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    Chemical process for preparing amide derivatives of antibiotic A 40926
    1.
    发明授权
    Chemical process for preparing amide derivatives of antibiotic A 40926 失效
    制备抗生素A 40926的酰胺衍生物的化学方法

    公开(公告)号：US06218505B1

    公开(公告)日：2001-04-17

    申请号：US09155869

    申请日：1998-10-07

    Applicant: Gianbattista Panzone ,  Alessandra Maria Marazzi ,  Ermenegildo Restelli ,  Anacleto Gianantonio

    Inventor： Gianbattista Panzone ,  Alessandra Maria Marazzi ,  Ermenegildo Restelli ,  Anacleto Gianantonio

    IPC: C07K1113

    CPC classification number: C07K9/008

    Abstract: Improved chemical process for preparing the compounds of formula (I), wherein: R1 represents (C9-C12)alkyl; M represents hydrogen, &agr;-D-mannopyranosyl or 6-O-acetyl-&agr;-D-mannopyranosyl and Y represents an amino group of formula —NR2-alk1-(NR3-alk2)p-(NR4-alk3)q-W. One aspect of the invention refers to the preparation of the intermediate compound of formula (III) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxy), by reacting a compound of formula (II) (which corresponds to the above compound of formula (I) wherein R1 and M are as above defined and Y is hydroxymethyl), with a (C1-C4)alkanol in the presence of a concentrated mineral acid, using the same alkanol as the reaction solvent and submitting the obtained ester compound to a reductive process by adding an alkali metal borohndride into the same reaction mixture. A further aspect of the invention refers to the amidation reaction for obtaining the compound of formula (I), which is carried out by reacting a compound of formula (III) with a suitable amine of formula (IV): NHR3-alk1-(NR4-alk2)p-(NR5-alk3)q-W, wherein R3, R4, R5, alk1, alk2, alk3, p, q and W are as defined in formula (I), in an inert organic solvent, in the presence of a condensing agent and setting the initial pH of the mixture (measured after diluting a sample of the reaction mixture with 9 volumes of water) at a value of from 6.5 to 9.0. By combining the above improved steps into a single process, it is possible to set up a particularly convenient process for preparing the compounds of formula (I). In addition, a purification method involving the use of polyamide resins and aqueous eluents is provided.

    Abstract translation: 制备式（I）化合物的改进的化学方法，其中：R 1表示（C 9 -C 12）烷基; M代表氢，α-D-吡喃甘露糖基或6-O-乙酰基-α-D-吡喃甘露糖基，Y代表式-NR2-alk1-（NR3-alk2）p-（NR4-alk3）q-W的氨基。 本发明的一个方面是指式（III）的中间体化合物（其对应于上述式（I）的化合物，其中R 1和M如上所定义且Y是羟基），通过使式 （II）（其对应于上述式（I）化合物，其中R 1和M如上所定义，Y是羟甲基）与（C1-C4）烷醇在浓无机酸存在下，使用相同的链烷醇 作为反应溶剂，并将所得的酯化合物通过向相同的反应混合物中加入碱金属硼氢化物而进行还原过程。 本发明的另一方面涉及获得式（I）化合物的酰胺化反应，其通过使式（III）的化合物与式（IV）的合适的胺反应来进行：NHR 3 - 烷基（NR 4 -alk2）p-（NR5-alk3）qW，其中R3，R4，R5，alk1，alk2，alk3，p，q和W如式（I）中所定义，在惰性有机溶剂中， 缩合剂并设定混合物的初始pH（在用9体积水稀释反应混合物的样品后测量）的值为6.5至9.0。 通过将上述改进的步骤结合到单一方法中，可以建立用于制备式（I）化合物的特别方便的方法。 此外，提供了涉及使用聚酰胺树脂和水性洗脱剂的纯化方法。

    Derivatives of antibiotic GE2270 factors C.sub.2a, D.sub.2 and E
    2.
    发明授权
    Derivatives of antibiotic GE2270 factors C.sub.2a, D.sub.2 and E 失效
    抗生素GE2270因子C2a，D2和E的衍生物

    公开(公告)号：US6008225A

    公开(公告)日：1999-12-28

    申请号：US101077

    申请日：1998-06-29

    Applicant: Sergio Lociuro ,  Paolo Tavecchia ,  Romeo Ciabatti ,  Ermenegildo Restelli

    Inventor： Sergio Lociuro ,  Paolo Tavecchia ,  Romeo Ciabatti ,  Ermenegildo Restelli

    IPC: A61K38/00 ,  A61K31/00 ,  A61K38/05 ,  A61P31/00 ,  A61P31/04 ,  C07K5/078 ,  C07K5/06 ,  C07K7/56

    CPC classification number: C07K5/06139 ,  A61K38/00

    Abstract: Mono- or di-substituted derivatives of GE2270 factors C.sub.2a, D.sub.2 and E of general formula (I), wherein W represents a moiety of formula (a), (b) or (c), R.sup.1 and R.sup.2 representing a variety of substituents, X.sup.1 is methyl, X.sup.2 is a --CH.sub.2 --W.sup.1 moiety and X.sup.3 is methylamino or amino, or X.sup.1 is a --CH.sub.2 --W.sup.1 moiety, X.sup.2 is methoxymethylene and X.sup.3 is methylamino, with the proviso that when X.sup.3 is amino, then W must be 2-(aminocarbonyl)-pyrrolidinyl; with the further proviso that when W is 2-(aminocarbonyl)-pyrrolidinyl, then W.sup.1 cannot be hydroxy; and the pharmaceutically acceptable salts thereof. The mono- or di-substituted derivatives of antibiotic GE 2270 of formula (I) are antimicrobial agents mainly active against gram positive bacteria. ##STR1##

    Abstract translation: PCT No.PCT / EP97 / 00628 Sec。 371日期1998年6月29日第 102（e）日期1998年6月29日PCT 1997年2月12日提交PCT公布。 公开号WO97 / 30078 日期：1997年8月21日通式（I）的GE2270因子C2a，D2和E的二取代衍生物，其中W表示式（a），（b）或（c）的部分，R1和R2表示 各种取代基，X1是甲基，X2是-CH2-W1部分，X3是甲基氨基或氨基，或X1是-CH2-W1部分，X2是甲氧基亚甲基，X3是甲基氨基，条件是当X3是氨基 那么W必须是2-（氨基羰基） - 吡咯烷基; 进一步的条件是当W是2-（氨基羰基） - 吡咯烷基时，则W1不能是羟基; 及其药学上可接受的盐。 式（I）的抗生素GE2270的单取代或二取代衍生物是主要对革兰氏阳性细菌有活性的抗微生物剂。

    Antibiotic A/16686 recovery process
    4.
    发明授权
    Antibiotic A/16686 recovery process 失效
    抗生素A / 16686恢复过程

    公开(公告)号：US5539087A

    公开(公告)日：1996-07-23

    申请号：US444808

    申请日：1995-05-18

    Applicant: Ermenegildo Restelli ,  Luigia Mainoli

    Inventor： Ermenegildo Restelli ,  Luigia Mainoli

    IPC: C12P21/00 ,  C07K1/14 ,  C07K1/36 ,  C07K11/00 ,  C07K14/195 ,  C07K14/41 ,  C12P21/02 ,  C12R1/045 ,  A61K38/12 ,  C07K1/30 ,  C12P21/04

    CPC classification number: C07K11/00 ,  C07K1/36

    Abstract: The present invention is directed to a process for recovering the antibiotics produced by fermentation of Actinoplanes sp. ATCC 33076 or a producing mutant thereof, from a fermentation broth or a process stream, which comprises extraction of the antibiotics by a non-ionic surfactant or a cationic surfactant miscible with or dispersable in water and capable of dissolving the antibiotics, formation of two phases in the first of which the antibiotic and the surfactant are present together, and separation of the antibiotic from the surfactant by addition of suitable organic solvents.

    Abstract translation: 本发明涉及一种回收由Actinoplanes sp。发酵生产的抗生素的方法。 ATCC 33076或其产生的突变体，其包括通过非离子表面活性剂或与水混溶或可分散在水中并能够溶解抗生素的非离子表面活性剂或阳离子表面活性剂提取抗生素，形成两相 其中首先将抗生素和表面活性剂一起存在，并通过加入合适的有机溶剂将抗生素与表面活性剂分离。

    Apparatus for the separation of a resin from a reaction mixture
    7.
    发明申请
    Apparatus for the separation of a resin from a reaction mixture 审中-公开
    用于从反应混合物中分离树脂的装置

    公开(公告)号：US20080023046A1

    公开(公告)日：2008-01-31

    申请号：US11827164

    申请日：2007-07-10

    Applicant: Ermenegildo Restelli ,  Espedito Forace ,  Alfio Messina ,  Antonio Ferreri

    Inventor： Ermenegildo Restelli ,  Espedito Forace ,  Alfio Messina ,  Antonio Ferreri

    IPC: B01D11/02

    CPC classification number: B01D29/01 ,  B01D29/54 ,  B01D29/965

    Abstract: An apparatus is provided for the separation of a resin from a reaction mixture. The apparatus comprises a column fitted with a side port, two inlet/outlet ports, and two flanges. Each flange is fitted with a multilayer net screen supported by a support grid. The column itself is attached to a support structure. A process is provided for using this apparatus to remove a resin from a reaction mixture, wherein the reaction mixture is added to the apparatus and the resin is filtered off, remaining in the column as the waste leaves. The remaining resin is then washed and eluted to provide a purified product.

    Abstract translation: 提供了用于从反应混合物中分离树脂的装置。 该装置包括一个装有侧面端口的列，两个入口/出口和两个凸缘。 每个法兰都装有一个由支撑网格支撑的多层网屏。 柱本身连接到支撑结构。 提供了一种使用该装置从反应混合物中除去树脂的方法，其中将反应混合物加入到装置中，并且将树脂滤出，随着废物离开而残留在塔中。 然后洗涤剩余的树脂并洗脱，得到纯化产物。

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