摘要:
Disclosed are rifamycin derivatives having antibacterial activities, wherein the compounds have the following general formula: wherein: R is hydrogen or acetyl; R1 and R2 are independently selected from the group consisting of hydrogen, (C1-4)alkyl, benzyloxy, mono- and di-(C1-3)alkylamino-(C1-4)alkyl, (C1-3)alkoxy, (C1-4)alkyl, hydroxy-methyl, hydroxy-(C2-4)-alkyl, and nitro or R1 and R2 taken together with two consecutive carbon atoms of the pyridine nucleus form a benzene ring optionally substituted by one or two methyl or ethyl groups and R3 is hydroxyalkyl(C1-4). In addition, processes to obtain these compounds are described.
摘要:
Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
摘要:
Crystalline polymorphous forms of rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ, useful in the production of medicinal preparations containing rifaximin for oral and topical use and obtained by means of a crystallization carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a determinate temperature and for a determinate period of time, followed by a drying carried out under controlled conditions until reaching a settled water content in the end product, are the object of the invention.
摘要:
Crystalline polymorphous forms of rifaximin (INN), referred to as rifaximin α and rifaximin β, and a poorly crystalline form referred to as rifaximin γ, useful in the production of medicaments containing rifaximin for oral and topical use and obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by addition of water at a fixed temperature and for a fixed period of time, followed by a drying under controlled conditions until reaching a precise water content in the end product, are the object of the invention.
摘要:
The present invention relates to a process for the preparation of gabapentin and, more in particular, to a method of synthesis of 1,1-cyclohexane acetic acid monoamide, an intermediate used in the preparation of gabapentin, comprising the basic hydrolysis reaction of α, -diaminocarbonyl-β,β-pentamethylene glutarimide.
摘要:
A process for the preparation of 1,1-cyclohexanediacetic acid monoamide comprising the amination of 1,1-cyclohexanediacetic acid anhydride by reaction with aqueous NH3 at a temperature lower than 30° C. by using a NH3/anhydride molar ratio lower than 3, and the product precipitation through the acidification of the reaction mixture; a precipitation process of 1,1-cyclohexanediacetic acid monoamide; and a process for the synthesis of gabapentin comprising the above preparation of 1,1-cyclohexanediacetic acid monoamide, the Hofmann transposition of the same monoamide, the purification of a gabapentin salt and the crystallization from organic solvent.
摘要:
A process for the purification of gabapentin by treatment of a crude aqueous gabapentin hydrochloride solution with a strong cationic ion exchange resin.
摘要:
A process for the purification of gabapentin by treatment of a crude aqueous gabapentin hydrochloride solution with a strong cationic ion exchange resin.
摘要:
Crystalline polymorphous forms of the rifaximin (INN) antibiotic named rifaximin α and rifaximin β, and a poorly crystalline form named rifaximin γ have been discovered. These forms are useful in the production of medicinal preparations for oral and topical use and can be obtained by means of a crystallization process carried out by hot-dissolving the raw rifaximin in ethyl alcohol and by causing the crystallization of the product by the addition of water at a determinate temperature and for a determinate period of time. The crystallization is followed by drying carried out under controlled conditions until a specific water content is reached in the end product.