163253-35-8 Usage
Description
The fluoroquinolone antibacterial agent sitafloxacin hydrate
was developed by Daiichi Sankyo and was approved
and launched last year in Japan. Sitafloxacin’s mode of action
is through inhibition of DNA gyrase and topoisomerase
IV. It is indicated for the treatment of inflammatory infections
such as laryngopharyngitis, adenoiditis, acute bronchitis,
pneumonia, secondary infections due to chronic respiratory
lesions, cystitis, pyelonephritis, urethritis, cervicitis,
otitismedia, sinusitis, periodontitis, and pericoronitis and jaw
inflammation. Due to its broad spectrum of potent antibacterial
activity, sitafloxacin is expected to be clinically effective
in treating severe cases of bacterial infection, relapse/recrudescence of infection and infections in which resistant
bacteria are suspected to be the cause.
Chemical Properties
Off-White Solid
Uses
Different sources of media describe the Uses of 163253-35-8 differently. You can refer to the following data:
1. Sitafloxacin is a new-generation, broad-spectrum oral fluoroquinolone antibiotic.
It is very active against many Gram-positive, Gram-negative and anaerobic clinical isolates, including strains resistant to other fluoroquinolones, was recently approved in
2. Antibacterial
Synthesis
The optically pure fluorocyclopropylamine 111 intermediate
was prepared as described in thescheme. Condensation of
diphenylmethyl amine 104 with acetaldehyde followed by
treatment with trichloromethyl chloroformate in the presence
of triethylamine gave N-vinyl carbamoyl chloride 105 in
53% yield. This intermediate was reacted with sodium benzyloxide
(generated in situ) to afford N-vinylcarbamate 106
in 82% yield. Fluorocyclopropanation of 106 with zinc–
monofluorocarbenoid generated from fluorodiiodomethane
and diethylzinc provided N-(2-fluorocyclopropyl)carbamate
107 in 90% yield and with a diastereomeric ratio of 93:7
favoring the cis-isomer. Hydrogenolysis of the CBz and the
diphenylmethyl groups was accomplished with catalytic 10%
palladium on charcoal and was followed by treatment with
TsOH to afford dl-108 as its tosylate salt. Acylation of dl-
108 TsOH with l-menthyl chloroformate gave a 1:1 mixture
of the diastereomeric carbamate 109 which upon four repeated
recrystallizations from hexane/ethyl acetate afforded
optically pure 110 in 26% yield. Acidic hydrolysis of 110
furnished 111 as its HCl salt in 88% yield.
Check Digit Verification of cas no
The CAS Registry Mumber 163253-35-8 includes 9 digits separated into 3 groups by hyphens. The first part of the number,starting from the left, has 6 digits, 1,6,3,2,5 and 3 respectively; the second part has 2 digits, 3 and 5 respectively.
Calculate Digit Verification of CAS Registry Number 163253-35:
(8*1)+(7*6)+(6*3)+(5*2)+(4*5)+(3*3)+(2*3)+(1*5)=118
118 % 10 = 8
So 163253-35-8 is a valid CAS Registry Number.
InChI:InChI=1/C19H18ClF2N3O3.H2O/c20-14-15-8(17(26)9(18(27)28)5-25(15)12-4-10(12)21)3-11(22)16(14)24-6-13(23)19(7-24)1-2-19;/h3,5,10,12-13H,1-2,4,6-7,23H2,(H,27,28);1H2/t10-,12?,13+;/m0./s1