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1.发明授权(Cyanomethylene) phosphoranes as carbonyl 1,1-dipole synthons for use in constructing combinatorial libraries 失效（氰基亚甲基）磷烷作为羰基1,1偶极子合成子，用于构建组合文库
公开(公告)号：US5834588A
公开(公告)日：1998-11-10
申请号：US503070
申请日：1995-07-14
申请人： Harry H. Wasserman , Wen-Bin Ho
发明人： Harry H. Wasserman , Wen-Bin Ho
IPC分类号： C07B61/00 , C07C67/39 , C07C227/26 , C07C229/22 , C07C231/14 , C07C235/78 , C07C269/06 , C07C271/22 , C07D313/00 , C07F9/535 , C07K1/04 , C07K1/08 , C07K1/02
CPC分类号： C07K1/082 , C07C227/26 , C07C231/14 , C07C269/06 , C07C67/39 , C07D313/00 , C07F9/5352 , C07K1/047 , C07C2103/18 , C40B40/00
摘要： The invention is directed to systematic synthetic and testing strategies for .alpha.-keto acids, esters and amides. The method of synthesis comprises (A) reacting (cyanomethylene)triphenylphosphorane with a carbonyl compound selected from carboxylic acids (RCOOH) and acyl chlorides (RCOCl) to make a cyano keto phosphorane, (B) oxidizing said phosphorane and (C) reacting the oxidized product with a nucleophile (NuH) to make the product .alpha.-keto acid, ester or amide. Systematic synthesis and testing are achieved by a modular approach in which arrays of molecules are generated by variation of R and Nu.
摘要翻译： 本发明涉及α-酮酸，酯和酰胺的系统合成和测试策略。 合成方法包括：（A）使（氰基亚甲基）三苯基正膦与选自羧酸（RCOOH）和酰基氯（RCOCl）的羰基化合物反应制得氰基酮基正膦，（B）氧化所述的正极，（C）使氧化的 具有亲核试剂（NuH）的产物使产物为α-酸，酯或酰胺。 通过模块化方法实现系统合成和测试，其中通过R和Nu的变化产生分子阵列。
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2.发明授权公开(公告)号：US06369194B1
公开(公告)日：2002-04-09
申请号：US09188478
申请日：1998-11-09
申请人： Harry H. Wasserman
发明人： Harry H. Wasserman
IPC分类号： C07K102
CPC分类号： C07D295/185 , C07D207/16 , C07D211/16 , C07D317/58
摘要： The invention relates to compounds of formula where R is a structural diversity element selected from the group consisting of alkyl, cycloalkyl, aryl, heteroaryl, peptidyl, heteroatom-substituted alkyl, cycloalkyl, and amines; and Nu is a structural diversity element derived from a nucleophile, NuH, selected from the group consisting of amines, amino acids, peptide, water, hydrogen sulfide, alcohols, and thiols. The invention also relates to arrays and combinatorial libraries of such compounds, and to a method of preparing such compounds.
摘要翻译： 本发明涉及式（I）的化合物，R是选自烷基，环烷基，芳基，杂芳基，肽基，杂原子取代的烷基，环烷基和胺的结构多样性元素; Nu是衍生自选自胺，氨基酸，肽，水，硫化氢，醇和硫醇的亲核试剂NuH的结构多样性元件。 本发明还涉及这些化合物的阵列和组合文库，以及制备这种化合物的方法。
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公开(公告)号：US4929751A
公开(公告)日：1990-05-29
申请号：US109804
申请日：1987-10-19
IPC分类号： C07C69/738 , C07D231/12 , C07D263/32 , C07D401/06 , C07D403/06 , C07D405/06
CPC分类号： C07D401/06 , C07C69/738 , C07D263/32 , C07D403/06 , C07D405/06
摘要： A vinyl tricarbonyl compound of the formula ##STR1## or its monohydrate of the formula ##STR2## wherein R.sub.1 is a hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, and cycloalkyl with 3 to 7 carbon atoms,R.sub.2 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic,R.sub.3 is hydrogen, halogen, unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl with 3 to 7 carbon atoms, cyano, nitro, or a heterocyclic, andR.sub.4 is unsubstituted or substituted C.sub.1 to C.sub.30 alkyl, unsubstituted or substituted aryl, arylalkyl, cycloalkyl are 3 to 7 carbon atoms. Such vinyl tricarbonyl compound is effective against tumor cells.
摘要翻译： 其中R1是氢，卤素，未取代或取代的C1至C30烷基，未取代或取代的芳基，芳基烷基和具有3至7个碳原子的环烷基的式IMAMA的乙烯基三羰基化合物或其一水合物 R 2为氢，卤素，未取代或取代的C 1 -C 30烷基，未取代或取代的芳基，芳基烷基，具有3至7个碳原子的环烷基，氰基，硝基或杂环基，R 3为氢，卤素，未取代或取代的C 1至C 30 烷基，未取代或取代的芳基，芳基烷基，具有3至7个碳原子的环烷基，氰基，硝基或杂环，并且R 4是未取代或取代的C 1至C 30烷基，未取代或取代的芳基，芳烷基，环烷基具有3至7个碳原子 。 这种乙烯基三羰基化合物对肿瘤细胞有效。
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4.发明授权.beta.-Lactams, their production, intermediates thereto and derivatives thereof 失效β-内酰胺，其生产，中间体及其衍生物
公开(公告)号：US4178286A
公开(公告)日：1979-12-11
申请号：US736343
申请日：1976-10-28
IPC分类号： C07D223/10 , C07D201/02 , C07D205/08 , C07D205/095 , C07D207/263 , C07D211/76 , C07D409/06 , C07D405/06
CPC分类号： C07D201/02 , C07D205/08 , C07D205/095
摘要： .gamma.-lactones are converted into both known and new azetidine carboxylic acids which can be transformed readily to the corresponding .beta.-lactams by oxidative decarboxylation. The .beta.-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams such as nocardicin.
摘要翻译： γ-内酯被转化为已知的和新的氮杂环丁烷羧酸，其可以通过氧化脱羧而容易地转化成相应的β-内酰胺。 β-内酰胺及其取代产物是合成生物活性内酰胺如诺卡霉素的有用中间体。
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公开(公告)号：US4190579A
公开(公告)日：1980-02-26
申请号：US865593
申请日：1977-12-29
IPC分类号： C07D205/08 , C07F7/12 , C07D403/06 , C07D407/06 , C07D409/06
CPC分类号： C07F7/12 , C07D205/08
摘要： Azetidine carboxylic acid esters are converted into enol silyl ethers which, as enamino ketene acetals, undergo ready oxidative cleavage of the ethylenically unsaturated double bond, e.g. by dye-sensitized photo-oxygenation, to form beta-lactams. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams.
摘要翻译： 氮杂环丁烷羧酸酯转化成烯醇甲硅烷基醚，其作为烯氨基乙烯酮缩醛进行烯属不饱和双键的即时氧化裂解， 通过染料敏化光氧化，形成β-内酰胺。 β-内酰胺及其取代产物是合成生物活性内酰胺的有用中间体。
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6.发明授权Beta-lactams, their production from azetidine carboxylic acids, intermediates thereto and derivatives thereof 失效β-内酰胺类，其由氮杂环丁烷羧酸制备，其中间体及其衍生物
公开(公告)号：US4163743A
公开(公告)日：1979-08-07
申请号：US831441
申请日：1977-09-08
IPC分类号： C07D205/06 , C07D205/08 , C07D207/267 , C07D403/06 , C07D405/06 , C07D407/06
CPC分类号： C07D205/08 , C07D205/06
摘要： Azetidine-2-carboxylic acids are transformed readily to the corresponding beta-lactams by iminium salt formation and reaction of the salt with a suitable nucleophile. The beta-lactams and substitution products thereof are useful intermediates in the synthesis of biologically active lactams such as nocardicin.
摘要翻译： 氮杂环丁烷-2-羧酸通过亚胺盐形成和盐与合适的亲核试剂的反应容易地转化成相应的β-内酰胺。 β-内酰胺及其取代产物是合成生物活性内酰胺如诺卡霉素的有用中间体。
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