25420-97-7Relevant articles and documents
Preparation method of clindamycin hydrochloride impurities
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Paragraph 0094; 0101; 0102; 0103; 0104; 0105, (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 structure-activity relationships of novel lincomycin derivatives. Part 1. Newly generated antibacterial activities against Gram-positive bacteria with erm gene by C-7 modification
Wakiyama, Yoshinari,Kumura, Ko,Umemura, Eijiro,Ueda, Kazutaka,Masaki, Satomi,Kumura, Megumi,Fushimi, Hideki,Ajito, Keiichi
, p. 368 - 380 (2016/06/09)
We synthesized 7(S)-7-deoxy-7-arylthiolincomycin derivatives possessing a heterocyclic ring at the C-7 position via sulfur atom by either Mitsunobu reaction of 2,3,4-tris-O-(trimethylsiliyl)lincomycin or S N 2 reaction of 7-O-methanesulfonyl-2,3,4-tri-O-t
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.
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.
LINCOMYCIN DERIVATIVE AND ANTIBACTERIAL AGENT CONTAINING THE SAME AS ACTIVE INGREDIENT
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Page/Page column 46, (2008/12/08)
This invention provides compounds of formula (I) or its pharmacologically acceptable salt or solvate, wherein A represents aryl or a monocyclic or bicyclic heterocyclic group, R1 represents a halide, nitro, substituted C1-6 alkyl, optionally substituted amino, C1-6 alkyloxycarbonyl, optionally substituted aryl, a heterocyclic group, or heterocyclic carbonyl, R2 represents a hydrogen atom or C1-6 alkyl, R3 represents C1-6 alkyl, all of R4, R5, and R6 represent a hydrogen atom, R7 represents C1-6 alkyl, m is 1 or 2, and n is 1. The compounds are novel lincomycin derivatives having a potent activity against resistant pneumococci. The compounds can be used as an antimicrobial agent and are useful for preventing or treating bacterial infectious diseases.