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    Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof
    1.
    发明授权
    Process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives thereof 失效
    制备1,5-（阿基米诺）-1,5-二脱氧-D-葡萄糖苷及其衍生物的方法

    公开(公告)号：US5151519A

    公开(公告)日：1992-09-29

    申请号：US521282

    申请日：1990-05-07

    申请人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    发明人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    IPC分类号： C07D211/46 ,  C07D307/20 ,  C07D493/10

    CPC分类号： C07D493/10 ,  C07D211/46 ,  C07D307/20

    摘要： A process for the preparation of 1,5-(alkylimino)-1,5-dideoxy-D-glucitol and derivatives of the formula: ##STR1## wherein R is hydrogen, alkyl of 1 to 13 carbon atoms, and aralkyl wherein alkyl is a lower alkyl of 2 to 6 carbon atoms, and aryl is phenyl, unsubstituted or substituted with lower alkyl of 1 to 6 carbon atoms, halo, lower alkoxy of 1 to 4 carbon atoms or thio lower alkyl of 1 to 4 carbon atoms by the steps of: treating L-sorbose with 2,2-dimethoxypropane to yield 1,2:4,6-di-O-(1-methylethylidene)-.alpha.-L-sorbanose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; adsorbing the compound on an ion exchange resin and hydrogenating to produce compounds of the above formula.

    摘要翻译： 制备1,5-（烷基亚氨基）-1,5-二脱氧-D-葡萄糖醇的方法和下式的衍生物：其中R是氢，1至13个碳原子的烷基，和其中烷基是 2至6个碳原子的低级烷基，芳基是未取代的或被1至6个碳原子的低级烷基取代的苯基，卤素，1至4个碳原子的低级烷氧基或1至4个碳原子的硫代低级烷基， 步骤：用2,2-二甲氧基丙烷处理L-山梨糖，得到1,2：4,6-di-O-（1-甲基亚乙基）-α-L-山梨糖; 在溶剂中用硫酸处理该化合物以产生1,2-O-（1-甲基乙基）-α-L-呋喃核糖; 连续用磺酰氯和胺处理，得到6-（取代的氨基）-6-脱氧-1,2-（1-甲基乙基）-α-L-呋喃核糖; 将化合物吸附在离子交换树脂上并进行氢化以制备上式的化合物。

    Process for the preparation of 6-(n-butylamino)-6-deoxy-1,2-O-(imeihylethylidine)-a-L-Sorbofuranose and derivatives thereof
    2.
    发明授权
    Process for the preparation of 6-(n-butylamino)-6-deoxy-1,2-O-(imeihylethylidine)-a-L-Sorbofuranose and derivatives thereof 失效
    6-（正丁基氨基）-6-脱氧-1,2-（1-甲基乙基）-a-L-呋喃核糖及其衍生物的制备方法

    公开(公告)号：US5281724A

    公开(公告)日：1994-01-25

    申请号：US720335

    申请日：1991-06-25

    申请人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    发明人： James R. Behling ,  Payman Farid ,  Ish Khanna ,  John R. Medich ,  Mike Prunier ,  Mike G. Scaros ,  Richard M. Weier

    IPC分类号： C07D211/46 ,  C07D307/20 ,  C07D493/10

    CPC分类号： C07D493/10 ,  C07D211/46 ,  C07D307/20

    摘要： A process for the preparation of 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and 6-(n-substituted amino)-6-deoxy-1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose and derivatives of the formula: ##STR1## wherein R' is benzyl or R, wherein R is hydrogen, alkyl of 1 to 13 carbon atoms, and aralkyl wherein alkyl is a lower alkyl of 2 to 6 carbon atoms and aryl is phenyl, unsubstituted or substituted with lower alkyl of 1 to 6 carbon atoms, halo, lower alkoxy of 1 to 4 carbon atoms or thio lower alkyl of 1 to 4 carbon atoms by the steps of: treating L-sorbose with 2,2-dimethoxy propane to yield 1,2:4,6-di-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; treating the compound with sulfuric acid in a solvent to produce 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose; and consecutively treating with sulfonyl chloride and with an amine to yield 6-(substituted amino)-6-deoxy- 1,2-O-(1-methylethylidine)-.alpha.-L-sorbofuranose.

    摘要翻译： 制备1,2-O-（1-甲基乙基）-α-L-呋喃核糖和6-（正 - 取代氨基）-6-脱氧-1,2-（1-甲基乙基） - α -L-呋喃核糖和下式的衍生物：其中R'是苄基或R，其中R是氢，1至13个碳原子的烷基和芳烷基，其中烷基是2至6个碳原子的低级烷基和芳基 是未取代的或被1至6个碳原子的低级烷基取代的苯基，卤素，1至4个碳原子的低级烷氧基或1至4个碳原子的硫代低级烷基，其步骤为：用2,2-双 得到1,2：4,6-二-O-（1-甲基乙基）-α-L-呋喃核糖; 在溶剂中用硫酸处理该化合物以产生1,2-O-（1-甲基乙基）-α-L-呋喃核糖; 并用磺酰氯和胺连续处理，得到6-（取代的氨基）-6-脱氧-1,2-（1-甲基乙基）-α-L-呋喃核糖。

    Process for the preparation of heterocyclic alkylamide derivatives
    5.
    发明授权
    Process for the preparation of heterocyclic alkylamide derivatives 失效
    制备杂环烷基酰胺衍生物的方法

    公开(公告)号：US5432284A

    公开(公告)日：1995-07-11

    申请号：US118073

    申请日：1993-09-08

    申请人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

    发明人： John H. Dygos ,  Thomas R. Kowar ,  Kathleen T. McLaughlin ,  Gatis Plume ,  Michael L. Prunier ,  Richard J. Salzmann ,  Mike G. Scaros ,  Joseph J. Wieczorek

    IPC分类号： C07D295/145 ,  C07D207/09 ,  C07D211/32 ,  C07D211/60

    CPC分类号： C07D295/145

    摘要： The present invention relates to a novel process for the preparation of heterocyclic alkylamide derivatives having the following formula: ##STR1## and the pharmaceutically acceptable acid addition salt thereof wherein X represents halo, alkyl having 1 to 6 carbon atoms, hydrido, trifluoromethyl, phenyl, or lower alkoxy having 1 to 6 carbon atoms; Y represents the group --CN or --CONH.sub.2 ; R.sub.2 represents alkyl having 1 to 6 carbon atoms; R.sub.3 represents acetyl, benzoyl, phenacetyl or trifluoroacetyl; m is the integer 1 or 2 and n is an integer from 1 to 3 inclusive; which comprises alkylating an aminoalkanol using a benzaldehyde/aminoalkanol/ketone mixture in the presence of a platinum catalyst to give an alkyl substituted phenylmethylaminoalkanol; halogenating the alkanol using a halogenating agent to give a haloalkyl alkylbenzenemethanamine salt; treating the salt with substituted phenyl piperidinealkanenitrile or substituted phenyl pyrrolidinealkanenitrile in the presence of base and dimethyl sulfoxide to give a substituted phenyl substituted aminoalkyl piperidinealkanenitrile or substituted aminoalkyl pyrrolidinealkanenitrile; hydration of the nitrile to give the corresponding amide; and N-debenzylation of the amide followed by acetylation to give the compounds of formula I wherein Y is --CONH.sub.2.

    摘要翻译： 本发明涉及制备具有下式的杂环烷基酰胺衍生物的新方法：其中X表示卤素，具有1至6个碳原子的烷基，羟基，三氟甲基（I）及其药学上可接受的酸加成盐 ，苯基或具有1至6个碳原子的低级烷氧基; Y代表基团-CN或-CONH 2; R 2表示具有1至6个碳原子的烷基; R3表示乙酰基，苯甲酰基，苯乙酰基或三氟乙酰基; m为1或2的整数，n为1〜3的整数， 其包括在铂催化剂存在下使用苯甲醛/氨基烷醇/酮混合物烷基化氨基烷醇，得到烷基取代的苯基甲基氨基烷基醇; 使用卤化剂卤化烷醇得到卤代烷基烷基苯甲胺盐; 在碱和二甲基亚砜的存在下用取代的苯基哌啶烷腈或取代的苯基吡咯烷烷腈处理盐，得到取代的苯基取代的氨基烷基哌啶烷腈或取代的氨基烷基吡咯烷烷腈; 腈水合得到相应的酰胺; 和酰胺的N-去苄基化，然后进行乙酰化，得到其中Y为-CONH 2的式I化合物。

    Process for producing n-substituted polyhydroxy nitrogen-containing heterocycles utilizing acetobacteraceae and corynebacterium
    6.
    发明授权
    Process for producing n-substituted polyhydroxy nitrogen-containing heterocycles utilizing acetobacteraceae and corynebacterium 失效
    利用醋杆菌属和棒状杆菌生产含n-取代多羟基含氮杂环的方法

    公开(公告)号：US5401645A

    公开(公告)日：1995-03-28

    申请号：US851818

    申请日：1992-03-16

    申请人： Roy W. Grabner ,  Bryan H. Landis ,  Mike G. Scaros ,  Rick J. Rutter

    发明人： Roy W. Grabner ,  Bryan H. Landis ,  Mike G. Scaros ,  Rick J. Rutter

    IPC分类号： C08L5/00 ,  C07C213/02 ,  C07D207/12 ,  C07D211/46 ,  C07H15/12 ,  C07H15/18 ,  C12N11/00 ,  C12P17/04 ,  C12P17/06 ,  C12P17/10 ,  C12P17/12 ,  C12P19/26 ,  C12R1/01 ,  C12R1/02 ,  C12P19/02 ,  C12P19/12

    CPC分类号： C07H15/12 ,  C07C213/02 ,  C07D207/12 ,  C07D211/46 ,  C07H15/18 ,  C12P19/26

    摘要： A process for producing N-substituted amino compounds, a process for oxidizing an N-substituted amino compound with a microbe, or cell fragment or cell free extract thereof, and a process for oxidizing an N-substituted amino compound with a microbe, or cell fragment or cell free extract thereof and reducing the oxidized N-substituted amino compound to N-substituted-polyhydroxy piperidines based on N-substituted mannosamines, allosamines and altrosamines, N-substituted polyhydroxy pyrrolidines, and N-substituted polyhydroxy azetidines. In addition, a one pot process for producing N-substituted-polyhydroxy piperidines based on N-substituted mannosamines, allosamines and altrosamines, N-substituted polyhydroxy pyrrolidines, and N-substituted polyhydroxy azetidines from the respective sugar is disclosed. A second embodiment comprises novel compositions of N-substituted-amino-6-deoxy-2-ketohexuloses based on mannose, allose and altrose, N-substituted-amino-5-deoxy-2-ketopentuloses and 4-(N-substituted)-amino-1,3-dihydroxy-2-butanones.

    摘要翻译： 用于生产N-取代的氨基化合物的方法，用微生物氧化N-取代的氨基化合物的方法或其细胞片段或无细胞提取物，以及用微生物或细胞氧化N-取代的氨基化合物的方法 基于N-取代的甘露糖胺，异构胺和阿替罗斯胺，N-取代的多羟基吡咯烷酮和N-取代的多羟基氮杂环丁烷将氧化的N-取代的氨基化合物还原为N-取代的多羟基哌啶。 另外，公开了一种基于N-取代的甘露糖胺，异构胺和二异丙胺，N-取代的多羟基吡咯烷酮和N-取代的多羟基氮杂环丁烷从各自的糖生产N-取代的多羟基哌啶的一锅法。 第二个实施方案包含基于甘露糖，阿洛糖和阿卓糖，N-取代的 - 氨基-5-脱氧-2-酮戊酸和4-（N-取代的） - 酮基的N-取代的 - 氨基-6-脱氧-2-酮基六氢离子的新组合物， 氨基-1,3-二羟基-2-丁酮。

    Synthesis of N-(N-(3,3-dimethylbutyl)-L-&agr;-aspartyl)L-phenylalanine1-methyl ester by reductive alkylation and crystallization/ isolation in aqueous methanol
    9.
    发明授权
    Synthesis of N-(N-(3,3-dimethylbutyl)-L-&agr;-aspartyl)L-phenylalanine1-methyl ester by reductive alkylation and crystallization/ isolation in aqueous methanol 有权
    通过在甲醇水溶液中还原烷基化和结晶/分离合成N-（N-（3,3-二甲基丁基）-L-α-天冬氨酰基）L-苯丙氨酸1-甲酯

    公开(公告)号：US06281380B1

    公开(公告)日：2001-08-28

    申请号：US09572843

    申请日：2000-05-18

    申请人： Indra Prakash ,  Mike G. Scaros ,  Kurt L. Wachholder

    发明人： Indra Prakash ,  Mike G. Scaros ,  Kurt L. Wachholder

    IPC分类号： C07C22900

    CPC分类号： C07K5/06113

    摘要： N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester is produced by reductive alkylation and crystallization/isolation in methanol and water. The production method is efficient and low cost, as compared with conventional N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester synthesis and results in high purity N-[N-(3,3-dimethylbutyl)-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.

    摘要翻译： 通过在甲醇和水中还原烷基化和结晶/分离产生N- [N-（3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯。 与常规N- [N-（3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯合成相比，制备方法是有效和低成本的，并且导致高纯度的N- [N - （3,3-二甲基丁基）-L-α-天冬氨酰基] -L-苯丙氨酸1-甲酯。