- Preparation method of plazomicin
-
The invention discloses a preparation method of plazomicin. According to the invention, 6'amino of sisomicin and Cbz-ONB make a nucleophilic substitution reaction under the action of selective coordination and chelation of zinc acetate to obtain a compound 2; all hydroxyl groups and other amino groups of the compound 2 are protected by using silanization reagent to generate a full silanization product; the full silanization product and N-t-butyloxycarboryl-4-amino-2(S)-hydroxybutyric acid make selective condensation and a silane protection group is removed to obtain a compound 4; other amino groups in the compound 4 are protected by a Boc protecting group to obtain a compound 5; and then reaction is performed on the compound 5 to obtain plazomicin. Compared with an original research route,the disclosed process has advantages of being short in synthesis steps, mild in experimental conditions, simple, easy to operate and thus is suitable for industrial production.
- -
-
Paragraph 0032-0034
(2020/03/29)
-
- NOVEL ANTIBACTERIAL 3"-DERIVATIVES OF 4,6-DISUBSTITUTED 2,5-DIDEOXYSTREPTAMINE AMINOGLYCOSIDE ANTIBIOTICS
-
The present invention relates to novel aminoglycoside compounds having antimicrobial properties and being suitable, for example, as therapeutic agents for use in the treatment of mammalian disease and in particular to novel therapeutic agents suitable for use in the treatment of microbial infection in mammals. The present invention further relates to the use of pharmaceutical compositions comprising said agents in the treatment of medical conditions in mammals, in particular in the treatment of microbial infection. The agents and pharmaceutical compositions of the invention are of particular relevance in the treatment of diseases associated with antibiotic-resistant microbes. The invention further relates to compounds for use in the treatment of diseases whose treatment is made otherwise difficult due to antibiotic-class-related bacterial resistance and provides novel therapeutic agents suitable for use in the treatment of multidrug-resistant (MDR) infections.
- -
-
Page/Page column 198; 261; 262; 264
(2020/07/05)
-
- RNA targeting compounds and methods for making and using same
-
Disclosed are RNA targeting compounds, methods for using the subject RNA targeting compounds to treat myotonic dystrophy and other diseases are also disclosed.
- -
-
Page/Page column 53; 54
(2016/03/13)
-
- 5-Norbornene-2,3-dicarboximido Carbonochloridate. A New Stable Reagent for the Introduction of Amino-Protecting Groups
-
The synthesis of activated carbonates, based on a new carbonochloridate derived from N-hydroxy-5-norbornene-2,3-dicarboximide, is reported.These activated carbonic esters are excellent reagents for the introduction of all currently used urethane protecting groups.
- Henklein, Peter,Heyne, Hans-Ulrich,Halatsch, Wolf-Rainer,Niedrich, Hartmut
-
p. 166 - 167
(2007/10/02)
-