147650-54-2

Usage

Uses

Used in Pharmaceutical Industry:
3,4-O-Isopropylidene ClindaMycin is used as an intermediate compound for the preparation of Clindamycin impurities. Its role in this application is crucial for enhancing the purity and effectiveness of Clindamycin, which is a widely used antibiotic for treating various bacterial infections. By focusing on the development and refinement of Clindamycin impurities, 3,4-O-Isopropylidene ClindaMycin contributes to the overall improvement of antibiotic therapies and their potential to combat resistant bacterial strains.

Upstream product

• 17431-55-9 clindamycin hydrochloride 
• 77-76-9 2,2-dimethoxy-propane 
• 16684-06-3 clindamycin 
• 122-51-0 orthoformic acid triethyl ester 
• 859-18-7 lincomycin hydrochloride 
• 67-64-1 acetone 
• 21462-39-5 clindamycin hydrochloride 

Relevant academic research and scientific papers

Synthesis process of clindamycin palmitate hydrochloride

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.

A clindamycin phosphate ester synthesis method

The invention belongs to the technical field of chemical synthesis and specifically relates to a synthetic method of clindamycin phosphate. The method comprises the following steps of synthesis of clindamycin free alkali, ketonization reaction, phosphorylation reaction and aftertreatment. According to the invention, the weight yield of the clindamycin phosphate can reach over 80% by changing a charging sequence, steps and a catalyst.

CONJUGATE-BASED ANTIFUNGAL AND ANTIBACTERIAL PRODRUGS

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.