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12 条记录 (耗时 0.035 秒)

    Steroid intermediates and processes for their preparation
    8.
    发明授权
    Steroid intermediates and processes for their preparation 失效
    类固醇中间体及其制备方法

    公开(公告)号：US5502183A

    公开(公告)日：1996-03-26

    申请号：US256812

    申请日：1994-07-25

    申请人： David R. Andrews ,  Anantha R. Sudhakar

    发明人： David R. Andrews ,  Anantha R. Sudhakar

    IPC分类号： A61K31/57 ,  A61P31/04 ,  C07J1/00 ,  C07J5/00 ,  C07J7/00 ,  C07J13/00 ,  C07J21/00 ,  C07J31/00 ,  C07J41/00 ,  C07J43/00 ,  C07J51/00

    CPC分类号： C07J5/0053 ,  C07J1/0011 ,  C07J1/0048 ,  C07J13/005 ,  C07J13/007 ,  C07J21/00 ,  C07J31/006 ,  C07J41/005 ,  C07J41/0094 ,  C07J43/003 ,  C07J5/0076 ,  C07J5/0092 ,  C07J51/00 ,  C07J7/0085

    摘要： Novel steroids having a 9.alpha.-hydroxy or a 9.alpha.-carbonate substituent can be prepared from 9.alpha.-hydroxyandrostenedione and can be utilized in the synthesis of commercially valuable corticosteroids such as betamethasone. The 9.alpha.-carbonates are prepared by reaction of the corresponding 9.alpha.-hydroxy steroid with a sequence of excess base, trialkylsilyl chloride, alkyl haloformate and alkanol or by using excess base, alkyl haloformate and alkoxide. 9.alpha.-Carbonate-17-keto compounds can be treated with lithium acetylide and a lithium salt to afford the corresponding 17.alpha.-ethynyl-17.beta.-hydroxy-9.alpha.-carbonate. This compound is then esterified with a novel series of reagents to give the 17-ester which can be reduced the corresponding 17-allene. Oxidation of this allene to the bis-epoxide compound, followed by treatment with an alkali metal salt of a carboxylic acid under phase transfer conditions gives the 17.alpha.-hydroxy 21-ester 9.alpha.-carbonate. Elimination of the 9.alpha.-carbonate group affords the a 17.alpha.-hydroxy, 9(11)ene, which in a few subsequent steps can be converted to a variety of commercially important corticosteroids. Novel 9.alpha.-carbonate compounds are prepared in the various reaction steps.

    摘要翻译： PCT No.PCT / US93 / 00211 Sec。 371日期：1994年7月25日 102（e）日期1994年7月25日PCT提交1993年1月26日PCT公布。 公开号WO93 / 15103 日期：1993年8月5日。具有9α-羟基或9α-碳酸酯取代基的新型类固醇可以由9α-羟基雄烯二酮制备，并可用于合成市售有价值的皮质类固醇如倍他米松。 通过相应的9α-羟基类固醇与过量碱，三烷基甲硅烷基氯，烷基卤代甲酸酯和链烷醇的反应或通过使用过量的碱，卤代甲酸烷基酯和醇盐反应制备9α-碳酸酯。 可以用乙炔锂和锂盐处理9α-碳酸酯-17-酮化合物，得到相应的17α-乙炔基-17β-羟基-9α-碳酸酯。 然后将该化合物用新的一系列试剂酯化，得到可以还原相应的17-全烯的17-酯。 将该丙烯氧化成双环氧化合物，然后在相转移条件下用羧酸的碱金属盐处理，得到17α-羟基21-酯9α-碳酸酯。 消除9个α-碳酸酯基提供了17α-羟基，9（11）烯，其在后续的几个步骤中可转化为多种商业上重要的皮质类固醇。 在各种反应步骤中制备新的9种α-碳酸酯化合物。

    Optically active intermediates for the preparation of optically active substituted oximes, hydrazones and olefins useful as neurokinin antagonists
    9.
    发明授权
    Optically active intermediates for the preparation of optically active substituted oximes, hydrazones and olefins useful as neurokinin antagonists 失效
    用于制备用作神经激肽拮抗剂的光学活性取代的肟，腙和烯烃的光学活性中间体

    公开(公告)号：US06265614B1

    公开(公告)日：2001-07-24

    申请号：US09687905

    申请日：2000-10-13

    申请人： Anantha R. Sudhakar ,  Suhan Tang

    发明人： Anantha R. Sudhakar ,  Suhan Tang

    IPC分类号： C07C23900

    CPC分类号： C07C225/16 ,  C07B2200/07 ,  C07C251/40 ,  C07C271/18 ,  Y02P20/55

    摘要： Intermediates having the formula wherein BI is —CH2OH or —CH2ORP, and RP is an alcohol protecting group; a is 1, 2, or 3; TI is —OH or QI is phenyl, naphthyl ohr heteroaryl having 1-3 substituents; Ra and Rc are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl cycloalkyl, aryl, or —OH; or Ra and Rc together with the C—N—C chain to which they are bound, form a 5-7 membered ring; Rb and Rd are the same, and are H, or are selected from alkyl, cycloalkyl and aryl groups, the groups being optionally substituted with one or more substituents selected from alkyl, cycloalkyl, aryl, or —OH; and D is a directing group capable of directing lithiation alpha to a nitrogen atom of a nitrogen compound having D as a substituent bound to the nitrogen atom when the nitrogen compound is reacted with s-butyl lithium, are disclosed. The intermediates have an enantiomeric excess of the R enantiomer over the corresponding S enantiomer of greater than 85%, preferably, greater than 95%, and are useful for preparing optically active substituted oximes, hydrazones and olefins that are useful as neurokinin antagonists.

    摘要翻译： 具有甲醛的中间体是-CH 2 OH或-CH 2 ORP，RP是醇保护基; a是1,2或3; TI是-OH或Q 1是苯基，具有1-3个取代基的萘基芳基杂芳基; R a和R c是 相同且为H，或选自烷基，环烷基和芳基，该基团任选被一个或多个选自烷基环烷基，芳基或-OH的取代基取代; 或R a和R c与它们所连接的CNC链一起形成5-7元环; Rb和Rd相同，为H或选自烷基，环烷基和芳基，该基团任选被取代 与一个或多个选自烷基，环烷基，芳基或-OH的取代基取代; 并且D是当氮化合物与仲丁基锂反应时，能够将具有D作为与氮原子结合的取代基的氮化合物的氮原子引入锂化的导向基团。 中间体具有超过85％，优选大于95％的相应S对映异构体的R对映异构体的对映异构体过量，并且可用于制备可用作神经激肽拮抗剂的光学活性取代的肟，腙和烯烃。

    BISULFITE PURIFICATION OF AN ALPHA-KETO AMIDE
    10.
    发明申请
    BISULFITE PURIFICATION OF AN ALPHA-KETO AMIDE 有权
    一种ALPHA-KETO酰胺的双相纯化

    公开(公告)号：US20090326244A1

    公开(公告)日：2009-12-31

    申请号：US12518736

    申请日：2007-12-13

    申请人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    发明人： George S. K. Wong ,  Jeonghan Park ,  Tetsuo Iwama ,  Anantha R. Sudhakar

    IPC分类号： C07D209/52

    CPC分类号： C07D209/52

    摘要： A process for purifying the alpha-keto amide is (1R,5S)—N-[3-amino-1-(cyclobutylmethyl)-2,3-dioxopropyl]-3-[2(S)-[[[(1,1-dimethylethyl)amino]carbonyl]-amino]-3,3-dimethyl-1-oxobutyl]-6,6-dimethyl-3-azabicyclo[3.1.0]hexan-2(S)-carboxamide via a bisulfite adduct is disclosed.

    摘要翻译： 纯化α-酮酰胺的方法是（1R，5S）-N- [3-氨基-1-（环丁基甲基）-2,3-二氧代丙基] -3- [2（S） - [[ 1,1-二甲基乙基）氨基]羰基] - 氨基] -3,3-二甲基-1-氧代丁基] -6,6-二甲基-3-氮杂双环[3.1.0]己-2（S） - 甲酰胺通过亚硫酸氢盐加合物 披露