484670-64-6Relevant academic research and scientific papers
A preparation of a macrocyclic lactone method
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Paragraph 0024; 0029; 0030, (2017/12/28)
The invention relates to a new preparation method of macrolides, belonging to the field of medicinal chemistry. The invention further relates to a preparation method of Solithromycin. The new preparation method comprises the following step of carrying out 7-th position saccharide ring removal, hydroxyl oxidation and reductive amination with a side chain to obtain an important intermediate (5) having a formula shown in the specification. The preparation method of Solithromycin, disclosed by the invention, has the advantages of few side reactions, operation simpleness and convenience, high yield and high suitability for industrial production. The structure of the intermediate (5) is as shown in the specification.
Solithromycin and preparation method of intermediate thereof
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Paragraph 0061-0062, (2017/04/03)
The invention relates to solithromycin and a preparation method of an intermediate thereof. According to the preparation method, a target compound is prepared from clarithromycin as a starting material through the steps of hydroxyl group protection, hydroxyl group activation, sugar ring removal, oxidation, fluorization, side chain loading, deprotection, reduction and the like. The preparation method is high in yield and applicable to industrial application, and the operation is simple. The invention further provides a novel intermediate for preparing solithromycin and a preparation method of the novel intermediate.
PROCESSES FOR PREPARING MACROLIDES AND KETOLIDES AND INTERMEDIATES THEREFOR
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, (2015/09/22)
The invention described herein pertains to processes for the preparation of macrolide antibacterial agents. In particular, the invention pertains to processes for preparing macrolides and ketolides from erythromycin A.
HYDROGEN BOND FORMING FLUORO KETOLIDES FOR TREATING DISEASES
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, (2012/03/27)
The invention described herein pertains to a novel macrolide antibacterial agent of formula (I): A-L-Q, as defined herein, and pharmaceutically acceptable salts, solvates, and hydrates thereof. Inter alia, the new macrolide antibacterial agent is active a
Synthesis and antibacterial activity of C-12 pyrazolinyl spiro ketolides
Hu, Lei,Lan, Ping,Song, Qiu-Ling,Huang, Zhi-Jian,Sun, Ping-Hua,Zhuo, Chao,Wang, Ying,Xiao, Shunian,Chen, Wei-Min
scheme or table, p. 5943 - 5949 (2011/01/13)
A series of C-12 pyrazolinyl spiro ketolide derivatives were designed and synthesized. The C-12 modifications involved replacing the natural C-12 methyl group in clarithromycin core with different pyrazolinyl spiros via chemical synthesis. Potential anti-
Novel process for the preparation of telithromycin
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Page/Page column 13, (2008/06/13)
The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts wherein, R is
NOVEL PROCESS FOR THE PREPARATION OF TELITHROMYCIN
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Page/Page column 20, (2010/11/30)
The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts wherein, (R) is a.
Synthesis and antibacterial activity of novel C12 vinyl ketolides
Burger, Matthew T.,Lin, Xiaodong,Chu, Daniel T.,Hiebert, Christy,Rico, Alice C.,Seid, Mehran,Carroll, Georgia L.,Barker, Lynn,Huh, Kay,Langhorne, Mike,Shawar, Ribhi,Kidney, Jolene,Young, Kelly,Anderson, Scott,Desai, Manoj C.,Plattner, Jacob J.
, p. 1730 - 1743 (2007/10/03)
A novel series of C12 vinyl erythromycin derivatives have been discovered which exhibit in vitro and in vivo potency against key respiratory pathogens. The C12 modification involves replacing the natural C 12 methyl group in the erythromycin core with a vinyl group via chemical synthesis. From the C12 vinyl macrolide core, a series of C12 vinyl ketolides was prepared. Several compounds were found to be potent against macrolide-sensitive and -resistant bacteria. The C12 vinyl ketolides 6j and 6k showed a similar antimicrobial spectrum and comparable activity to the commercial ketolide telithromycin. However, the pharmacokinetic profiles of C12 vinyl ketolides 6j and 6k in rats differ from that of telithromycin by having higher lung-to-plasma ratios, larger volumes of distribution, and longer half-lives. These pharmacokinetic differences have a pharmacodynamic effect as both 6j and 6k exhibited better in vivo efficacy than telithromycin in rat lung infection models against Streptococcus pneumoniae and Haemophilus influenzae.
PROCESS FOR THE PREPARATION OF TELITHROMYCIN
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Page/Page column 24, (2008/06/13)
The present invention relates to the process for the preparation of compounds of formula (I) or its pharmaceutically acceptable salts.The novel compounds (i) 10,11-Anhydro-2',4"-di-O-benzoyl-12-O-imidazolylcarbonyl-6-O-methylerythromycin A of formula (Xa) (ii) 2',4"-di-O-benzoyl-11-amino-11-N-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]-11-deoxy-6-O- methylerythromycin A 11,12-cyclic carbamate of formula (XIa) (iii) 2'-O-benzoyl-11-amino-11-N-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]-11-deoxy-5-O-desosaminyl- 6-O-methylerythronolide A 11,12-cyclic carbamate of formula (XIIa) (iv) 2'-benzoyl-11-amino-11-N-[4-[4-(3-pyridyl)imidazol-1-yl]butyl]-11-deoxy-5-O- desosaminyl-6-O-methylerythronolide A 11,12-cyclic carbamate of formula (XIIa) and their use as intermediates in formation of compound of Formula (I). Also the process of preparation of compound of formula (XIIIa).
Synthesis and antibacterial activity of novel bifunctional macrolides
Akritopoulou-Zanze, Irini,Phelan, Kathleen M.,Marron, Thomas G.,Yong, Hong,Ma, Zhenkun,Stone, Greg G.,Daly, Melissa M.,Hensey, Dena M.,Nilius, Angela M.,Djuric, Stevan W.
, p. 3809 - 3813 (2007/10/03)
We report the discovery of a novel class of macrolide antibiotics that have improved antibacterial activity against Ery-resistant organisms.
