25420-97-7Relevant articles and documents
Preparation method of clindamycin hydrochloride impurities
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, (2020/01/08)
The invention relates to a preparation method of clindamycin hydrochloride impurities, which belongs to the field of medicines. The technical problem to be solved by the invention is that a method forefficiently preparing clindamycin hydrochloride impurities 7-epilincomycin and 7-epilincomycin hydrochloride reference substances is lacked in the prior art. The invention provides a preparation method of a clindamycin hydrochloride impurity intermediate shown as a formula II, which comprises the following steps: by using a compound shown as a formula I and R1COOH as raw materials, carrying out aMitsunobu substitution reaction for preparation, and adding amine and/or a nitrogen-containing aromatic heterocyclic compound into a reaction solution. The invention further provides a complete synthesis method of the 7-epilincomycin and the 7-epilincomycin hydrochloride. The complete synthesis method comprises the following steps: by taking lincomycin as a raw material, carrying out silicon protection group coating, selective deprotection, Mitsunobu substitution reaction and hydrolysis reaction to obtain the 7-epilincomycin, and further carrying out a chlorination reaction to prepare the 7-epilincomycin hydrochloride.
Synthesis and antibacterial activity of novel lincomycin derivatives. I. Enhancement of antibacterial activities by introduction of substituted azetidines
Kumura, Ko,Wakiyama, Yoshinari,Ueda, Kazutaka,Umemura, Eijiro,Watanabe, Takashi,Shitara, Eiki,Fushimi, Hideki,Yoshida, Takuji,Ajito, Keiichi
, p. 440 - 445 (2016/07/11)
The synthesis and antibacterial activity of (7S)-7-sulfur-Azetidin-3-yl lincomycin derivatives are described. Modification was achieved by a simple reaction of (7R)-7-O-methanesulfonyllincomycin and the corresponding substituted azetidine-2-Thiol. Several
LINCOSAMIDE DERIVATIVE, AND ANTIBACTERIAL AGENT COMPRISING THE SAME AS ACTIVE INGREDIENT
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Page/Page column 28, (2010/04/24)
An objective of the present invention is to provide compounds of formula (I) or their pharmacologically acceptable salts or solvates wherein A represents aryl while R1 represents a five- or six-membered monocyclic heterocyclic group, or A represents a four- to six-membered monocyclic heterocyclic group while R1 represents aryl or a five- or six-membered monocyclic heterocyclic group; R2 represents a hydrogen atom or C1-6 alkyl; R3 represents C1-6 alkyl or C3-6 cycloalkyl-C1-4 alkyl; R4, R5, and R6 represent a hydrogen atom; R7 represents C1-6 alkyl; and m is 1 to 3. The compounds are novel lincosamide derivatives that have a potent activity against resistant Streptococcus pneumoniae. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.