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32 条记录 (耗时 0.02 秒)

    Accelerated process for preparing O-methyl phenols, N-methyl heteroaromatic compounds, and methylated aminophenols
    7.
    发明授权
    Accelerated process for preparing O-methyl phenols, N-methyl heteroaromatic compounds, and methylated aminophenols 有权
    制备O-甲基苯酚，N-甲基杂芳族化合物和甲基化氨基酚的加速方法

    公开(公告)号：US06706929B2

    公开(公告)日：2004-03-16

    申请号：US10459763

    申请日：2003-06-12

    申请人： Wen-Chung Shieh ,  Steven Dell

    发明人： Wen-Chung Shieh ,  Steven Dell

    IPC分类号： C07C4320

    CPC分类号： C07D235/06 ,  C07C41/16 ,  C07D209/08 ,  C07D209/86 ,  C07D235/18 ,  C07C43/2055 ,  C07C43/205

    摘要： An accelerated process for preparing an O-methyl phenol comprising reacting a phenol with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to another aspect, the invention provides an accelerated process for preparing an N-methyl heteroaromatic compound comprising reacting an NH-containing heteroaromatic compound with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. According to an additional aspect, the invention provides an accelerated process for preparing a methylated aminophenol comprising reacting an aminophenol having at least one N—H with dimethyl carbonate in the presence of a catalyst selected from 1,8-diazabicyclo[5.4.0]undec-7-ene; 1,4-diazabicyclo[2.2.2]octane; and dimethylaminopyridine. The process of the invention is especially advantageous since the process: (1) utilizes an environmentally friendly methylating reagent, dimethylcarbonate; (2) produces a high yield of the O-methyl phenols, N-methyl aromatic amines, and/or methylated aminophenols, generally 97-100% conversion; and (3) does not require a high-pressure (autoclave) reactor.

    摘要翻译： 一种制备O-甲基苯酚的加速方法，包括使苯酚与碳酸二甲酯在选自1,8-二氮杂双环[5.4.0]十一碳-7-烯的催化剂存在下反应; 1,4-二氮杂双环[2.2.2]辛烷; 和二甲基氨基吡啶。 根据另一方面，本发明提供了一种制备N-甲基杂芳族化合物的加速方法，包括使含NH杂芳族化合物与碳酸二甲酯在选自1,8-二氮杂双环[5.4.0]十一碳烯 - 七烯 1,4-二氮杂双环[2.2.2]辛烷; 和二甲基氨基吡啶。 根据另一方面，本发明提供了一种制备甲基化氨基苯酚的加速方法，包括在选自1,8-二氮杂双环[5.4.0]十一碳-7-烯的催化剂存在下使具有至少一个NH的氨基苯酚与碳酸二甲酯反应 烯; 1,4-二氮杂双环[2.2.2]辛烷; 和二甲基氨基吡啶。 本发明的方法是特别有利的，因为该方法：（1）利用环境友好的甲基化试剂，碳酸二甲酯; （2）产生高产率的O-甲基苯酚，N-甲基芳族胺和/或甲基化氨基苯酚，一般为97-100％转化率; 和（3）不需要高压（高压釜）反应器。

    Synthesis of enantiomerically enriched 4-piperidinylglycine
    8.
    发明授权
    Synthesis of enantiomerically enriched 4-piperidinylglycine 失效
    对映体富集的4-哌啶基甘氨酸的合成

    公开(公告)号：US06670477B2

    公开(公告)日：2003-12-30

    申请号：US10090087

    申请日：2002-03-04

    申请人： Wen-Chung Shieh ,  Song Xue ,  Noela Marjory Reel ,  John Joseph Fitt

    发明人： Wen-Chung Shieh ,  Song Xue ,  Noela Marjory Reel ,  John Joseph Fitt

    IPC分类号： C07D21122

    CPC分类号： C07D211/34 ,  Y02P20/55

    摘要： A process for making enantiomerically enriched 4-piperidinylglycine having the formula (I), said process comprising (a) combining N-protected glycine ester with 4-piperidone to form didehydroamino acid ester; (b) reducing the didehydroamino acid ester with hydrogen gas in the presence of a rhodium catalyst selected from the group consisting of (R,R)-BPE-Rh; (S,S)-BPE-Rh; (R,R)-DuPHOS-Rh; (S,S)-DuPHOS-Rh; and combinations thereof; whereby a protected compound is formed; and (c) removing the protecting groups from the protected compound, whereby the 4-piperidinylglyeine having the formula (I) is formed, wherein X− is an anion wherein X is independently a halogen; and “*” designates an asymmetric carbon having (R)- or (S)-configuration. The process of the invention yields an enantiomerically enriched (R)-4-piperidineglycine or (S)-4-piperidineglycine.

    摘要翻译： 制备具有式（I）的对映体富集的4-哌啶基甘氨酸的方法，所述方法包括（a）将N-保护的甘氨酸酯与4-哌啶酮组合以形成二氢氨基酸酯; （b）在选自（R，R）-BPE-Rh的铑催化剂存在下，用氢气还原二氢氨基酸酯; （S，S）-BPE-Rh; （R，R）-DuPHOS-Rh; （S，S）-DuPHOS-Rh; 及其组合; 从而形成受保护的化合物; 和（c）从保护的化合物中除去保护基，由此形成具有式（I）的4-哌啶基甘氨酸，其中X 1是阴离子，其中X独立地是卤素; 和“*”表示具有（R） - 或（S） - 构型的不对称碳。 本发明的方法产生对映异构体富集的（R）-4-哌啶甘氨酸或（S）-4-哌啶甘氨酸。

    Method of manufacture of (-)-galanthamine in high yield and purity substantially free of epigalanthamine
    9.
    发明授权
    Method of manufacture of (-)-galanthamine in high yield and purity substantially free of epigalanthamine 失效
    （ - ） - 加兰他敏以高产率和纯度生产基本上不含表意文胺的方法

    公开(公告)号：US5428159A

    公开(公告)日：1995-06-27

    申请号：US224932

    申请日：1994-04-08

    申请人： Wen-Chung Shieh ,  John A. Carlson

    发明人： Wen-Chung Shieh ,  John A. Carlson

    IPC分类号： C07D491/10 ,  C07D491/08

    CPC分类号： C07D491/10

    摘要： (-)-Galanthamine is obtained in substantially high yield and purity substantially without concomitant production of epigalanthamine by conversion of racemic narwedine to (-)-narwedine and subsequent reduction to (-)-galanthamine using bulky organo-aluminum or organo-boron reducing agents.

    摘要翻译： （ - ） - 加兰他敏以基本上高的产率和纯度获得，基本上没有通过将外消旋的narwedine转化为（ - ） - narwedine并随后通过使用大体积的有机铝或有机硼还原剂将其还原为（ - ） - 加兰他敏而伴随产生表观念珠胺 。