80715-22-6

Usage

Chemical Properties

Liquid

InChI:InChI=1/C5H5BrO3/c1-3-4(2-6)9-5(7)8-3/h2H2,1H3

Synthetic route

4,5-Dimethyl-1,3-dioxole-2-one (37830-90-3) → 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6)

Conditions	Yield
With N-Bromosuccinimide; 2,2'-azobis(isobutyronitrile) In tetrachloromethane at 85℃; for 16h; Inert atmosphere;	95%
With N-Bromosuccinimide In chloroform Reflux; Large scale;	93.8%
With N-Bromosuccinimide; dibenzoyl peroxide In tetrachloromethane at 77℃; for 6h;	92%

4,5-Dimethyl-1,3-dioxole-2-one (37830-90-3) + a,a-azobisisobutyronitrile (AIBN) → 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6)

Conditions	Yield
With N-Bromosuccinimide In tetrachloromethane	90%

4-chloromethyl-5-methyl-1,3-dioxol-2-one (80841-78-7) → 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6)

Conditions	Yield
With sodium bromide In N,N-dimethyl-formamide at 20℃; for 1h;	75%
With sodium bromide In N,N-dimethyl-formamide at 20℃; for 1h;
With sodium bromide In N,N-dimethyl-formamide at 20℃; for 1.5h;
With sodium bromide In N,N-dimethyl-formamide; acetone at 40 - 45℃; for 5h; Product distribution / selectivity;

4,5-Dimethyl-1,3-dioxole-2-one (37830-90-3) + azobisisobutyronitrile (34241-39-9) → 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6)

Conditions	Yield
With N-Bromosuccinimide In tetrachloromethane	48%
With N-Bromosuccinimide In tetrachloromethane

N-Bromosuccinimide (128-08-5) + 4,5-Dimethyl-1,3-dioxole-2-one (37830-90-3) → 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6)

Conditions	Yield
2,2'-azobis(isobutyronitrile) In benzene at 20℃; for 0.5h; Heating / reflux;

5-[4'-(bromomethyl)[1,1'-biphenyl]-2-yl]-2-(triphenylmethyl)-1H-tetrazole + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate (144689-93-0) → trityl olmesartan medoxomil (144690-92-6)

Conditions	Yield
Stage #1: 5-[4'-(bromomethyl)[1,1'-biphenyl]-2-yl]-2-(triphenylmethyl)-1H-tetrazole; ethyl 4-(2-hydroxypropan-2-yl)-2-propyl-1H-imidazole-5-carboxylate With tert-butylamine hydrobromide; potassium carbonate In acetone at 0 - 55℃; for 32h; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one With potassium carbonate; potassium iodide In acetone at 20 - 55℃; for 3h;	98.5%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + ulifloxacin (112984-60-8) → prulifloxacin (123447-62-1)

Conditions	Yield
With potassium hydrogencarbonate In N,N-dimethyl-formamide at 0℃; for 5h; Large scale;	95.4%
With potassium hydrogencarbonate In N,N-dimethyl-formamide for 5h; Ambient temperature;	62%
Stage #1: ulifloxacin With potassium hydrogencarbonate In acetonitrile at 25 - 30℃; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one at 15 - 30℃; for 27 - 28.25h;
Stage #1: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one; ulifloxacin With potassium hydrogencarbonate In N,N-dimethyl-formamide at 0 - 28℃; for 3 - 4h; Stage #2: With hydrogenchloride In chloroform; water for 0.25h; pH=0.8 - 1.0;
Stage #1: ulifloxacin With N-ethyl-N,N-diisopropylamine In acetonitrile at 20℃; for 0.166667h; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one In acetonitrile at 10 - 30℃; for 21h; Product distribution / selectivity;

(2S,3S)-3-((2-(2-chloro-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)-5-fluoro-6-(thiophen-2-yl)pyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylic acid + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → (2S,3S)-(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl 3-((2-(2-chloro-5-trityl-5H-pyrrolo[2,3-b]pyrazin-7-yl)-5-fluoro-6-(thiophen-2-yl)pyrimidin-4-yl)amino)bicyclo[2.2.2]octane-2-carboxylate

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 20℃;	95%

carbon dioxide (124-38-9) + L-phenylalanine (63-91-2) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → (S)-2-(5-Methyl-2-oxo-[1,3]dioxol-4-ylmethoxycarbonylamino)-3-phenyl-propionic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester

Conditions	Yield
With caesium carbonate In N,N-dimethyl-formamide Ambient temperature;	94%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl iodide (80841-79-8)

Conditions	Yield
With potassium iodide In acetone Ambient temperature;	92%

carbon dioxide (124-38-9) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + benzyl-methyl-amine (103-67-3) → Benzyl-methyl-carbamic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester

Conditions	Yield
With caesium carbonate In N,N-dimethyl-formamide Ambient temperature;	90%

2-(6-(4-(2-(tert-butyldimethylsilyloxy)ethyl)piperazin-1-yl)-2-methylpyrimidin-4-ylamino)-N-(2-chloro-6-methylphenyl)thiazole-5-carboxamide (881381-50-6) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → C33H44ClN7O5SSi (881381-64-2)

Conditions	Yield
With caesium carbonate In N,N-dimethyl-formamide at 20℃;	89%

6α,9α-difluoro-11β-hydroxy-16α,17α-isopropylidenedioxy-3-oxo-androsta-1,4-diene-17β-carbothioic acid (80474-38-0) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → 6α,9α-Difluoro-11β-hydroxy-16α,17α-isopropylidenedioxy-3-oxo-androsta-1,4-diene-17β-carbothioic acid S-(5-methyl-2-oxo-1,3-dioxol4-ylmethyl) ester

Conditions	Yield
With potassium carbonate In water; ethyl acetate; N,N-dimethyl-formamide	85%

4-(1-methoxy-1-methylethyl)-2-propyl-1-{4-(2-trityltetrazol-5-yl)phenyl}phenylmethylimidazole-5-carboxylic acid (1040405-55-7) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → 4-(1-methoxy-1-methylethyl)-2-propyl-1-{4-(2-trityltetrazol-5-yl)phenyl}phenylmethylimidazole-5-carboxylic acid-5-methyl-2-oxo-[1,3]-dioxolene-4-yl-methyl ester (1040405-56-8)

Conditions	Yield
With potassium carbonate In N,N-dimethyl acetamide at 20℃; for 5h;	84%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + azilsartan (147403-03-0) → C35H28N4O11

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 60℃; for 6h;	83%

formic acid (64-18-6) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → 4-formyloxymethyl-5-methyl-1,3-dioxolen-2-one (91526-17-9)

Conditions	Yield
With trimethylamine In acetonitrile at 20℃; for 1h;	82%
With triethylamine In acetonitrile for 1h; Ambient temperature;	80%
With triethylamine In acetonitrile for 2h; Ambient temperature;

3-[[(1S)-1-(dimethylcarbamoyl)propyl]-(trans-4-methylcyclohexanecarbonyl)amino]-5-(3-methylbut-1-ynyl)thiophene-2-carboxylic acid + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → C30H40N2O7S

Conditions	Yield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.333333h; Microwave irradiation;	78%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + methyl 2-ethoxy-1-((2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]-imidazole-7-carboxylate (147403-52-9) → C31H26N4O8

Conditions	Yield
Stage #1: methyl 2-ethoxy-1-((2′-(5-oxo-4,5-dihydro-1,2,4-oxadiazol-3-yl)biphenyl-4-yl)methyl)-1H-benzo[d]-imidazole-7-carboxylate With potassium carbonate In N,N-dimethyl-formamide at -10 - 0℃; for 0.5h; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one In N,N-dimethyl-formamide at 20℃;	77.5%

5-(3,3-dimethylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-(2-oxo-2-thiomorpholino-ethyl)amino]thiophene-2-carboxylic acid + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → C30H38N2O8S

Conditions	Yield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.416667h; Microwave irradiation;	75%

5-(3-methylbut-1-ynyl)-3-[(trans-4-methylcyclohexanecarbonyl)-[(1S)-1-(morpholine-4-carbonyl)propyl]amino]thiophene-2-carboxylic acid. + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → C32H42N2O8S

Conditions	Yield
With potassium carbonate; sodium iodide In N,N-dimethyl-formamide at 80℃; for 0.333333h; Microwave irradiation;	74%

C28H40NO2P + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → C33H45BrNO5P

Conditions	Yield
In toluene at 130℃; for 21h; Inert atmosphere; Schlenk technique;	74%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + prulifloxacin (123447-62-1) → 6-Fluoro-1-methyl-7-[4-(5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl)-piperazin-1-yl]-4-oxo-4H-2-thia-8b-aza-cyclobuta[a]naphthalene-3-carboxylic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 39.9℃; for 3h;	72%
With N-ethyl-N,N-diisopropylamine In N,N-dimethyl-formamide at 24.9℃; Rate constant; also in presence of DIPA and TNBA, var concn. of DMDO-Br and amines;

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + (S)-3-(((tert-butoxycarbonyl)amino)methyl)-5-methylhexanoic acid (649748-09-4) → (S)-3-(tert-butoxycarbonylamino-methyl)-5-methyl-hexanoic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester (1026789-40-1)

Conditions	Yield
Stage #1: (S)-3-(((tert-butoxycarbonyl)amino)methyl)-5-methylhexanoic acid With caesium carbonate In methanol at 20℃; for 2h; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one In ISOPROPYLAMIDE	72%
Stage #1: (S)-3-(((tert-butoxycarbonyl)amino)methyl)-5-methylhexanoic acid With caesium carbonate In methanol at 20℃; for 2h; Stage #2: 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one In N,N-dimethyl acetamide	72%

carbon dioxide (124-38-9) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + benzylamine (100-46-9) → Benzyl-carbamic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester

Conditions	Yield
With caesium carbonate In N,N-dimethyl-formamide Ambient temperature;	70%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + N-benzyloxycarbonyl NFLX (105439-94-9) → N-benzyloxycarbonyl NFLX (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester (105439-93-8)

Conditions	Yield
With potassium carbonate In acetonitrile at 60℃;	69%

5-Propyl-azepane-2-carboxylic acid [2-chloro-1-(3,4,5-trihydroxy-6-methylsulfanyl-tetrahydro-pyran-2-yl)-propyl]-amide + 4-(dicyanomethylene)-2-methyl-6-(p-dimethylaminostyryl)-4H-pyran (96042-30-7) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → 1-(5-Methyl-2-oxo-[1,3]dioxol-4-ylmethyl)-5-propyl-azepane-2-carboxylic acid [2-chloro-1-(3,4,5-trihydroxy-6-methylsulfanyl-tetrahydro-pyran-2-yl)-propyl]-amide

Conditions	Yield
With potassium hydrogencarbonate In methanol; N,N-dimethyl-formamide	68%

tert-butyl 2-(methylamino)ethylcarbamate (122734-32-1) + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) → tert-butyl (2-(methyl((5-methyl-2-oxo-1,3-dioxol-4-yl)methyl)amino)ethyl)carbamate

Conditions	Yield
With potassium carbonate In N,N-dimethyl-formamide at 20℃; for 16h;	67.4%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + ethyl 6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-(1,3)thiazeto(3,2-a)quinoline-3-carboxylate (113028-17-4) → ethyl 6-fluoro-1-methyl-7-<4-<(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl>-1-piperazyl>-4-oxo-4H-<1,3>thiazeto<3,2-a>-quinoline-3-carboxylate

Conditions	Yield
With potassium hydrogencarbonate In N,N-dimethyl-formamide for 1h; Ambient temperature;	66%
With potassium hydrogencarbonate In N,N-dimethyl-formamide

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid (70458-96-7) → N-<(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl>norfloxacin (85195-76-2)

Conditions	Yield
With potassium hydrogencarbonate In N,N-dimethyl-formamide for 5h;	66%

potassium bicarbonate + 4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + 1-ethyl-6-fluoro-1,4-dihydro-4-oxo-7-(1-piperazinyl)-3-quinoline carboxylic acid (70458-96-7) → N-<(5-Methyl-2-oxo-1,3-dioxol-4-yl)methyl>norfloxacin (85195-76-2)

Conditions	Yield
In N-methyl-acetamide; water	66%

4-bromomethyl-1,3-dioxa-5-methylcyclopentene-2-one (80715-22-6) + (-)-6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)-4H-<1,3>thiazeto<3,2-a>quinoline-3-carboxylic acid → S-(-)-6-fluoro-1-methyl-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylic acid (1235993-71-1)

Conditions	Yield
With triethylamine In N,N-dimethyl-formamide at -5 - 5℃; for 3h; Product distribution / selectivity;	63%

Upstream product

• 128-08-5 N-Bromosuccinimide 
• 37830-90-3 4,5-Dimethyl-1,3-dioxole-2-one 
• 34241-39-9 azobisisobutyronitrile 
• 80841-78-7 4-chloromethyl-5-methyl-1,3-dioxol-2-one 

Downstream Products

• 91526-17-9 4-formyloxymethyl-5-methyl-1,3-dioxolen-2-one 
• 86005-08-5 (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl (S)-N-(tert-butoxycarbonyl)-3-hydroxy-α-methyltyrosinate 
• 105439-93-8 N-benzyloxycarbonyl NFLX (5-methyl-2-oxo-1,3-dioxol-4-yl)methyl ester 
• 123447-62-1 prulifloxacin 
• 156834-57-0 6-fluoro-1-methyl-4-oxo-7-<4-<(2-oxo-1-methylenepropyl)oxycarbonyl>-1-piperazinyl>-4H-<1,3>thiazeto<3,2-a>quinoline-3-carboxylic acid 
• 210988-85-5 2-Butyl-5-[methyl-(3-methyl-but-2-enoyl)-amino]-3-[2'-(1-trityl-1H-tetrazol-5-yl)-biphenyl-4-ylmethyl]-3H-imidazole-4-carboxylic acid 5-methyl-2-oxo-[1,3]dioxol-4-ylmethyl ester 
• 524070-84-6 (5-methyl-2-oxo-1,3-dioxol-4-yl)-methyl (5R,6S)-6-[(1R)-1-hydroxyethyl]-3-[3-(hydroxymethyl)-phenyl]-7-oxo-1-azabicyclo[3.2.0]hept-2-ene-2-carboxylate 
• 278793-42-3 C₂₇H₁₇Cl₃N₄O₇S 
• 881381-64-2 C₃₃H₄₄ClN₇O₅SSi 
• 859212-41-2 4-{4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-ylmethyl}-3-trifluoromethyl-N-{4-methyl-3-[4-(5-pyrimidinyl)pyrimidin-2-ylamino]phenyl}benzamide 
• 91526-18-0 4-hydroxymethyl-5-methyl-[1,3]dioxol-2-one 
• 123447-66-5 ethyl 6-fluoro-7-[4-(5-methyl-2-oxo-1,3-dioxolen-4-yl)methyl-1-piperazinyl]-4-oxo-1-phenyl-4H-[1,3]thiazeto[3,2-a]quinoline-3-carboxylate 

Relevant academic research and scientific papers

MONOETHYLENICALLY UNSATURATED MONOMERS AND USES THEREOF

The invention relates to a monoethylenically unsaturated monomer of formula (I), and to the use thereof for producing a polymer. The invention also relates to the polymer obtained by polymerising said monomer, and to the use thereof in a composition for producing coatings.

SSTR5 ANTAGONISTS

This disclosure is directed, at least in part, to SSTR5 antagonists useful for the treatment of conditions or disorders involving the gut-brain axis. In some embodiments, the SSTR5 antagonists are gut-restricted compounds. In some embodiments, the condition or disorder is a metabolic disorder, such as diabetes, obesity, nonalcoholic steatohepatitis (NASH), or a nutritional disorder such as short bowel syndrome.

Method for catalytically synthesizing 4-bromomethyl-5-methyl-1, 3-dioxole-2-ketone through cooperation of microwaves and ionic liquid

The invention relates to the technical field of organic synthesis, in particular to a method for catalytically synthesizing 4-bromomethyl-5-methyl-1, 3-dioxole-2-ketone through cooperation of microwaves and ionic liquid. The preparation method comprises the following steps: adding 4, 5-dimethyl-1, 3-dioxole-2-ketone as a raw material into an organic solvent, and adding bromine under the effect of an ionic liquid catalyst and microwave radiation to carry out bromination reaction; and carrying out reduced pressure distillation on the obtained reaction liquid, and rectifying to obtain the 4-bromomethyl-5-methyl-1, 3-dioxole-2-ketone. Under the combined action of the ionic liquid catalyst and microwave radiation, polarization of bromine is accelerated, the problem of low selectivity of bromine is solved, generation of polybrominated substances is avoided, and the yield and purity of the product are improved; and the production process is simplified, the reaction conditions are mild, the adopted lewis acidic ionic liquid can be recycled, use of a high-price bromination reagent is avoided, the production cost is reduced, and industrial production is facilitated.

Modulators of ROR-gamma Receptors, Composition and Use Thereof

The present invention provides novel methods to treat disease by modulating retinoid-related orphan receptor gamma (ROR-gamma) in vitro and in vivo with ursolic acid analogs, and compositions thereof. The methods and compounds disclosed herein are useful for inhibiting the differentiation of a population of T cells, or treating a disease related to Th17 cell responses in a subject. Examples of such diseases include, but are not limited to, autoimmune diseases, multiple sclerosis, rheumatoid arthritis, psoriasis and diabetes.

A method for preparing of plurichari (by machine translation)

The invention relates to a prepration method of a compound prulifloxacin as shown in the formula (I), wherein the chemical name of prulifloxacin is 6-floro-1-methyl-7-[4-(5-methyl-2-oxo1,3-dioxo hetercyclopentene-4-yl)methyl-1-piperazinyl-4-oxo-4H-[1,3] thiaazacyclobutane[3,2-a] quinoline-3-carboxylic acid. The preparation method provided by the invention is a preparation method of prulifloxacin suitable for industrialized production, simple in process, high in purity and high in yield.

BISARYLSULFONAMIDES USEFUL IN THE TREATMENT OF INFLAMMATION AND CANCER

A compound of formula (I), useful for the treatment of cancer, inflammation and inflammatory disorders, and a pharmaceutical composition containing the compound.

N-SUBSTITUTED-CYCLIC AMINO DERIVATIVE

The present invention provides a compound of formula (I): wherein R1a is optionally substituted C1-6 alkyl, etc.; R1m is hydrogen atom, etc.; G1, G2, G3 and G4 are (i), etc. ((i) G1 is -N(R1b)-, G2 is -CO-, G3 is -C(R1c)(R1d)-, and G4 is oxygen, etc.); R1b is optionally substituted C1-6 alkyl, etc.; R1c and R1d are each independently optionally substituted C1-6 alkyl, etc.; R2 is optionally substituted C1-6 alkyl, etc.; R3a, R3b, R3c, and R3d are each independently a group: -A-B (A is a single bond, etc., B is hydrogen atom, etc.), etc.; n is 1, etc.; R5 is C1-4 alkoxycarbonyl, etc., or a pharmaceutically acceptable salt thereof, which is useful as a renin inhibitor.

CRYSTALLINE FORM OF PRULIFLOXACIN AND PROCESSES FOR ITS PREPARATION

The present invention relates to a crystalline polymorphic form of 6-fluoro-1-methyl-7- {4-[(5-methyl-2-oxo-1,3-dioxol-4-yl)methyl]piperazin-1-yl}-4-oxo-4H-[1,3]-thiazeto-[3,2- a]-quinoline-3-carboxylic acid (prulifloxacin). More specifically, the invention relates to a crystalline form of prulifloxacin (herein referred to as Form A), and a method for preparing the crystalline Form A. The present invention further provides a pharmaceutical formulation comprising the novel form of prulifloxacin.

SUBSTITUTED QUINOLINES FOR USE AS VEGF INHIBITORS

A compound of formula (I), as well as pharmaceutically acceptable salts thereof and pharmaceutical compositions comprising a therapeutically effective amount of the compounds. The compound is useful in treatment of cancer, diabetic retinopathy, age-related macular degeneration, inflammation, stroke, ischemic myocardium, atherosclerosis, macular edema and psoriasis.

PROCESS FOR THE PREPARATION OF HIGHLY PURE PRULIFLOXACIN

The present invention provides an industrially advantageous process for the preparation of highly pure prulifloxacin of formula I and its pharmaceutically acceptable salts. The present i innvention a also provides a novel process for the purification of prulifloxacin acid addition salt.