包括任选酯化的苯甲酰基; （4）通过使步骤（3）中形成的5-氨基咪唑-4-甲酰胺的衍生物与原甲酸三乙酯反应形成在9位被取代的9-取代的次黄嘌呤化合物，形成次黄嘌呤嘌呤部分的六元杂环 - 具有通过酰胺基团连接到生理活性部分的烃基部分，其中包括任选酯化的苯甲酰基; 和（5）水解任意酯化的苯甲酰基的酯（如果存在）。
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公开(公告)号：US06407237B1
公开(公告)日：2002-06-18
申请号：US09505984
申请日：2000-02-16
IPC分类号： C07D47330
CPC分类号： C07D473/30
摘要： The bifunctional compound N-4-carboxyphenyl-3-(6-oxohydropurin-9-yl) propanamide monopotassium salt occurs in a number of crystal forms which differ in their stability. Of these forms, the most stable is designated Type I, which is a monopotassium salt monohydrate in which the water is held as water of crystallization. Other crystalline forms, designated Type II and Type III, convert to Type I. Methods are disclosed for the synthesis of Type I and for the conversion of Type II or Type III to Type I.
摘要翻译： 双官能化合物N-4-羧基苯基-3-（6-氧代氢嘌呤-9-基）丙酰胺单钾盐以稳定性不同的多种晶体形式存在。 在这些形式中，最稳定的是指定为I型的单钾盐一水合物，其中水被保持为结晶水。 其他指定为II型和III型的结晶形式转化为I型。公开了合成I型和II型或III型转化为I型的方法。
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6.发明授权Process for the preparation of serinol and of serinol derivatives, and products obtained therefrom 失效丝氨醇和丝氨醇衍生物的制备方法以及由此得到的产物
公开(公告)号：US4503252A
公开(公告)日：1985-03-05
申请号：US441777
申请日：1982-11-15
申请人： Ernst Felder , Sergio Bianchi , Heinrich Bollinger
发明人： Ernst Felder , Sergio Bianchi , Heinrich Bollinger
IPC分类号： C07C213/00 , C07C67/00 , C07C213/02 , C07C215/10 , C07D295/088 , C07C85/04 , C07C85/24
CPC分类号： C07D295/088
摘要： A method for the synthesis of serinol and serinol derivatives substituted at the nitrogen atoms by reacting a lower 1,3-dialkoxy-isopropyl halide with ammonia or an amine to form a 1,3-dialkoxy-isopropylamine and then removing the ether groups by heating with a hydrogen halide acid. The method allows the production of serinol and serinol derivatives using inexpensive starting materials in a simple manner and obtaining a high purity product which is free of interfering isomers. Novel compounds obtained by the method which are useful as pharmaceutical intermediates, X-ray contrasting agents and cytostatic or psychopharmacological drugs are also disclosed.
摘要翻译： 通过使低级1,3-二烷氧基 - 异丙基卤化物与氨或胺反应形成1,3-二烷氧基 - 异丙胺，然后通过加热除去醚基，合成在氮原子上取代的丝氨醇和丝氨醇衍生物的方法 与卤化氢酸反应。 该方法允许以简单的方式使用廉价的原料生产丝氨醇和丝氨醇衍生物，并获得不含干扰异构体的高纯度产物。 还公开了通过可用作药物中间体，X射线造影剂和细胞抑制剂或精神药物药物的方法获得的新型化合物。
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公开(公告)号：US06849735B1
公开(公告)日：2005-02-01
申请号：US09602048
申请日：2000-06-23
IPC分类号： A61P25/28 , C07D233/88 , C07D233/90 , C07D473/30
CPC分类号： C07D233/90 , C07D473/30
摘要： An improved method of synthesis of a 9-substituted hypoxanthine derivative comprises the steps of: (1) reacting aminocyanacetamide with triethyl orthoformate to form an imidoester derivative of aminocyanacetamide; (2) forming a compound having a reactive amino group on a hydrocarbyl moiety, the hydrocarbyl moiety being linked through an amide group to a physiologically active moiety or an esterified derivative of a physiologically active moiety including therein an esterified benzoyl group; (3) reacting the imidoester with the compound having the reactive amino group on the hydrocarbyl moiety to form a derivative of aminoimidazole-4-carboxamide substituted at the 1-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; (4) forming the six-membered heterocyclic ring of the purine moiety of the hypoxanthine by reacting the derivative of 5-aminoimidazole-4-carboxamide formed in step (3) with triethyl orthoformate to form a 9-substituted hypoxanthine compound substituted at the 9-position with a hydrocarbyl moiety linked through an amide group to a physiologically active moiety including therein an optionally esterified benzoyl group; and (5) hydrolyzing the ester of the optionally esterified benzoyl group if present.
摘要翻译： 合成9-取代的次黄嘌呤衍生物的改进方法包括以下步骤：（1）使氨基异氰酸乙酰胺与原甲酸三乙酯反应，形成氨基异氰酸乙酰胺的酰亚胺酯衍生物; （2）在烃基部分上形成具有反应性氨基的化合物，烃基部分通过酰胺基与生理活性部分或生理活性部分的酯化衍生物连接，其中包括酯化苯甲酰基; （3）使酰亚胺酯与在烃基部分上具有反应性氨基的化合物反应，以形成在1-位取代的氨基咪唑-4-甲酰胺的衍生物，其中烃基部分通过酰胺基团连接到包括其中的生理活性部分 任选酯化的苯甲酰基; （4）通过使步骤（3）中形成的5-氨基咪唑-4-甲酰胺的衍生物与原甲酸三乙酯反应形成在9位被取代的9-取代的次黄嘌呤化合物，形成次黄嘌呤嘌呤部分的六元杂环 - 具有通过酰胺基团连接到生理活性部分的烃基部分，其中包括任选酯化的苯甲酰基; 和（5）水解任意酯化的苯甲酰基的酯（如果存在）。
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公开(公告)号：US06415876B1
公开(公告)日：2002-07-09
申请号：US09529790
申请日：2000-04-20
申请人： Heinrich Bollinger , Max Keller
发明人： Heinrich Bollinger , Max Keller
IPC分类号： B25F500
摘要： A motor housing (11) is mounted in a handle body (10) so as to slide in the longitudinal direction. A tubular pipe (37) that can slide in a bore (38) of the body (10) projects from the back of the housing (11). Compressed air can be applied to the bore (38) through a switching valve (40). A piston (14) with a piston rod (17) can slide in the housing and a tool can be secured to its front end. A flutter valve (23) which alternatingly connects the bore (38) to the two cylinder chambers (27, 28) is built into the valve housing (22). The piston (14) alternatingly opens the connection to an outgoing air conduit (29-31). A pre-stressed spring (47) is set between the body (10) and the housing (11). In operation, the housing (11) oscillates out of step with the piston (14), so that their initial forces are largely compensated and no vibrations are transmitted to the handle body (10).
摘要翻译： 电动机壳体（11）安装在把手主体（10）中，以沿纵向方向滑动。 可以在主体（10）的孔（38）中滑动的管状管（37）从壳体（11）的后部突出。 压缩空气可以通过切换阀（40）施加到孔（38）。 具有活塞杆（17）的活塞（14）可以在壳体中滑动，并且工具可以固定到其前端。 将阀孔（38）交替地连接到两个气缸室（27,28）的摆动阀（23）被内置在阀壳体（22）中。 活塞（14）交替地打开与输出空气管道（29-31）的连接。 预应力弹簧（47）设置在主体（10）和壳体（11）之间。 在操作中，壳体（11）与活塞（14）不同步地摆动，使得它们的初始力被大大地补偿，并且没有振动传递到手柄本体（10）。
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公开(公告)号：US4537714A
公开(公告)日：1985-08-27
申请号：US511672
申请日：1983-07-07
IPC分类号： C07C231/00 , C07C67/00 , C07C231/02 , C07C231/12 , C07K5/075 , C07C103/52
CPC分类号： C07K5/0613 , Y02P20/55
摘要： The invention relates to a selective process for the preparation of N-L-.alpha.-aspartyl-L-phenylalanine-1-lower alkyl ester which comprises:A. reacting an L-aspartic acid 4-arylmethyl ester with a(i) 1,3-diketone; or(ii) acylacetic ester; in the presence of a base to form the salt of(i') L-N-(1-alkyl-2-acyl-vinyl)-aspartic acid 4-arylmethyl ester; or(ii') L-N-(1-alkyl-2-alkoxycarbonyl-vinyl)-aspartic acid 4-arylmethyl ester, and then either:(1) reacting salt (i') or (ii') with an organic or inorganic acid halide having the formula X-A, wherein X represents a halogen and A has the meaning indicated hereinafter, or with an acid anhydride to form ##STR1## wherein R represents an alkyl radical with 1 to 6 carbon atoms;R' represents an alkyl or alkoxy radical with 1 to 6 carbon atoms;Ar represents the phenyl, nitrophenyl, halogenphenyl or alkylphenyl radical; andA represents an acyl with 2 to 12 carbon atoms, alkoxycarbonyl with 2 to 12 carbon atoms, or a phosphoric acid, phosphorous acid, sulfuric acid, sulfurous acid or sulfonic acid radical; and reacting ester (I) with an L-phenylalanine lower alkyl ester; or(2) reacting a salt of (i') or (ii') with a phosphorazo-L-phenyl lower alkyl ester; to form(i") N-L-.alpha.-N'-(1-alkyl-2-acyl-vinyl)-aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester; or(ii") N-L-.alpha.-N'-(1-alkyl-2-alkoxycarbonyl)aspartyl-L-phenylalanine-1-lower alkyl-4-arylmethyl ester;B. reacting (i") or (ii") with a strong acid to split off the respective N-(1-alkyl-2-acyl-vinyl) or N-(1-alkyl-2-alkoxycarbonyl-vinyl) protective group and produce:(iii) N-L-.alpha.-aspartyl-L-phenylalanine-1-lower alkyl-4-(arylmethyl)ester; andC. subjecting ester (iii) to catalytic hydrogenation to selectively split off the 4-(arylmethyl)-ester group and leave the N-L-.alpha.-aspartyl-L-phenylalanine-1-lower alkyl ester product.Novel intermediates for the synthesis are also disclosed.
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