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91. 发明申请

US20170246135A1 BETA-SUBSTITUTED GAMMA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 有权
公开(公告)号：US20170246135A1
公开(公告)日：2017-08-31
申请号：US15594904
申请日：2017-05-15
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： BERND JANDELEIT , WOLF-NICOLAS FISCHER , KERRY J. KOLLER
IPC分类号： A61K31/197 , A61K31/662 , C07C229/08 , C07F9/48 , C07C237/30 , C07C239/18 , C07C309/69 , A61K31/41 , C07C229/42
CPC分类号： A61K31/197 , A61K31/41 , A61K31/662 , A61K47/542 , C07C229/08 , C07C229/42 , C07C237/30 , C07C239/18 , C07C239/20 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

92. 发明授权

US09682921B2 β-substituted γ-amino acids and analogs as chemotherapeutic agents 有权
公开(公告)号：US09682921B2
公开(公告)日：2017-06-20
申请号：US15181020
申请日：2016-06-13
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： Bernd Jandeleit , Wolf-Nicolas Fischer , Kerry J. Koller
IPC分类号： C07C229/08 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/48 , A61K47/48 , A61K31/197 , A61K31/41 , A61K31/662 , C07C229/42 , C07C237/30 , C07C239/20 , C07C239/18 , C07F9/32
CPC分类号： A61K31/197 , A61K31/41 , A61K31/662 , A61K47/542 , C07C229/08 , C07C229/42 , C07C237/30 , C07C239/18 , C07C239/20 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.

93. 发明授权

US09394237B2 β-substituted β-amino acids and analogs as chemotherapeutic agents 有权
标题翻译：氨基酸和类似物作为化学治疗剂
公开(公告)号：US09394237B2
公开(公告)日：2016-07-19
申请号：US14613143
申请日：2015-02-03
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： Bernd Jandeleit , Wolf-Nicolas Fischer , Kerry J. Koller
IPC分类号： C07C229/08 , C07C233/35 , C07C271/46 , C07C309/69 , C07F9/48 , A61K31/197 , A61K31/662 , C07C229/22 , C07C229/34 , C07C237/30 , C07C239/20 , C07C237/04 , C07F9/32
CPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662 , C07C229/08 , C07C229/22 , C07C229/34 , C07C229/42 , C07C233/35 , C07C237/04 , C07C237/20 , C07C237/30 , C07C239/20 , C07C271/46 , C07C309/66 , C07C309/69 , C07F9/306 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
摘要翻译：＆amp; bgr; - 取代的和bgr-氨基酸，和取代的＆bgr - - 氨基酸衍生物和＆amp;取代的＆amp; bgr - 氨基酸类似物和（生物）等体积以及它们作为化学治疗剂的用途。取代和取代的 - 氨基酸衍生物和（取代） - 氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，并且在表达LAT1 / 4F2hc转运蛋白的肿瘤中表现出快速吸收和保留。还公开了合成取代的和取代的 - 氨基酸衍生物和取代的和 - 取代的 - 氨基酸类似物的方法和使用该化合物治疗癌症的方法。取代和取代的 - 氨基酸衍生物和“取代的” - 氨基酸类似物在表达LAT1 / 4F2hc转运蛋白的肿瘤细胞中表现出选择性吸收，并且当在体内施用于受试者时，其累积在癌细胞中。取代的＆bgr - - 氨基酸衍生物和“取代的”和“氨基酸”类似物和（生物）等分子体对几种肿瘤类型表现出细胞毒性。

94. 发明授权

US09394236B2 β-substituted γ-amino acids and analogs as chemotherapeutic agents 有权
标题翻译：取代的γ-氨基酸和类似物作为化学治疗剂
公开(公告)号：US09394236B2
公开(公告)日：2016-07-19
申请号：US14613130
申请日：2015-02-03
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： Bernd Jandeleit , Wolf-Nicolas Fischer , Kerry J. Koller
IPC分类号： C07C229/08 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/48 , A61K47/48 , A61K31/197 , A61K31/41 , A61K31/662 , C07C229/42 , C07C237/30 , C07C239/20 , C07C239/18 , C07F9/32
CPC分类号： A61K31/197 , A61K31/41 , A61K31/662 , A61K47/542 , C07C229/08 , C07C229/42 , C07C237/30 , C07C239/18 , C07C239/20 , C07C271/46 , C07C309/69 , C07D257/04 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted γ-amino acids, β-substituted γ-amino acid derivatives, and β-substituted γ-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates, capable of passing through the blood-brain barrier, and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres and methods of using the compounds for treating tumors are also disclosed. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an improved selectivity toward tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted γ-amino acid derivatives and β-substituted γ-amino acid analogs and (bio)isosteres exhibit an increased efficacy on a variety of tumor types.
摘要翻译：＆bgr; - 取代的γ-氨基酸，＆被取代的γ-氨基酸衍生物和＆gt;取代的γ-氨基酸类似物和（生物）等电点及其作为化学治疗剂的用途。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，能够通过血脑屏障，并且在肿瘤中表现出快速的摄取和保留表达LAT1 / 4F2hc转运蛋白。还公开了合成取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等离子体的方法和使用该化合物治疗肿瘤的方法。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体对于表达LAT1 / 4F2hc转运蛋白的肿瘤细胞表现出改善的选择性，并且当在体内施用于受试者时积累在癌细胞中。取代的γ-氨基酸衍生物和取代的γ-氨基酸类似物和（生物）等分子体对各种肿瘤类型表现出增加的功效。

95. 发明申请

US20160185710A1 BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 审中-公开
公开(公告)号：US20160185710A1
公开(公告)日：2016-06-30
申请号：US15063171
申请日：2016-03-07
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： Bernd JANDELEIT , Wolf-Nicolas FISCHER , Kerry J. KOLLER
IPC分类号： C07C229/42 , C07C271/46 , C07C237/20 , C07F9/30 , C07C309/66
CPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662 , C07C229/08 , C07C229/22 , C07C229/34 , C07C229/42 , C07C233/35 , C07C237/04 , C07C237/20 , C07C237/30 , C07C239/20 , C07C271/46 , C07C309/66 , C07C309/69 , C07F9/306 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.

96. 发明申请

US20150218086A1 BETA-SUBSTITUTED BETA-AMINO ACIDS AND ANALOGS AS CHEMOTHERAPEUTIC AGENTS 有权
标题翻译：作为化学治疗剂的β-取代的氨基酸和类似物
公开(公告)号：US20150218086A1
公开(公告)日：2015-08-06
申请号：US14613143
申请日：2015-02-03
申请人： QUADRIGA BIOSCIENCES, INC.
发明人： BERND JANDELEIT , WOLF-NICOLAS FISCHER , KERRY J. KOLLER
IPC分类号： C07C229/08 , C07C271/46 , C07C233/35 , C07F9/48 , C07C309/69
CPC分类号： A61K31/197 , A61K31/255 , A61K31/27 , A61K31/662 , C07C229/08 , C07C229/22 , C07C229/34 , C07C229/42 , C07C233/35 , C07C237/04 , C07C237/20 , C07C237/30 , C07C239/20 , C07C271/46 , C07C309/66 , C07C309/69 , C07F9/306 , C07F9/3264 , C07F9/48 , C07F9/4816
摘要： β-Substituted β-amino acids, β-substituted β-amino acid derivatives, and β-substituted β-amino acid analogs and (bio)isosteres and their use as chemotherapeutic agents are disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres are selective LAT1/4F2hc substrates and exhibit rapid uptake and retention in tumors expressing the LAT1/4F2hc transporter. Methods of synthesizing the β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and methods of using the compounds for treating cancer are also disclosed. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs exhibit selective uptake in tumor cells expressing the LAT1/4F2hc transporter and accumulate in cancerous cells when administered to a subject in vivo. The β-substituted β-amino acid derivatives and β-substituted β-amino acid analogs and (bio)isosteres exhibit cytotoxicity toward several tumor types.
摘要翻译：＆amp; bgr; - 取代的和bgr-氨基酸，和取代的＆bgr - - 氨基酸衍生物和＆amp;取代的＆amp; bgr - 氨基酸类似物和（生物）等体积以及它们作为化学治疗剂的用途。取代和取代的 - 氨基酸衍生物和（取代） - 氨基酸类似物和（生物）等分子体是选择性LAT1 / 4F2hc底物，并且在表达LAT1 / 4F2hc转运蛋白的肿瘤中表现出快速吸收和保留。还公开了合成取代的和取代的 - 氨基酸衍生物和取代的和 - 取代的 - 氨基酸类似物的方法和使用该化合物治疗癌症的方法。取代和取代的 - 氨基酸衍生物和“取代的” - 氨基酸类似物在表达LAT1 / 4F2hc转运蛋白的肿瘤细胞中表现出选择性吸收，并且当在体内施用于受试者时，其累积在癌细胞中。取代的＆bgr - - 氨基酸衍生物和“取代的”和“氨基酸”类似物和（生物）等分子体对几种肿瘤类型表现出细胞毒性。

97. 发明授权

US08703747B2 Aminophosphinic derivatives that can be used in the treatment of pain 有权
标题翻译：可用于治疗疼痛的氨基亚磷酸衍生物
公开(公告)号：US08703747B2
公开(公告)日：2014-04-22
申请号：US13055096
申请日：2009-07-22
申请人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
发明人： Bernard Roques , Hervé Poras , Marie-Claude Fournie-Zaluski
IPC分类号： A61K31/66 , A01N57/00 , A01N57/18
CPC分类号： C07F9/306 , A61K31/662 , A61K31/67 , A61K31/675 , A61K39/08 , A61K45/06 , C07F9/301 , C07F9/303 , C07F9/3211 , C07F9/3241 , C07F9/4816 , C07F9/59 , C07F9/655345
摘要： The present invention relates to a compound of the following general formula (I): R1—NH—CH(R2)—P(═O)(OR3)—CH2—C(R4)(R5)—CONH—CH(R6)—COOR7 (I) or a pharmaceutically acceptable salt of the latter, an isomer or a mixture of isomers in any proportions, especially a mixture of enantiomers, and in particular a racemic mixture, for which R1 represents a —C(═O)—O—C(R8)(R9)—OC(═O)—R10 group; R2 represents an optionally substituted hydrocarbon-based chain, an aryl or heteroaryl group or a methylene group substituted by a heterocycle; R3 represents a hydrogen atom or a —C(R12)(R13)—OC(═O)—R14 group; R4 and R5 form, together with the carbon that bears them, a saturated hydrocarbon-based ring or an optionally substituted piperidine ring or R4 represents a hydrogen atom and R5 represents a phenyl or a benzyl that is optionally substituted, a heteroaromatic ring or a methylene group substituted by a heterocycle; R6 represents an optionally substituted hydrocarbon-based chain or a phenyl or a benzyl that is optionally substituted; and R7 represents a hydrogen atom or a benzyl, alkyl, heteroaryl, alkylheteroaryl, —CHMe—COOR18, —CHR19—OC(═O)OR20 and —CHR19—OC(═O)OR20 group. The present invention also relates to the use of these compounds as a medicinal product, and in particular for the treatment of pain, more advantageously neuropathic and neuroinflammatory pain, to their method of synthesis and also to the compositions containing them.
摘要翻译：本发明涉及以下通式（I）的化合物：R1-NH-CH（R2）-P（= O）（OR3）-CH2-C（R4）（R5）-CONH-CH（R6） -COOR7（I）或其后者的药学上可接受的盐，任何比例的异构体或异构体混合物，特别是对映异构体的混合物，特别是外消旋混合物，其中R1表示-C（= O） - O-C（R 8）（R 9）-OC（= O）-R 10基; R2表示任选取代的烃基链，芳基或杂芳基或被杂环取代的亚甲基; R3表示氢原子或-C（R12）（R13）-OC（= O）-R14基团; R4和R5与带有它们的碳一起形成饱和烃基环或任选取代的哌啶环，或R4表示氢原子，R 5表示任选取代的苯基或苄基，杂芳环或亚甲基被杂环取代的基团; R6表示任选取代的烃基链或任选取代的苯基或苄基; 并且R 7表示氢原子或苄基，烷基，杂芳基，烷基杂芳基，-CHMe-COOR 18，-CHR 19 -OC（= O）OR 20和-CHR 19 -OC（= O）OR 20基团。本发明还涉及这些化合物作为药用产品的用途，特别是用于治疗其合成方法的疼痛，更有利的是神经性和神经炎性疼痛，以及含有它们的组合物。

98. 发明申请

US20140107078A1 HYPOPHOSPHOROUS ACID DERIVATIVES HAVING ANTIHYPERALGIC ACTIVITY AND BIOLOGICAL APPLICATIONS THEREOF 有权
标题翻译：具有抗真菌活性的亲水性衍生物及其生物应用
公开(公告)号：US20140107078A1
公开(公告)日：2014-04-17
申请号：US14118379
申请日：2012-05-16
申请人： Francine Acher , Jean-Philippe Pin , Cyril Goudet , Alain Eschalier , Jérôme Busserolles , Delphine Rigault , Isabelle Lemasson , Sara Cesarini , Brono Commare
发明人： Francine Acher , Jean-Philippe Pin , Cyril Goudet , Alain Eschalier , Jérôme Busserolles , Delphine Rigault , Isabelle Lemasson , Sara Cesarini , Brono Commare
IPC分类号： C07F9/30 , C07F9/38
CPC分类号： C07F9/3834 , C07F9/301 , C07F9/306 , C07F9/3808 , C07F9/4816
摘要： The invention relates to hypophosphorous acid derivatives of formula (I) wherein —X is H or OH, —R represents one or several radicals R1-R5, identical or different, two of R1-R5 optionally occupying the same position on the phenyl group, one to four of R1-R5 being H and the others being selected in the group comprising -0-(CH2)n—COOH; —S—(CH2)n—COOH; —NH—(CH2)n—COOH; -0-(CH,R′)—COOH; —O—(CH2)n—OH; OR′, —R′ being a C1-C3 alkyl radical; —OH; —COOH; halogen, particularly —F, —CI, —Br, —I, —CF3; —OCF3; —N02; —CH═CH—COOH; —(CH2)n—COOH; O—(CH2)n—P03H2; O—(CF2)n—P03H2; O—(CH2)n—S03H; O—(CH2)n—CONHOH; O—(CH2)n-tetrazol; O—(CH2)n-hydroxyisoxazol—n=1 to 5, preferably 1-3; said hypophosrous acid derivatives being diastereoisomers or enantiomers.
摘要翻译：本发明涉及式（I）的次磷酸衍生物，其中-X是H或OH，-R代表一个或几个R 1 -R 5基，R 1 -R 5相同或不同，任选占苯基上相同位置， R1-R5中的一至四个为H，其它选自包含-O-（CH 2）n -COOH的基团; -S-（CH 2）n -COOH; -NH-（CH 2）n -COOH; -O-（CH，R'） - COOH; -O-（CH 2）n -OH; OR'，-R'为C1-C3烷基; -哦; -COOH; 卤素，特别是-F，-C 1，-Br，-I，-CF 3; -OCF3; -N02; -CH = CH-COOH; - （CH 2）n -COOH; O-（CH 2）n -PO 3 H 2; O-（CF 2）n -PO 3 H 2; O-（CH 2）n -SO 3 H; O-（CH2）n-CONHOH; O-（CH 2）n - 四唑; O-（CH 2）n - 羟基异恶唑-N = 1至5，优选1-3; 所述次磷酸衍生物是非对映异构体或对映异构体。

99. 发明申请

US20110245386A1 Method for the Production of Mixed-Substituted Dialkylphosphinic Acids, Esters, and Salts, and Use Thereof 审中-公开
标题翻译：混合取代的二烷基次膦酸，酯和盐的制备方法及其用途
公开(公告)号：US20110245386A1
公开(公告)日：2011-10-06
申请号：US13140236
申请日：2009-10-06
申请人： Michael Hill , Werner Krause , Martin Sicken
发明人： Michael Hill , Werner Krause , Martin Sicken
IPC分类号： C08K5/5313 , C07F9/30 , C07F9/32 , C08L67/02 , C08L77/06
CPC分类号： C09K21/12 , C07F9/301 , C07F9/306 , C07F9/3211 , C07F9/4816 , C07F9/4866 , C08K5/5313
摘要： The invention relates to a method for producing mixed-substituted dialkyiphosphinic acids, esters, and salts, characterized in that a) a phosphinic acid source (I) is reacted with olefins (IV) in the presence of a catalyst A to obtain an alkylphosphonous acid, the salt or ester (II) thereof, b) the obtained alkylphosphonous acid, the salt or ester (II) thereof is reacted with an olefin (IV) in the presence of a catalyst B to obtain the mixed-substituted dialkylphosphinic acid derivative (III), wherein R1, R2, R3, R4, R11, R12, R13, R14 are identical or different from each other and independently represent, inter alia, H, C1-C18-alkyl, C6-C18-aryl, C6-C18-aralkyl, C6-C18-alkylaryl, X represents H, C1-C18-alkyl, C8-C18-aryl, C6-C18-aralkyl, C8-C18-alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonated nitrogenous base, catalyst A represents transition metals and/or transition metal compounds and/or catalyst systems composed of a transition metal and/or a transition metal compound and at least one ligand, and catalyst B represents compounds forming peroxides, and/or peroxo compounds, and/or azo compounds.
摘要翻译：本发明涉及一种制备混合取代二亚磷酸，酯和盐的方法，其特征在于a）在催化剂A存在下，使次膦酸源（I）与烯烃（Ⅳ）反应得到烷基亚磷酸，其盐或酯（II），b）在催化剂B存在下，将得到的烷基亚膦酸，其盐或酯（II）与烯烃（IV）反应，得到混合取代的二烷基次膦酸衍生物 III），其中R 1，R 2，R 3，R 4，R 11，R 12，R 13，R 14彼此相同或不同，并且独立地表示H，C 1 -C 18烷基，C 6 -C 18 - 芳基，C 6 -C 18 - 烷基，C 6 -C 18烷基芳基，X代表H，C 1 -C 18烷基，C 8 -C 18 - 芳基，C 6 -C 18 - 芳烷基，C 8 -C 18烷基芳基，Mg，Ca，Al，Sb，Sn，Ge，Ti ，Fe，Zr，Zn，Ce，Bi，Sr，Mn，Cu，Ni，Li，Na，K和/或质子化的含氮碱，催化剂A表示过渡金属和/或过渡金属化合物和/ 一个过境 n金属和/或过渡金属化合物和至少一种配体，催化剂B表示形成过氧化物的化合物，和/或过氧化合物和/或偶氮化合物。

100. 发明申请

US20110237721A1 Method for Producing Mono-Carboxy-Functionalized Dialkylphosphinic Acids, Esters and Salts Using a Vinyl Ester of a Carboxylic Acid and the Use Thereof 有权
公开(公告)号：US20110237721A1
公开(公告)日：2011-09-29
申请号：US13132153
申请日：2009-10-06
申请人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
发明人： Michael Hill , Mathias Dietz , Werner Krause , Martin Sicken
IPC分类号： C08K5/5313 , C07F9/30 , C07F9/32
CPC分类号： C09K21/12 , C07F9/301 , C07F9/4816 , C07F9/4866 , C08K5/5313
摘要： The invention relates to a method for producing mono-carboxy-functionalized dialkyiphosphinic acids, esters and salts using a vinyl ester of a carboxylic acid. The method is characterized by the following steps: a) reacting a phosphinic acid source (I) with olefins (IV) in the presence of a catalyst A to give an alkylphosphinic acid, the salt or the ester (II) thereof, b) reacting the alkylphosphinic acid so obtained, the salt or the ester (II) thereof with a vinyl ester of a carboxylic acid of formula (V) in the presence of a catalyst B to give a mono-functionalized dialkylphosphinic acid derivative (VI) and c) reacting the mono-functionalized dialkyiphosphinic acid derivative (VI) so obtained in the presence of a catalyst C to give a mono-functionalized dialkylphosphinic acid derivative (VII) and d) reacting the mono-functionalized dialkyiphosphinic acid derivative (VII); with an oxidant or in the presence of a catalyst D to give a mono-carboxy-functionalized dialkylphosphinic acid derivative (III), wherein R1, R2, R3, R4, R5, R6 are the same or different and independently of each other inter alia represent H, C1-C18 alkyl, C6-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl and X and Y are the same or different and independently of each other represent H, C1-C18 alkyl, C8-C18 aryl, C6-C18 aralkyl, C6-C18 alkylaryl, Mg, Ca, Al, Sb, Sn, Ge, Ti, Fe, Zr, Zn, Ce, Bi, Sr, Mn, Cu, Ni, Li, Na, K and/or a protonated nitrogen base and the catalysts A and D are transition metals and/or transition metal compounds and/or catalyst systems which are composed of a transition metal and/or a transition metal compound and at least one ligand, and the catalyst B is a peroxide-forming compound and/or a peroxo compound and/or an azo compound, and the catalyst C is an acid or a base.

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