CONTAINERLESS SYNTHESIS OF AMORPHOUS AND NANOPHASE ORGANIC MATERIALS
    72.
    发明申请
    CONTAINERLESS SYNTHESIS OF AMORPHOUS AND NANOPHASE ORGANIC MATERIALS 有权
    不规则合成非晶态和纳米有机材料

    公开(公告)号:US20120197005A1

    公开(公告)日:2012-08-02

    申请号:US13361164

    申请日:2012-01-30

    CPC分类号: B01J19/10

    摘要: The invention provides a method for producing a mixture of amorphous compounds, the method comprising supplying a solution containing the compounds; and allowing at least a portion of the solvent of the solution to evaporate while preventing the solute of the solution from contacting a nucleation point. Also provided is a method for transforming solids to amorphous material, the method comprising heating the solids in an environment to form a melt, wherein the environment contains no nucleation points; and cooling the melt in the environment.

    摘要翻译: 本发明提供一种制备无定形化合物混合物的方法,该方法包括提供含有该化合物的溶液; 并允许溶液的至少一部分溶剂蒸发,同时防止溶液的溶质接触成核点。 还提供了将固体转化为无定形材料的方法,该方法包括在环境中加热固体以形成熔体,其中环境不含成核点; 并在环境中冷却熔体。

    PROCESS FOR THE PREPARATION OF OXCARBAZEPINE
    73.
    发明申请
    PROCESS FOR THE PREPARATION OF OXCARBAZEPINE 有权
    制备奥沙拉贝的方法

    公开(公告)号:US20110065917A1

    公开(公告)日:2011-03-17

    申请号:US12991600

    申请日:2009-05-06

    IPC分类号: C07D223/18

    CPC分类号: C07D223/22

    摘要: The present invention relates to an improved process for the preparation of 10-oxo-10,11-dihydiO-5H-dibenz[b,fjazepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[b,f]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of α-hydroxy acids, and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

    摘要翻译: 本发明涉及通过使10-甲氧基-5H-二苯并[b,f]喹唑啉反应制备10-氧代-10,11-二氢-5H-二苯并[b,fjazepine-5-甲酰胺(奥卡西平) 吖庚因(10-甲氧基亚氨基芪)和碱金属氰酸盐存在的α-羟基酸,也涉及从亚氨基茋制备卡马西平的方法。 此外,本发明涉及10-甲氧基卡马西平的新结晶形式。

    Phosphoramidite ligand and production method of allylic amine using the same
    74.
    发明授权
    Phosphoramidite ligand and production method of allylic amine using the same 失效
    亚磷酰胺配体和烯丙基胺的制备方法使用相同

    公开(公告)号:US07863443B2

    公开(公告)日:2011-01-04

    申请号:US12045269

    申请日:2008-03-10

    申请人: Erick M. Carreira

    发明人: Erick M. Carreira

    IPC分类号: C07D223/18

    摘要: The present invention provides a production method of an allylic amine represented by the formula (III): wherein R3 is as defined in the specification, which comprises reacting by an allylic alcohol represented by the formula (II): wherein R3 is as defined in the specification, with sulfamic acid, in the presence of a phosphoramidite ligand represented by the formula (I): wherein each symbol is as defined in the specification, and an iridium complex. According to the present invention, a primary allylic amine can be produced directly from an allylic alcohol, without use of an activator for an allylic alcohol and conversion of an allylic alcohol into an activated compound thereof.

    摘要翻译: 本发明提供由式(III)表示的烯丙胺的制备方法:其中R3如说明书中所定义,其包括由式(II)表示的烯丙醇:其中R 3如 在氨基磺酸的情况下,在由式(I)表示的亚磷酰胺配体的存在下,其中每个符号如说明书中所定义,和铱络合物。 根据本发明,可以直接从烯丙醇制备初级烯丙基胺,不使用烯丙醇的活化剂和将烯丙醇转化成其活化化合物。

    SMALL MOLECULE COMPOUNDS FOR STEM CELL DIFFERENTIATION
    75.
    发明申请
    SMALL MOLECULE COMPOUNDS FOR STEM CELL DIFFERENTIATION 有权
    小分子化合物用于干细胞分化

    公开(公告)号:US20100159596A1

    公开(公告)日:2010-06-24

    申请号:US12561235

    申请日:2009-09-16

    摘要: Methods and small molecule compounds for stem cell differentiation are provided. One example of a class of compounds that may be used is represented by the compound having the structure IA or IB in the form of free base or a pharmaceutically acceptable salt, hydrate, solvate or N-oxide thereof: R1 is independently hydrogen or (C1-C6)alkyl; R2 is independently hydrogen, (C1-C6)alkyl, aryl, or heteroaryl; R2′ is independently hydrogen, (C1-C6)alkyl, CF3 or C2F5; R3 is independently (C1-C6)alkyl, aryl, 2-tetrahydrofurylmethyl, an aliphatic tertiary amine, or 4-methoxybenzyl; or R2 and R3 may be joined together to form a 5 or 6 member ring lactone; R4 is independently hydrogen, (C1-C6)alkyl, a 2- or 4-R5-substituted aromatic ring selected from a 4-R5-phenyl or a 2-R5-5-pyridyl, aryl, heteroaryl, aliphatic tertiary amine or halogen; and R5, R5′, R6, R6′, R7, R7′, are each independently hydrogen, (C1-C6)alkyl, aryl, optionally substituted phenyl, heteroaryl, a heterocyclic ring, an aliphatic tertiary amine, or halogen.

    摘要翻译: 提供了干细胞分化的方法和小分子化合物。 可以使用的一类化合物的一个实例由具有游离碱或其药学上可接受的盐,水合物,溶剂合物或N-氧化物形式的结构IA或IB的化合物表示:R1独立地是氢或(C1 -C 6)烷基; R2独立地是氢,(C1-C6)烷基,芳基或杂芳基; R2'独立地是氢,(C1-C6)烷基,CF3或C2F5; R3独立地为(C1-C6)烷基,芳基,2-四氢呋喃基甲基,脂肪族叔胺或4-甲氧基苄基; 或者R 2和R 3可以连接在一起以形成5或6元环内酯; R4独立地为氢,(C1-C6)烷基,选自4-R5-苯基或2-R5-5-吡啶基,芳基,杂芳基,脂族叔胺或卤素的2或4-R 5 - 取代的芳环 ; 和R 5,R 5',R 6,R 6',R 7,R 7'各自独立地为氢,(C 1 -C 6)烷基,芳基,任选取代的苯基,杂芳基,杂环,脂族叔胺或卤素。

    Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride
    78.
    发明申请
    Novel process for preparation of 10-oxo-10, 11-dihydro-5h-dibenz [b,f] azepine-5-carbox- amide (oxcarbazepine) via intermediate, 10-methoxy-5h-debenz[b,f] azepine-5-carbonyl- chloride 审中-公开
    通过中间体10-甲氧基-5H-脱苄基[b,f]吖庚因 - (1H) - 酮制备10-氧代-10,11-二氢-5H-二苯并[b,f]吖庚因-5-甲酰胺(奥卡西平) 5-羰基氯

    公开(公告)号:US20070032647A1

    公开(公告)日:2007-02-08

    申请号:US10576546

    申请日:2004-10-15

    IPC分类号: C07D223/18

    CPC分类号: C07D223/28

    摘要: A process for preparation of 10-oxo-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (oxcarbazepine) via intermediate 10-methoxy-5H-dibenz[b,f]azepine-5-carbonyl chloride, comprising the steps: a) Preparation of an intermediate 10-methoxy-5H-dibenz[b,f]azepine-5 carbonyl, chloride from 10-methoxyiminostillbene using bis (trichloromethyl) carbonate (BTC) with organic base such as aliphatic or aromatic tertiary amines in organic solvent; b) Conversion of the intermediate to 10-methoxy-5H-dibenz[b,f]azepine-5-carboxamide using ammonia in organic solvent; c) Formation of oxcarbazepine from step (b) using Bronsted acid in an organic solvent at a temperature between 25° C.-80° C., preferably at 50° C. to 70° C.; and d) Isolation of oxcarbazepine.

    摘要翻译: 通过中间体10-甲氧基-5H-二苯并[b,f]吖庚因-5-羰基制备10-氧代-10,11-二氢-5H-二苯并[b,f]吖庚因-5-甲酰胺(奥卡西平)的方法 氯化物,包括以下步骤:a)使用碳酸二(三氯甲基)酯(BTC)与有机碱如脂族或者其它物质,由10-甲氧基亚氨基茋制备中间体10-甲氧基-5H-二苯并[b,f]吖庚因-5-羰基氯化物 有机溶剂中的芳香族叔胺; b)使用氨在有机溶剂中将中间体转化为10-甲氧基-5H-二苯并[b,f]吖庚因-5-甲酰胺; c)在25℃-80℃,优选在50℃至70℃的温度下,使用布朗斯台德酸在有机溶剂中形成步骤(b)中的奥卡西平。 和d)奥卡西平的分离。