Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof
    2.
    发明授权
    Process for the preparation of substantially pure stavudine and related intermediates useful in the preparation thereof 失效
    制备基本上纯粹的司他夫定及其制备中有用的中间体的方法

    公开(公告)号:US06635753B1

    公开(公告)日:2003-10-21

    申请号:US09163321

    申请日:1998-09-30

    IPC分类号: C07H19073

    CPC分类号: C07H19/06

    摘要: There are disclosed novel Stavudine solvates as follows: Stavudine NN-dimethyllacetamide solvates; Stavudine NN-dimethylacrylamide solvates and Stavudine NN-dimethylpropionamide solvates and processes for producing Stavudine NN-dimethylacetamide solvates, Stavudine NN dimethylacrylamide solvates and Stavudine NN dimethylpropionamide solvates which results in pure Stavudine.

    摘要翻译: 公开了新的司他夫定溶剂合物如下:司他夫定NN-二甲基乙酰胺溶剂合物; 司他夫定NN-二甲基丙烯酰胺溶剂化物和司他夫定NN-二甲基丙酰胺溶剂化物和用于生产司他夫定NN-二甲基乙酰胺溶剂合物,司他夫定NN二甲基丙烯酰胺溶剂合物和司他夫定NN二甲基丙酰胺溶剂化物的方法,其产生纯的司他夫定。

    Process for the preparation of phenylcarbamates
    4.
    发明授权
    Process for the preparation of phenylcarbamates 失效
    苯基氨基甲酸酯的制备方法

    公开(公告)号:US07767843B2

    公开(公告)日:2010-08-03

    申请号:US11365596

    申请日:2006-03-02

    IPC分类号: C07C269/04

    CPC分类号: C07C269/04 C07C271/44

    摘要: A process for the preparation of aminoalkyl phenyl carbamate compounds of Formula I, wherein R1 and R2 independently are hydrogen or a C1-6 alkyl; R3 and R4 are the same or different and each is a C1-6 alkyl; or R3 and R4 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; R5 and R6 independently are hydrogen, linear, branched or cyclic C1-6 alkyl; or R5 and R6 together with the nitrogen to which they are attached form a cyclic three to eight membered ring, with or without a heteroatom like nitrogen or oxygen; the carbon centre designated “*” can be racemic or enantiomerically enriched in the (R)- or (S)- configuration; and pharmaceutically acceptable acid addition salts thereof.

    摘要翻译: 制备式I氨基烷基苯基氨基甲酸酯化合物的方法,其中R 1和R 2独立地是氢或C 1-6烷基; R3和R4相同或不同,各自为C1-6烷基; 或者R 3和R 4与它们所连接的氮一起形成具有或不具有氮或氧的杂原子的环状三元至八元环; R 5和R 6独立地是氢,直链,支链或环状C 1-6烷基; 或R 5和R 6与它们所连接的氮一起形成具有或不具有杂原子如氮或氧的环状三元至八元环; 指定为“*”的碳中心可以是(R) - 或(S) - 构型的外消旋或对映异构体富集; 及其药学上可接受的酸加成盐。

    Process to prepare, 1,4-dihydropyridine intermediates and derivatives thereof
    5.
    发明授权
    Process to prepare, 1,4-dihydropyridine intermediates and derivatives thereof 失效
    制备方法,1,4-二氢吡啶中间体及其衍生物

    公开(公告)号:US06858747B2

    公开(公告)日:2005-02-22

    申请号:US10819910

    申请日:2004-04-08

    CPC分类号: C07D211/90

    摘要: An improved catalyst is disclosed for a process involving the preparation of benzylidene intermediates useful in the preparation of 1,4-dihydropyridine compounds and derivatives thereof useful as medicines such as for example felodipine. This is accomplished by the condensation of an aldehyde and an acetoacetate in the presence of a novel catalyst system that includes a pyridyl carboxylic acid and a secondary amine. It has been found that through the use of the present invention the purity and yield of the desired isomer of the benzylidene intermediate can be maximized, thus avoiding the requirement of additional purification steps. The use of these intermediates can then be further reacted to form the required dihydropyridines, again having a very high purity and yield compared with the prior art.

    摘要翻译: 公开了一种改进的催化剂,其用于制备可用作制备1,4-二氢吡啶化合物及其衍生物的亚苄基中间体的方法,其用作药物,例如非洛地平。 这可以通过醛和乙酰乙酸酯在包含吡啶羧酸和仲胺的新型催化剂体系的存在下缩合来实现。 已经发现,通过使用本发明,可以使亚苄基中间体的所需异构体的纯度和产率最大化,从而避免了额外的纯化步骤的需要。 然后可以将这些中间体的使用进一步反应以形成所需的二氢吡啶,与现有技术相比,再次具有非常高的纯度和产率。

    Preparation of atorvastatin
    9.
    发明授权
    Preparation of atorvastatin 失效
    阿托伐他汀的制备

    公开(公告)号:US07193090B2

    公开(公告)日:2007-03-20

    申请号:US10800741

    申请日:2004-03-16

    IPC分类号: C07D207/00

    CPC分类号: C07D207/416 C07D207/34

    摘要: A process for preparing (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester comprising: (a) reduction of 5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-oxo-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester; (b) hydrolysis of (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-3-hydroxy-1-pentanoic acid, (R)-2-hydroxy-1,2,2-triphenylethyl ester using an alkali base in a solvent to form the acid; (c) alkylation of the acid forming (R)-5-[2-(4-fluorophenyl)-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrol-1-yl]-5-hydroxy-3-oxo-1-heptanoic acid, tert-butylester.

    摘要翻译: 制备(R)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基] -5 - 羟基-3-氧代-1-庚酸叔丁酯包括:(a)还原5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基 )羰基] -1H-吡咯-1-基] -3-氧代-1-戊酸,(R)-2-羟基-1,2,2-三苯乙基酯; (b)(R)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基] 3-羟基-1-戊酸,(R)-2-羟基-1,2,2-三苯基乙基酯,使用碱在溶剂中形成酸; (c)酸形成(R)-5- [2-(4-氟苯基)-5-(1-甲基乙基)-3-苯基-4 - [(苯基氨基)羰基] -1H-吡咯-1-基 吡啶-3-基] -5-羟基-3-氧代-1-庚酸叔丁酯。

    Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers
    10.
    发明授权
    Process for recovery of the desired cis-1,3-oxathiolane nucleosides from their undesired trans-isomers 失效
    从所需的反式异构体中回收所需的顺式-1,3-氧硫杂环戊烷核苷的方法

    公开(公告)号:US06600044B2

    公开(公告)日:2003-07-29

    申请号:US09881705

    申请日:2001-06-18

    IPC分类号: C07D41104

    CPC分类号: C07D411/04

    摘要: A process for the preparation of 1,3-oxathiolane nucleoside analogues in predominantly the cis-form, from mixture of cis-/trans-1,3-oxathiolane nucleosides or their protected derivatives thereof, comprising: (i) treatment of the cis-/trans-1,3-oxathiolane nucleosides (or protected derivatives thereof) with a pyrimidine base (or it derivatives thereof) and an acid, (ii) adding a suitable acid to the obtained cis-/trans-mixture of isomers, (iii) selective crystallization of the desired cis-isomer salt from a solvent or combination of solvents, and (iv) treatment of the predominantly cis-isomer salt with a suitable base to offer the free 1,3-oxathiolane nucleosides, and thereafter optionally repeating steps (i) to (iv) inclusive.

    摘要翻译: 从顺式 - 反式-1,3-氧硫杂环戊烷核苷或其受保护的衍生物的混合物制备主要为顺式的1,3-氧硫杂环戊烷核苷类似物的方法,包括:(i) (或其衍生物)和酸,(ii)向得到的异构体的顺式 ​​- 反式混合物中加入合适的酸,(iii)反式-1,3-氧硫杂环戊烷核苷(或其保护的衍生物)与嘧啶碱 )从溶剂或溶剂组合中选择性结晶所需的顺式异构体盐,和(iv)用合适的碱处理主要为顺式异构体盐以提供游离的1,3-氧硫杂环戊烷核苷,然后任选重复步骤 (i)至(iv)包括在内。