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    • 52. 发明申请
    • Process for preparation of alpha-ketoglutaric acid
    • α-酮戊二酸的制备方法
    • US20120095261A1
    • 2012-04-19
    • US12925133
    • 2010-10-13
    • Guoji Zhang
    • Guoji Zhang
    • C07C277/00C07C59/185
    • C07C277/08C07C51/02C07C51/41C07C51/412C07C51/43C07C51/47C07C67/347C07C279/02C07C69/63C07C59/347
    • A process for preparation of α-ketoglutaric acid, which is adapted for preparing L-arginine α-ketoglutarate 1:1 and 2:1, comprising the steps of: (a) reacting methyl dichloroacetate and acrylic acid methyl ester with sodium methoxide to obtain dimethyl 2,2-dichloroglutarate; (b) reacting the dimethyl 2,2-dichloroglutarate from step (a) with hydroxide solution to obtain crude α-ketoglutaratic acid aqueous solution; (c) purifying the crude α-ketoglutaratic acid aqueous solution to obtain purified α-ketoglutaratic acid aqueous solution; and (d) adjusting a concentration of the purified α-ketoglutaratic acid aqueous solution by adding water, thereby a yield of the purified α-ketoglutaratic acid aqueous solution is approximately 75%. While avoiding the use of massive organic solvents, the process of the present invention has a remarkable high yield to realize mass production with low manufacturing cost and shortened production time.
    • 一种制备α-酮戊二酸的方法,其适用于制备1 - 1和2:1的L-精氨酸α-酮戊二酸,包括以下步骤:(a)使二氯乙酸甲酯和丙烯酸甲酯与甲醇钠反应,得到 2,2-二氯戊二酸二甲酯; (b)使来自步骤(a)的2,2-二氯戊二酸二甲酯与氢氧化物溶液反应,得到粗α-酮戊二酸水溶液; (c)纯化粗α-酮戊二酸水溶液,得到纯化的α-酮戊二酸水溶液; 和(d)通过加水调节纯化的α-酮戊二酸水溶液的浓度,由此纯化的α-酮戊二酸水溶液的收率为约75%。 在避免使用大量有机溶剂的同时,本发明的方法具有显着的高产率,可以实现批量生产,制造成本低,生产时间缩短。
    • 54. 发明授权
    • Method for producing fluorine-containing carboxylic acid ester
    • 含氟羧酸酯的制造方法
    • US08039665B2
    • 2011-10-18
    • US12665269
    • 2008-06-18
    • Takeshi Kondo
    • Takeshi Kondo
    • C07C69/63
    • C07C67/00C07C69/63
    • A method for producing a fluorine-containing carboxylic acid ester represented by the general formula R1HCFCOOR2 involves reacting a fluorine-containing ether represented by the general formula R1HCFCF2OR2 with water in the presence of a solid catalyst. The solid catalyst is at least one selected from the group consisting of alumina, titania, zirconia, sulfated zirconia, an activated carbon on which sulfuric acid is supported, a resin having acid sites, and aluminum phosphate. In the general formulas R1HCFCOOR2 and R1HCFCF2OR2, R1 represents a fluorine atom or a C1-4 perfluoroalkyl group, and R2 represents a monovalent organic group.
    • 由通式R1HCFCOOR2表示的含氟羧酸酯的制造方法包括在固体催化剂存在下使由通式R 1 HCFCF 2 OR 2表示的含氟醚与水反应。 固体催化剂是选自氧化铝,二氧化钛,氧化锆,硫酸化氧化锆,负载硫酸的活性炭,具有酸性位置的树脂和磷酸铝的至少一种。 在通式R1HCFCOOR2和R1HCFCF2OR2中,R1表示氟原子或C1-4全氟烷基,R2表示一价有机基团。
    • 55. 发明申请
    • Latent acids and their use
    • 潜在酸及其用途
    • US20110217654A1
    • 2011-09-08
    • US13028323
    • 2011-02-16
    • Hitoshi YamatoToshikage AsakuraAkira MatsumotoKeita TanakaYuichi Nishimae
    • Hitoshi YamatoToshikage AsakuraAkira MatsumotoKeita TanakaYuichi Nishimae
    • G03F7/004C07C69/753C07D311/74C07C69/63C07D307/77C07D207/277C07C309/82C07C69/96C07C271/24C07D265/30C07D233/38C08F28/02G03F7/20
    • C07C69/63B33Y70/00B33Y80/00C07C69/753C07C69/96C07C271/24C07C309/82C07D207/277C07D233/38C07D265/30C07D307/77C07D311/74C08F28/02G03F7/004G03F7/20
    • The invention pertains to a compound generating an acid of the formula I or II, for instance corresponding sulfonium and iodonium salts, as well as corresponding sulfonyloximes wherein X is CH2 or CO; Y is O, NR4, S, O(CO), O(CO)O, O(CO)NR4, OSO2, O(CS), or O(CS)NR4; R1 is for example C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, interrupted C2-C18alkyl, interrupted C3-C30cycloalkyl, interrupted C3-C30cycloalkyl-C1-C18alkyl, interrupted C4-C30cycloalkenyl, phenyl, naphthyl, anthracyl, phenanthryl, biphenylyl, fluorenyl or heteroaryl, all unsubstituted or are substituted; or R1 is NR12R13; R2 and R3 are for example C3-C30cycloalkylene, C3-C30cycloalkyl-C1-C18alkylene, C1-C18alkylene, C1-C10haloalkylene, C2-C12alkenylene, C4-C30cycloalkenylene, phenylene, naphthylene, anthracylene, phenanthrylene, biphenylene or heteroarylene; all unsubstituted or substituted; R4 is for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl; R12 and R13 are for example C3-C30cycloalkyl, C3-C30cycloalkyl-C1-C18alkyl, C1-C18alkyl, C1-C10haloalkyl, C2-C12alkenyl, C4-C30cycloalkenyl, phenyl-C1-C3-alkyl, Ar, (CO)R15, (CO)OR15 or SO2R15; and Ar is phenyl, biphenylyl, fluorenyl, naphthyl, anthracyl, phenanthryl or heteroaryl, all unsubstituted or substituted.
    • 本发明涉及产生式I或II的酸的化合物,例如相应的锍盐和碘鎓盐,以及其中X是CH 2或CO的相应的磺酰肟; Y是O,NR4,S,O(CO),O(CO)O,O(CO)NR4,OSO2,O(CS)或O(CS)NR4; R 1是例如C 1 -C 18烷基,C 1 -C 10卤代烷基,C 2 -C 12烯基,C 4 -C 30环烯基,苯基-C 1 -C 3烷基,C 3 -C 30环烷基,C 3 -C 30环烷基-C 1 -C 18烷基,间断的C 2 -C 18烷基,间断的C 3 -C 30环烷基, 间断的C 3 -C 30环烷基-C 1 -C 18烷基,间断的C 4 -C 30环烯基,苯基,萘基,蒽基,菲基,联苯基,芴基或杂芳基,全部未取代或被取代; 或R1是NR12R13; R2和R3是例如C 3 -C 30亚环烷基,C 3 -C 30环烷基-C 1 -C 18亚烷基,C 1 -C 18亚烷基,C 1 -C 10卤代亚烷基,C 2 -C 12亚烯基,C 4 -C 30亚环烯基,亚苯基,亚萘基,亚蒽基,亚菲基,亚联苯基或亚杂芳基。 全部未取代或取代; R4是例如C 3 -C 30环烷基,C 3 -C 30环烷基-C 1 -C 18烷基,C 1 -C 18烷基,C 1 -C 10卤代烷基,C 2 -C 12链烯基,C 4 -C 30环烯基,苯基-C 1 -C 3烷基; R 12和R 13例如为C 3 -C 30环烷基,C 3 -C 30环烷基-C 1 -C 18烷基,C 1 -C 18烷基,C 1 -C 10卤代烷基,C 2 -C 12烯基,C 4 -C 30环烯基,苯基-C 1 -C 3烷基,Ar,(CO)R 15 CO)OR15或SO2R15; 并且Ar是苯基,联苯基,芴基,萘基,蒽基,菲基或杂芳基,全部是未取代或取代的。
    • 57. 发明申请
    • DHA DERIVATIVES AND THEIR USE AS MEDICAMENTS
    • DHA衍生物及其作为药物使用
    • US20100267828A1
    • 2010-10-21
    • US12740377
    • 2008-10-30
    • Anne Kristin HolmeideRagnar Hovland
    • Anne Kristin HolmeideRagnar Hovland
    • A61K31/232C07C69/587C07C67/00C12P7/64A61P3/10A61P3/04A61P29/00
    • C07C69/587C07C67/26C07C67/28C07C69/63
    • The present disclosure relates to compounds of the general formula (I): wherein R1 and R2 are the same or different and are chosen from a hydrogen atom, a hydroxy group, an alkyl group, a halogen atom, an alkoxy group, an acyloxy group, an acyl group, an alkenyl group, an alkynyl group, an aryl group, an alkylthio group, an alkoxycarbonyl group, an alkylsulfinyl group, an alkylsulfonyl group, an amino group, and an alkylamino group; or any pharmaceutically acceptable salt, solvate, complex, or pro-drug thereof; and their use as medicaments for the treatment of various diseases and conditions, for example, reduction of elevated triglyceride levels, i.e., hypertriglyceridemia, reduction of non-HDL cholesterol, reduction of glucose and HbA1c, and improvement of insulin resistance. The present disclosure also relates to a pharmaceutical composition comprising compounds of formula (I), as well as to processes for preparing compounds according to formula (I).
    • 本公开内容涉及通式(I)的化合物:其中R 1和R 2相同或不同,并且选自氢原子,羟基,烷基,卤素原子,烷氧基,酰氧基 酰基,烯基,炔基,芳基,烷硫基,烷氧基羰基,烷基亚磺酰基,烷基磺酰基,氨基和烷基氨基; 或其药学上可接受的盐,溶剂化物,复合物或前体药物; 以及它们作为用于治疗各种疾病和病症的药物的用途,例如降低甘油三酯水平升高,即高甘油三酯血症,降低非HDL胆固醇,降低葡萄糖和HbA1c以及改善胰岛素抵抗。 本公开还涉及包含式(I)化合物的药物组合物,以及用于制备根据式(I)的化合物的方法。