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
LINCOMYCIN DERIVATIVES AND ANTIBACTERIAL AGENTS CONTAINING THE SAME AS THE ACTIVE INGREDIENT
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Page/Page column 47, (2010/03/02)
An objective of the present invention is to provide compounds of formula (1) or their pharmacologically acceptable salts or solvates wherein A represents aryl; R1 represents N-optionally substituted C1-6 alkyl-N-optionally substituted C1-6 alkylamino-C1-6 alkyl; R2 represents a hydrogen atom or optionally substituted C1-6 alkyl; R3 represents optionally substituted C1-6alkyl or C3-6 cycloalkyl-C1-4 alkyl; m is 1 to 3; n is 0; and p is 0 to 2. The compounds are novel lincomycin derivatives that have a potent activity against resistant Streptococcus pneumoniae, which have recently posed problems, in the treatment of infectious diseases. Further, the compounds are usable as antimicrobial agents and are useful for preventing or treating bacterial infectious diseases.