- Synthesis and structure-activity relationship of novel glycylcycline derivatives leading to the discovery of GAR-936
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A number of new glycylcyclines were synthesized for structure-activity relationship study. Many of the derivatives exhibit potent, broad spectrum antibacterial activity against both tetracycline susceptible and resistant organisms. GAR-936 (TBG-MINO) shows better activity than the previously reported DMG-MINO and DMG-DMDOT.
- Sum, Phaik-Eng,Petersen, Peter
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- Purification method of tigecycline
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The invention discloses a purification method of tigecycline in the technical field of medicinal chemistry. The purification method of tigecycline comprises the following specific steps: S1, adding 9-aminominocycline hydrochloride and N-tert-butylglycyl chloride hydrochloride, and carrying out a reaction under stirring; S2, after the reaction is completed, adding a protective agent, and adjustingthe pH value of the reaction solution to 7.0-7.4 with 14-20% of ammonia water; S3, carrying out chromatography; and S4, collecting the purified desorption solution, drying, filtering to remove the drying agent, and drying under reduced pressure to obtain the tigecycline finished product. The method provided by the invention has the advantages of high yield, good impurity removal effects, low organic solvent consumption, recoverability, simple process and easy control, and is especially suitable for industrial production.
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Paragraph 0019-0029
(2020/12/08)
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- Synthetic method of minocycline and derivative of minocycline
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The invention relates to a synthetic method of minocycline and substituted minocycline, and especially synthesis of 9-amino minocycline. 9-amino minocycline is an important intermediate of tigecycline, and tigecycline is mostly used for control on multiple resistant bacteria. The raw materials are easily available; the synthetic route is short; reaction conditions are mild; the yield is high; thetechnology is simple; and the synthetic method is suitable for large scale production.
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Paragraph 0026; 0027
(2019/09/13)
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- A by to a fund of rapamycin synthesis of tigecycline new method (by machine translation)
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The invention provides a synthesis of erythromycin by to a fund of tigecycline new method, comprises the following steps: would go to a fund ycin nitration, catalytic reduction, with tert-butyl amine acetyl chloride hydrochloride reaction, further nitration reaction, catalytic reduction, methylation reaction to obtain a crude product such as prostacyclin for canada 6 step reaction can; be the final purification tigecycline. Short reaction steps of this invention, high purity, low cost, non-toxic and the like, is suitable for mass production. (by machine translation)
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- Preparation method of tigecycline
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The invention relates to a preparation method of tigecycline. The preparation method comprises the following steps of condensating N-t-butylglycine with 9-aminosancycline under the action of a compound condensating agent, and making the tigecycline through nitration and reductive methylation. The preparation method is simple and convenient in process; an obtained product is high in yield and high in purity.
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Paragraph 0018; 0019; 0026
(2017/07/22)
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- PROCESS FOR THE PREPARATION OF TIGECYCLINE
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The present invention relates to an improved process for the preparation of tigecycline. The process comprises treating minocycline hydrochloride with nitrating agent at low temperature followed by reduction in presence of catalyst to produce 9-aminominocycline disulphate in granular form. It is then reacted with N-t-butylglycyl chloride hydrochloride at pH below 3 under nitrogen atmosphere to obtain tigecycline.
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Page/Page column 14-15
(2010/04/25)
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- TIGECYCLINE FORMULATIONS
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The invention is directed to a frozen pharmaceutical formulation suitable for administration to a subject parenterally, comprising a therapeutically effective amount of tigecycline and an agent selected from the group consisting of lactose, dextrose, glucose, mannose, sucrose, ribose, xylose and a combination thereof, wherein the formulation in a pre-frozen state at about 22° C. or in an unfrozen state at about 22° C. has a pH in the range of from 4.0 to 5.5. Preferably, the formulation is suitable for storage at or below about ?20° C. over a period of at least about 2 months, preferably 6 months, more preferably 26 months. Alternatively, the formulation is suitable for storage at about 22° C. over a period of about 24 hours.
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- ANTIBIOTIC COMPOUNDS
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The present invention relates to the new crystalline solid form Xl of Tigecycline and a process of preparing the same. Form Xl of Tigecycline is particularly suitable for the isolation of Tigecycline in the last step of the synthesis of Tigecycline. Further the present invention relates to a process of preparing amorphous Tigecycline by spray drying form Xl or another crystalline form of Tigecycline.
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Page/Page column 7
(2009/09/05)
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- PROCESSES FOR PREPARATION OF CRYSTALLINE TIGECYCLINE FORM II
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The present invention provides processes for the preparation of crystalline forms of Tigecycline.
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Page/Page column 10
(2009/07/03)
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- PROCESSES FOR PREPARATION OF 9-HALOACETAMIDOMINOCYCLINES
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The present invention provides substantially pure intermediates, 9- haloacetomidominocyclines, and process of preparing them that are useful for the preparation of glycylcyclines, specifically Tigecycline.
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Page/Page column 10
(2008/12/06)
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- Processes for purification of tigecycline
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The invention is directed to improved processes of purifying tigecycline.
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Page/Page column 2
(2008/12/08)
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- TIGECYCLINE AND METHODS OF PREPARING 9-NITROMINOCYCLINE
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Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
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Page/Page column 60
(2010/11/25)
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- CRYSTALLINE SOLID FORMS OF TIGECYCLINE AND METHODS OF PREPARING SAME
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Crystalline solid forms of tigecycline, Form I, Form II, Form III, Form IV, and Form V, compositions comprising these crystalline solid forms, and processes for preparing these crystalline solid forms are described herein.
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Page/Page column 15-16
(2008/06/13)
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- TIGECYCLINE AND METHODS OF PREPARATION
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Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
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Page/Page column 59
(2010/11/25)
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- METHODS OF PURIFYING TIGECYCLINE
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Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
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Page/Page column 59
(2010/11/25)
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- TIGECYCLINE AND METHODS OF PREPARING 9-AMINOMINOCYCLINE
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Methods of preparing and purifying tetracyclines, such as tigecycline, are disclosed. Also disclosed are tetracycline compositions, such as tigecycline compositions, prepared by these methods.
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Page/Page column 58-59
(2010/11/25)
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