147650-54-2Relevant articles and documents
Synthesis process of clindamycin palmitate hydrochloride
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Paragraph 0029; 0032-0034; 0038-0040; 0044-0046; 0048-0050, (2021/04/10)
The invention provides a synthesis process of clindamycin palmitate hydrochloride. Clindamycin hydrochloride as a parent and pyridine are mixed and heated, 2,2-dimethoxypropane is added, a reaction is performed sufficiently, and the residual pyridine and 2,2-dimethoxypropane are distilled off after the reaction is ended to reduce the generation of byproducts; then acetone is added to separate out solids, water and sodium hydroxide are added to obtain 3,4-o-isopropylidene-clindamycin with few impurities, and palmitoyl chloride and the 3,4-o-isopropylidene-clindamycin are mixed at a certain temperature and fully react, thereby facilitating the subsequent generation of high-purity products and increasing the target product content; and then a protecting group is removed by acidolysis, washing is performed with a detergent and water to remove the impurities, sodium sulfate is added to remove the water and the residual detergent, and finally hydrochloric acid is added to treat viscous liquid at a certain temperature, thereby reducing the production of byproducts and increasing the product yield.
CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS
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Paragraph 0449, (2015/01/06)
The invention provides conjugate-based antifungal or antibacterial prodrugs formed by coupling at least one anti-fungal agent or antibacterial agent with at least one linker and/or carrier. The prodrugs are of formula: (i) (AFA)m-X-(L)n; (ii) [(AFA)m′-X]p-L; (iii) AFA-[X-(L)n′]q; or (iv) (AFA)m″-X, wherein: AFA is an antifungal agent or an antibacterial agent; L is a carrier; X is a linker; m ranges from 1 to 10; n ranges from 2 to 10; m′ is 1 to 10; p is 1 to 10; n′ is 1 to 10; and q is 1 to 10, provided that q′ and n are not both 1; and m″ is 1 to 10. The invention also provides nanoparticles comprising the conjugate-based prodrugs. Additionally, the invention also provides non-conjugated antifungal and antibacterial agents in the form of nanoparticles.