cas 10118-90-8, Minocycline | Articles data

Articles about 10118-90-8Total 12 be found

Palladium catalyzed C-N bond formation in the synthesis of 7-amino-substituted tetracyclines.
A facile synthesis of 7-alkylamino- and 7-cycloalkylaminotetracycline derivatives has been accomplished using an in situ generated aminostannane precursor. This procedure is advantageous in that it allows the concise synthesis of a number of unreported tetracycline derivatives that are cumbersome to prepare through traditional methods. These compounds are crucial to understanding structure activity relationships in the D-ring of tetracycline-type antibiotics and the acquired efflux resistance mechanism to this class of antibiotics.
Koza, Darrell J,Nsiah, Yaw A
p. 5025 - 5027
(2002)
Read Online

Synthesis method of minocycline hydrochloride
The invention discloses a preparation method of minocycline hydrochloride. The preparation method is characterized by comprising the following steps: with demeclocycline hydrochloride as an initial raw material, carrying out a dehydroxylation reaction to obtain 6-deoxy-6-demeclocycline (intermediate I for short); carrying out acetyl protection on the intermediate I to obtain 3,10,12,12a-tetraacetyl-6-deoxy-6-demeclocycline (intermediate II for short); carrying out the BuchwaldHartwig reaction on the intermediate II to obtain 3,10,12,12a-tetraacetylminocycline (intermediate III for short); hydrolyzing the intermediate III to obtain minocycline free alkali (intermediate IV for short); and salifying the intermediate IV to obtain minocycline hydrochloride. According to the invention, nitrification, diazotization and azo reactions used in traditional minocycline hydrochloride synthesis processes are avoided, so dangerous factors in the production process are reduced, operation is simple, environmental pollution is avoided, and the method has industrial production prospects.
-
Paragraph 0022; 0048-0051

(2021/03/31)

Synthetic method of minocycline and derivative of minocycline
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.
-
Paragraph 0024; 0025

(2019/09/13)

Preparation method of minocycline hydrochloride
The invention provides a preparation method of minocycline hydrochloride. The preparation method comprises the following steps: 1) preparing sancycline: preparing the sancycline by taking demeclocycline hydrochloride as a raw material; 2) preparing 7-iodosancycline: under a strong acid condition, taking N-iodosuccinimide and the sancycline to react to prepare a reaction solution, namely the 7-iodosancycline; 3) preparing the minocycline hydrochloride: taking the 7-iodosancycline and dimethylaminotrimethyl tin to react in an amine solvent and an amide solvent under the action of a palladium complex catalyst to prepare a reaction solution, and adjusting the pH (Potential of Hydrogen) of the reaction solution to be 0.8 to 1.0 with concentrated hydrochloric acid; after de-coloring with active carbon, adjusting the pH of the reaction solution to be 3.8 to 4.0 with ammonia water; freezing and crystallizing; after filtering, drying a filter cake to obtain the minocycline hydrochloride. The minocycline hydrochloride prepared by the preparation method has the advantages of low cost, stable structure, few isomer impurities, low content of epimers and relatively high product purity.
-
(2017/08/30)

Tigecycline impurity process for stereoselective preparation of
The invention discloses a tigecycline impurity stereoselective preparation method. According to the invention, minocycline hydrochloride is adopted as a raw material, and is stirred in lower alkanol and liquid acid; the temperature is increased to 35-45 DEG C; the temperature is maintained and a reaction is allowed for 2-5h; the temperature is reduced, and the pH value of the mixed liquid is regulated to 6.5-8.5, such that solid is precipitated; a reaction is carried out for 2h under controlled temperature; the pH value is retested and the pH value is not changed; the material is filtered; a lower alkanol solvent is used for washing a filter cake; and drying is carried out, such that tigecycline impurity E is obtained. The purity can be higher than 98.0%, and a yield is higher than 50%.
-
Paragraph 0041; 0042

(2017/06/24)

MINOCYCLINE DERIVATIVES
This invention relates generally to minocycline derivatives, and to compositions, including pharmaceutical compositions, containing such minocycline derivatives. The invention also relates to methods of synthesizing minocycline derivatives and to methods for using such minocycline derivatives as anti-bacterial agents for treating or preventing infections.
-
Paragraph 0052-0053

(2014/10/04)

Substituted Tetracycline Compounds
The present invention pertains, at least in part, to novel substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms.
-
Page/Page column 107

(2010/12/29)

TETRACYCLINE COMPOUNDS FOR THE TREATMENT OF RHEUMATOID ARTHRITIS AND RELATED METHODS OF TREATMENT
The present invention pertains, at least in part, to substituted tetracycline compounds. The present invention also pertains to methods for treating rheumatoid arthritis in a subject, comprising administering to the subject a tetracycline compound of the invention.
-
Page/Page column 36

(2010/04/25)

CRYSTALLINE MINOCYCLINE BASE AND PROCESSES FOR ITS PREPARATION
The invention provides crystalline minocycline base. In particular, three crystalline polymorphic forms, designated Form I, Form Il and Form III, of minocycline base are provided. These are characterised by XRD and IR data. Processes for preparing the new polymorphic forms are also provided. For example, Form I is prepared by dissolving and/or suspending amorphous minocycline base in an organic solvent chosen from ethers followed by crystallisation from the mixture.
-
Page/Page column 8

(2008/12/08)

Compositions and methods for treating hemorrhagic virus infections and other disorders
Cytokine-receptor and cytokine antagonist-enriched blood-dervided compositions and methods of preparing and using the compositions are provided. Also provided are compositions and methods for the treatment or prevention of disorders, especially acute inflammatory disorders involving pathological responses of the immune system, such as viral hemorrhagic diseases, sepsis, rheumatoid arthritis and other autoimmune disorders, acute cardiovascular events, flare-ups and acute phases of multiple sclerosis, wasting disorders and other disorders involving deleterious expression of cytokines and other factors, including tumor necrosis factor (TNF) and interleukin-1 (IL-1) are provided.
-
(2008/06/13)

Process for purifying 7-dimethylamino-6-demethyl-6-deoxytetracycline
A process for purifying 7-dimenthylamino-6-demethyl-6-deoxytetracycline represented by the following formula, STR1 which comprises dissolving 7-dimethylamino-6-demethyl-6-deoxytetracycline or its hydrochloride having a lower purity in a mixed solvent of an alcohol and water by using hydrochloric acid and then adjusting the pH of the solution to 3.5 to 4.5 to recrystallize the hydrochloride having a higher purity.
-
(2008/06/13)