Fluoroquinolone Antibiotic Sitafloxacin Intermediate CAS 127199-45-5

Unit Price: USD 1.0000 / Gram
Payment Type: T/T
Incoterm: CIF
Min. Order: 1 Gram
Delivery Time: 15 Days

Basic Info

Model No.: 127199-45-5

Additional Info

Packaging: As Quantity

Productivity: As Order


Transportation: Air

Place of Origin: CHINA

Supply Ability: IN STOCK

Product Description

SITAFLOXACIN intermediate (S)-7-tert-Butoxycarbonylamino-5-azaspiro[2.4]heptane CAS number 127199-45-5, its synthesis ideas are the following: Firstly, synthesis of racemate of (S)-7-tert-Butoxycarbonylamino-5-azaspiro[2.4]heptane, and then split to get a single configuration of compounds, This method creates another waste of chiral compounds. secondly, use 1- (dimethoxymethyl) cyclopropanecarbaldehyde as raw material, the use of cyanide or nitromethane in the process,take a great security risks in the production, inconvenience to enlarge. Thirdly, use 5-chloro-5-azaspiro [2.4] heptan-7-one as the raw material, the use of catalyst reduction process to obtain chiral amine, but the reduction efficiency is not high, ee value is not more than 60%.
The fourth,use beer yeast reduction to get chiral alcohol, and then do mitsunobu reaction to get chiral amine, this method to reduce the volume efficiency is low, amplification is difficult. The last method is use (5-bromoacetyl) cyclopropanecarboxylate with acetic acid and potassium acetate to give the corresponding first step of the intermediate, and then the Noyori hydrogenation reaction is carried out. The corresponding second intermediate is reacted with the ethanol solution of hydrochloric acid to give the corresponding third step of the intermediate, and the third step of the intermediate is reacted with aniline in the presence of cesium carbonate to give the target crude product SITAFLOXACIN intermediate CAS number 127199-45-5

Thera. Category: Antibacterial 

Cas No.: 127199-45-5

Synonyms:  ((5-thiazolyl)methyl)-(4-nitrophenyl)carbonate hydrochloride;carbonic acid 4-nitrophenyl 5-thiazolylmethyl ester hydrochloride;5-THIAZOLYLMETHYL 4-NITROPHENYLCARBONATE, MONOHYDROCHLORIDE;5-(Thiazolyl)methyl 4-nitrobenzoate hydrochloride;4-Nitrophenyl (thiazol-5-ylMethyl) carbonate hydrochloride


NW: 212.2887


Assay: ≥99%

Packing:Export worthy packing

Material Safety Data Sheet:Available on request

Usage: Use to making Sitafloxacin which is a fluoroquinolone antibiotic that shows promise in the treatment of Buruli ulcer. 

Related intermediates:

1) (S)-7-tert-Butoxycarbonylamino-5-azaspiro[2.4]heptane CAS number 127199-45-5

2) Carbamic acid, [(7S)-5-(phenylmethyl)-5-azaspiro[2.4]hept-7-yl]-, 1,1-dimethylethyl ester CAS 144282-37-1 


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