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41. 发明授权

US07345164B2 Production method of 5′-acyloxynucleoside compound 失效
标题翻译： 5'-酰氧基核苷化合物的制备方法
公开(公告)号：US07345164B2
公开(公告)日：2008-03-18
申请号：US10829950
申请日：2004-04-23
申请人： Daisuke Takahashi , Kunisuke Izawa
发明人： Daisuke Takahashi , Kunisuke Izawa
IPC分类号： C07H19/067 , C07H19/167
CPC分类号： C07H19/06 , C07H1/00 , C07H19/16
摘要： A production method for conveniently producing a 5′-acyloxynucleoside compound shown by the formula [A] in a good yield while suppressing formation of by-products, including subjecting a 2′,3′,5′-triacyloxynucleoside compound represented by the formula [I] to selective deacylation in an alcohol represented by the formula [II] using a base selected from the group consisting of alkali metal hydroxide, alkali metal alkoxide and alkali metal carbonate: wherein each symbol in the formula is as defined in the specification.
摘要翻译：包括使式[A]所示的2'，3'，5'-三酰氧基核苷化合物抑制副产物的形成，以良好的产率方便地制备式[A]所示的5'-酰氧基核苷化合物的方法， I]使用选自碱金属氢氧化物，碱金属醇盐和碱金属碳酸盐的碱选自式[II]表示的醇中的选择性脱酰基：其中式中的每个符号如说明书中所定义。

42. 发明申请

US20080015353A1 PROCESS FOR PRODUCTION OF 4-ACETYLPYRIMIDINES AND CRYSTALS THEREOF 审中-公开
标题翻译：生产4-乙酰基嘧啶及其结晶的方法
公开(公告)号：US20080015353A1
公开(公告)日：2008-01-17
申请号：US11832769
申请日：2007-08-02
申请人： Daisuke Takahashi , Kunisuke Izawa
发明人： Daisuke Takahashi , Kunisuke Izawa
IPC分类号： C07D239/02 , C07D403/02
CPC分类号： C07D239/38 , C07C45/68 , C07C45/70 , C07C49/255
摘要： Compound (II) is reacted with formate in the presence of an alkali metal alkoxide and the like to give compound (III); then this is reacted with compound (IVa) or compound (IVb) to give compound (V); then this is reacted with compound (VI) to give compound (VII); and then this is deprotected to give compound (I). The present invention provides an industrially advantageous production method of a 4-acetylpyrimidine compound useful as a synthetic intermediate for a pharmaceutical product: wherein X is a methylthio group and the like, R1 is a lower alkyl group and the like, R2 is a lower alkyl group optionally having substituent(s) and the like, M is an alkali metal and X1 is a halogen atom.
摘要翻译：在碱金属醇盐等存在下使化合物（II）与甲酸酯反应，得到化合物（III）; 然后使其与化合物（IVa）或化合物（IVb）反应，得到化合物（V）; 然后使其与化合物（VI）反应，得到化合物（VII）; 然后将其脱保护，得到化合物（I）。本发明提供了可用作药物合成中间体的4-乙酰基嘧啶化合物的工业上有利的制备方法：其中X是甲硫基等，R 1是低级烷基， R 2是任选具有取代基等的低级烷基，M是碱金属，X 1是卤素原子。

43. 发明申请

US20060270850A1 Processes for preparation of pyrimidine derivatives and intermediates 审中-公开
标题翻译：制备嘧啶衍生物和中间体的方法
公开(公告)号：US20060270850A1
公开(公告)日：2006-11-30
申请号：US11417233
申请日：2006-05-04
申请人： Daisuke Takahashi , Kunisuke Izawa
发明人： Daisuke Takahashi , Kunisuke Izawa
IPC分类号： C07D239/16
CPC分类号： C07D413/12
摘要： Compound (I) is reacted with compound (II) to give compound (III), which is then reacted with compound (IX) to give compound (VIII), which is then preferably deprotected by an enzyme reaction to give compound (XII). The present invention provides an advantageous process for preparing a pyrimidine derivative useful as an enzyme inhibitor, and a synthetic intermediate: wherein P is an alkyl group and the like, R1 and R2 are alkyl groups and the like, R3 is an alkyl group optionally having substituent(s) and the like, R4 is a hydrogen atom and the like, R5 is an aralkyl group optionally having substituent(s) and the like, and Y is a heteroaryl group optionally having substituent(s) and the like.
摘要翻译：化合物（I）与化合物（II）反应，得到化合物（III），然后与化合物（IX）反应，得到化合物（VIII），然后优选通过酶反应脱保护，得到化合物（Ⅻ）。本发明提供了制备可用作酶抑制剂的嘧啶衍生物的有利方法和合成中间体：其中P为烷基等，R 1和R 2， SUP>是烷基等，R 3是任选具有取代基等的烷基，R 4是氢原子等，R 任选具有取代基等的芳烷基，Y是任选具有取代基的杂芳基等。

44. 发明申请

US20050209257A1 5-Protected aminopyrimidine compound, production method thereof and intermediate therefor 失效
标题翻译： 5-保护氨基嘧啶化合物及其制备方法及其中间体
公开(公告)号：US20050209257A1
公开(公告)日：2005-09-22
申请号：US11081616
申请日：2005-03-17
申请人： Daisuke Takahashi , Kunisuke Izawa
发明人： Daisuke Takahashi , Kunisuke Izawa
IPC分类号： C07D239/46 , C07D239/47 , A61K31/513
CPC分类号： C07D239/47
摘要： The present invention provides a production method of 5-aminopyrimidine compound represented by the formula (5) by reacting a glycine compound represented by the formula (1) with t-butoxybisdimethylaminomethane, dimethylformamidedimethylacetal or dimethylformamidediethylacetal to produce a dialkylaminomethylene compound represented by the formula (2), reacting the compound of formula (2) in the presence of an acid to produce a hydroxymethylene compound represented by the formula (3), and reacting the compound of formula (3) with an amidine compound represented by the formula (4) or a salt thereof.
摘要翻译：本发明提供由式（1）表示的甘氨酸化合物与叔丁氧基二甲基氨基甲烷，二甲基甲酰胺二甲基乙缩醛或二甲基甲酰胺二乙基缩醛反应制备式（2）所示的5-氨基嘧啶化合物的制备方法，由式（2）表示的二烷基氨基亚甲基化合物），使式（2）的化合物在酸的存在下反应，生成由式（3）表示的羟基亚甲基化合物，并使式（3）的化合物与式（4）表示的脒化合物或式其盐。

45. 发明申请

US20050137404A1 Azlactone compound and method for preparation thereof 失效
标题翻译：吖内酯化合物及其制备方法
公开(公告)号：US20050137404A1
公开(公告)日：2005-06-23
申请号：US10980298
申请日：2004-11-04
申请人： Daisuke Takahashi , Kunisuke Izawa
发明人： Daisuke Takahashi , Kunisuke Izawa
IPC分类号： C07D263/42 , C07D263/18
CPC分类号： C07D263/42
摘要： Compounds represented by formula (II): wherein M is a hydrogen atom, sodium, potassium, or lithium; P is a hydrogen atom, an alkyl group, and the like; and the wavy line indicates a cis form, a trans form, or a mixture thereof for the double bond to which it is attached, may be prepared by hydrolyzing a compound represented by formula (I), or a salt thereof: wherein R1 and R2 are the same or different and each is an alkyl group, or R1 and R2 together with the adjacent nitrogen atom may form an aliphatic heterocycle, and P and the wavy line are as defined above, in the presence of alkali metal hydroxide.
摘要翻译：由式（II）表示的化合物：其中M是氢原子，钠，钾或锂; P是氢原子，烷基等; 并且波浪线表示其连接的双键的顺式，反式或其混合物，可以通过水解式（I）表示的化合物或其盐来制备：其中R ^{1和R 2相同或不同，并且各自为烷基，或R 1和R 2连同在碱金属氢氧化物的存在下，相邻的氮原子可以形成脂族杂环，P和波浪线如上所定义。}

46. 发明授权

US06906224B2 Process for producing α-aminoketones 失效
标题翻译：生产α-氨基酮的方法
公开(公告)号：US06906224B2
公开(公告)日：2005-06-14
申请号：US10695809
申请日：2003-10-30
申请人： Tomoyuki Onishi , Naoko Hirose , Takayuki Suzuki , Takashi Nakano , Masakazu Nakazawa , Kunisuke Izawa
发明人： Tomoyuki Onishi , Naoko Hirose , Takayuki Suzuki , Takashi Nakano , Masakazu Nakazawa , Kunisuke Izawa
IPC分类号： C07C213/00 , C07C215/28 , C07C221/00 , C07C225/16 , C07C269/06 , C07C271/16 , C07C271/18 , C07D263/04 , C07D263/18 , C07D263/20 , C07D301/26 , C07C209/62 , C07D301/28
CPC分类号： C07D263/04 , C07B2200/07 , C07C213/00 , C07C221/00 , C07C269/06 , C07D263/18 , C07D263/20 , C07D301/26 , C07C215/08 , C07C225/16 , C07C271/16 , C07C271/18
摘要： A process for producing α-aminohalomethyl ketones or N-protected α-aminohalomethyl ketones from specified 3-oxazolidin-5-one derivatives via 5-halomethyl-5-hydroxy-3-oxazolidine derivatives. By this process, α-aminohalomethyl ketones and compounds relating to them can be obtained efficiently and economically in industrial scale.
摘要翻译：通过5-卤代甲基-5-羟基-3-恶唑烷衍生物从指定的3-恶唑烷-5-酮衍生物生产α-氨基卤甲基酮或N-保护的α-氨基卤甲基酮的方法。通过该方法，可以在工业规模上有效和经济地获得与其相关的α-氨基卤甲基酮和化合物。

47. 发明授权

US06765100B2 Method for producing epoxide crystal 失效
标题翻译：环氧化物晶体的制备方法
公开(公告)号：US06765100B2
公开(公告)日：2004-07-20
申请号：US09973191
申请日：2001-10-10
申请人： Tomoyuki Onishi , Naoko Hirose , Yasuyuki Otake , Takashi Nakano , Yutaka Honda , Masakazu Nakazawa , Kunisuke Izawa
发明人： Tomoyuki Onishi , Naoko Hirose , Yasuyuki Otake , Takashi Nakano , Yutaka Honda , Masakazu Nakazawa , Kunisuke Izawa
IPC分类号： C07D30124
CPC分类号： C07C269/06 , C07B2200/07 , C07C269/08 , C07D263/24 , C07D303/36 , C07C271/16
摘要： The invention relates to a method for industrially producing highly pure (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide (crystal) or (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoalcohol. The method for producing N-carbamate-protected &bgr;-aminoepoxide crystal, includes one or more of the following steps (a) to (d): (a) dissolving (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoalcohol containing at least the diastereomer as an impurity in a solvent including at least one or more selected from aromatic hydrocarbon solvent, saturated hydrocarbon solvent, aqueous mixture solvent, acetone and 2-propanol, to remove insoluble matters; (b) treating the (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoalcohol with a base, thereby converting the N-carbamate-protected &bgr;-aminoalcohol to (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide; (c) treating the (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide containing at least the diastereomer as an impurity with an acid, thereby converting the diastereomer as an impurity to (4S, 5R) or (4R, 5S) oxazolidin-2-one derivative, and optionally separating and removing the resulting oxazolidin-2-one derivative in water or an aqueous mixture solvent; and (d) crystallizing the (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide in a mixture solvent of water and water-miscible organic solvent. By the methods of the present invention, highly pure (2R, 3S)- or (2S, 3R)-N-carbamate-protected &bgr;-aminoepoxide or (2R, 3S) or (2S, 3R)-N-carbamate-protected &bgr;-aminoalcohol can be efficiently produced.
摘要翻译：本发明涉及工业生产高纯度（2R，3S） - 或（2S，3R）-N-氨基甲酸酯保护的β-氨基环氧化物（晶体）或（2R，3S） - 或（2S，3R）-N 氨基甲酸酯保护的β-氨基醇。制备N-氨基甲酸酯保护的β-氨基环氧化物晶体的方法包括一个或多个以下步骤（a）至（d）:( a）将（2R，3S） - 或（2S，3R）-N-氨基甲酸酯在包含至少一种或多种选自芳族烃溶剂，饱和烃溶剂，含水混合物溶剂，丙酮和2-丙醇的溶剂的溶剂中至少含有作为杂质的非对映体的β-保护的β-氨基醇，以除去不溶物;（b）用碱处理（2R，3S） - 或（2S，3R）-N-氨基甲酸酯保护的β-氨基醇，从而将N-氨基甲酸酯保护的β-氨基醇转化为（2R，3S） - 或（2S，3R ）-N-氨基甲酸酯保护的β-氨基环氧化物;（c）用酸处理至少含有非对映体作为杂质的（2R，3S） - 或（2S，3R）-N-氨基甲酸酯保护的β-氨基环氧化物，由此将非对映异构体作为杂质转化为（4S，5R）或（4R，5S）恶唑烷-2-酮衍生物，任选分离和除去得到的恶唑烷-2-酮衍生物在水或含水混合溶剂中; 和（d）在水和水混溶性有机溶剂的混合溶剂中结晶（2R，3S） - 或（2S，3R）-N-氨基甲酸酯保护的β-氨基环氧化物。通过本发明的方法，高纯度（2R，3S） - 或（2S，3R）-N-氨基甲酸酯保护的β-氨基环氧化物或（2R，3S）或（2S，3R）-N-氨基甲酸酯保护的β - 氨基醇可以有效地生产。

48. 发明授权

US06579976B2 Process for producing 2′,3′-diethyl substituted nucleoside derivatives 失效
标题翻译：制备2'，3'-二乙基取代的核苷衍生物的方法
公开(公告)号：US06579976B2
公开(公告)日：2003-06-17
申请号：US09427082
申请日：1999-10-26
申请人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa
发明人： Satoshi Takamatsu , Satoshi Katayama , Naoko Hirose , Kunisuke Izawa
IPC分类号： C07H19173
CPC分类号： C07H19/04
摘要： There can be provided an excellent industrial process for producing compounds having sugar-moiety hydroxyl groups or halogen atoms reduced in nucleic acids or in derivatives thereof by allowing O-thiocarbonyl derivatives of sugar-moiety hydroxyl groups or allowing halogenated derivatives in the sugar-moiety, in the nucleic acids or in derivatives thereof to react with any one of hypophosphorous acids (including salts thereof) and phosphites (esters) which are inexpensive, non-toxic and safely usable as radical reducing agents in industrial scale, in the presence of a radical reaction initiator. The process of the present invention is an industrially useful and highly safe process for reducing sugar-moiety hydroxyl groups and halogen atoms in nucleic acids or derivatives thereof (including nucleic acid-related compounds) at low costs.
摘要翻译：可以提供通过使糖部分羟基的O-硫代羰基衍生物或糖部分中的卤代衍生物在核酸或其衍生物中还原的具有糖部分羟基或卤素原子的化合物的优异工业方法，在核酸或其衍生物中，在碱性存在下，与工业规模的廉价，无毒和可安全地用作自由基还原剂的次磷酸（包括其盐）和亚磷酸酯（酯）中的任何一种反应，反应引发剂。本发明的方法是以低成本还原核酸或其衍生物（包括核酸相关化合物）中的糖部分羟基和卤素原子的工业上有用和高度安全的方法。

49. 发明授权

US06538160B2 Process for producing &agr;-aminohalomethyl ketone derivatives 失效
公开(公告)号：US06538160B2
公开(公告)日：2003-03-25
申请号：US09730605
申请日：2000-12-07
申请人： Tomoyuki Onishi , Yasuyuki Otake , Masakazu Nakazawa , Kunisuke Izawa
发明人： Tomoyuki Onishi , Yasuyuki Otake , Masakazu Nakazawa , Kunisuke Izawa
IPC分类号： C07C22100
CPC分类号： C07C269/06 , C07D301/26 , C07D303/36 , Y02P20/55 , C07C271/18
摘要： Herein is disclosed a process for producing an &agr;-aminohalomethyl ketone derivative which comprises subjecting to catalytic reduction the corresponding &agr;-aminodihalomethyl ketone derivative, and which process is efficient and suited for industrial production thereof.

50. 发明授权

US6093846A Process for preparing optically active 2-hydroxy-methyl-3-phenylpropionic acid 失效
标题翻译：光学活性2-羟基 - 甲基-3-苯基丙酸的制备方法
公开(公告)号：US6093846A
公开(公告)日：2000-07-25
申请号：US450740
申请日：1999-11-30
申请人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
发明人： Hiroyuki Nohira , Takayuki Suzuki , Takayuki Hamada , Kunisuke Izawa
IPC分类号： C07B57/00 , C07C51/487 , C07C59/48 , C07C211/27 , C07C215/44
CPC分类号： C07C215/44 , C07C211/27 , C07C51/487 , C07C59/48
摘要： A process for preparing optically active 2-hydroxymethyl-3-phenylpropionic acid by resolving (RS)-2-hydroxymethyl-3-phenylpropionic acid via crystallization of an optically active amine salt, where the amine is optically active cis-1-amino-2-indanol salt, optically active .alpha.-methylbenzylamine salt, or optically active 3-methyl-2-phenyl-1-butylamine salt.
摘要翻译：通过用光学活性胺盐的结晶拆分（RS）-2-羟甲基-3-苯基丙酸来制备光学活性的2-羟甲基-3-苯基丙酸的方法，其中胺是光学活性的顺式-1-氨基-2 - 茚满盐，光学活性α-甲基苄胺盐或光学活性3-甲基-2-苯基-1-丁胺盐。

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