cas 1056039-83-8, 2-(2-Methyl-2H-tetrazol-5-yl)-5-(4,4,5,5-tetraMethyl-1,3,2-dioxaborolan-2-yl)pyridine

Articles about 1056039-83-8Total 11 be found

An improved efficient synthesis of the antibacterial agent torezolid
An improved and efficient method for the preparation of torezolid based on Suzuki cross-coupling reaction as the key step was developed on a gram scale in five steps. The total yield was 44% and the optical purity of torezolid by the improved method was above 99%.
Li, Gang,Yuan, Bao-Kun,Tang, Wu,Zhao, Hong-Yi,Lin, Zi-Yun,Huang, Hai-Hong
p. 143 - 146
(2015)
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Preparation method of tedizolid phosphate
The invention discloses a preparation method of tedizolid phosphate, and belongs to the technical field of medicines. The preparation method of tedizolid phosphate comprises the following steps: 1, synthesizing a compound IV; 2, synthesizing a compound II
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Paragraph 0027; 0108; 0112; 0113

(2021/03/18)

Preparation method of high-purity tedizolid phosphate
The invention discloses a preparation method of high-purity tedizolid phosphate. The preparation method comprises the following steps: 1, with 2-methyl-5-(5-bromopyridin-2-yl)tetrazole as a starting material and tetrakis(triphenylphosphine)palladium (Pd(PPh3)4) as a catalyst, and reacting the starting material and the catalyst with bis(pinacolato)diboron to generate a compound as shown in a formula 1, namely bromine-converted pinacol borate; 2, subjecting a compound shown in a formula 3 and (5R)-3-(4-bromo-3-fluorophenyl)-5-(hydroxymethyl)oxazolidin-2-one to Suzuki coupling under the catalyticaction of tetrakis(triphenylphosphine)palladium (Pd(PPh3)4) to obtain (R)-3-[4-[2-(2-methyltetrazol-5-yl)pyridin-5-yl]-3-fluorophenyl]-5-one; and 3, preparing tedizolid phosphate from a compound as shown in a formula 5 under the condition of phosphorylation of phosphorus oxychloride.
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Paragraph 0020

(2020/05/30)

One-pot synthesized tedizolid
The invention relates to a preparation method of tedizolid indicated in the formula I. The preparation method includes: taking 5-bromine-2-(2-methyl-2H-tetrazole-5-radical) pyridine indicated in the formula II as a raw material to be reacted with boric acid indicated in the formula III to obtain 2-(2-methyl-2H-tetrazole-5-radical)-5-(4,4,5,5-tetramethyl-1,3-dioxane-2-radical) pyridine indicated in the formula IV under the action of a palladium catalyst; allowing compound without separation to be directly in Suzuki coupling reaction with (5R)-3-(4-bromine-3-fluorophenyl)-5-hydroxymethyl oxazolane-2-ketone indicated in the formula V under the action of the palladium catalyst to obtain the tedizolid indicated in the formula I. The preparation method of the one-pot synthesized tedizolid is easy in obtaining of the raw materials, simple in production process, short in production cycle, less in discharge of three wastes (waste gas, waste water and industrial residue), and a one-pot method is high in yield and has great practical value.
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Paragraph 0007; 0014; 0015; 0016; 0117; 0018; 0019-0022

(2018/03/01)

Copper Catalyzed Assembly of N-Aryloxazolidinones: Synthesis of Linezolid, Tedizolid, and Rivaroxaban
The total synthesis of oxazolidinone-based pharmaceuticals, linezolid, tedizolid and rivaroxaban is reported. They are synthesized using a recently reported copper-catalyzed one-pot cyclization and arylation as the key step to construct the N-aryloxazolidinone core. Active pharmaceutical ingredients (API) were synthesized from a common synthetic pool of a simple protected amino alcohol in 22 %, 61 % and 40 % total synthesis yields, respectively.
Mahy, William,Leitch, Jamie A.,Frost, Christopher G.
p. 1305 - 1313
(2016/03/19)

New synthesis process of oxazolinone antibiotic
According to the method of the present invention, a methyl tetrazole pyridine bromide (2) and pinacol diboron are subjected to a reaction under catalysis of a transition metal to obtain a boronic acid pinacol ester (3), the compound (3) is separated or is not separated, and the separated compound (3) or the un-separated compound (3) and Cbz-protected bromobenzene (4) are subjected to a reaction under catalysis of a transition metal to obtain a key intermediate (1) of tedizolid. According to the present invention, the compound (3) is not subjected to separation purification, and reacts with the compound (4) in a kettle to generate the compound (1).
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Paragraph 0034; 0035; 0036

(2016/10/08)

ANTIMICROBIAL INDOLINE COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
The present invention provides indoline heterocyclic compounds of the following formula I: or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods f
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Page/Page column 21-22

(2010/04/23)

Methods and Processes For Syntheses and Manufacture of Antimicrobial 1(Ortho-Fluorophenyl)dihydropyridones
Provided herein are methods and processes for synthesis and manufacture of compounds of formula I: or its crystal forms, pharmaceutical acceptable salts, prodrugs, hydrates, or solvates thereof.
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Page/Page column 31

(2010/08/18)

Antimicrobial ortho-Fluorophenyl Oxazolidinones For Treatment of Bacterial Infections
The present invention provides certain ortho-fluorophenyl oxazolidinones of the following formula I: or pharmaceutically acceptable salts or prodrugs thereof that are antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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Page/Page column 31

(2009/03/07)

ANTIBACTERIAL CONDENSED THIAZOLES
Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk - is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (-0-), thioether (-S-) or amino (-NR)- link, wherein R is hydrogen, -CN or C1-C3 alky!; X is -C(=O)NR6-, or -C(=O)O- wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is -N= or -CH= Z2 is -N= or -C(R1)=; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkOXy or (C1-C2)alkylthio, nitro, or nitrile (-CN); R2 is a group Q1 -[Alk1]q-Q2 -, wherein q is 0 or 1; AIkl is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (-O-), thioether (-S-) or amino (-NR)- link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms
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Page/Page column 41

(2009/07/17)

ANTIMICROBIAL HETEROCYCLIC COMPOUNDS FOR TREATMENT OF BACTERIAL INFECTIONS
The present invention provides heterocyclic compounds of the following formula (I) : or pharmaceutically acceptable salts, prodrugs, solvates, or hydrates thereof useful as antibacterial agents, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.
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(2008/12/08)