Aspoxicillin | 63358-49-6

Aspoxicillin Properties

Melting point	195-198° (dec)
Boiling point	985.1±65.0 °C(Predicted)
Density	1.51±0.1 g/cm3(Predicted)
storage temp.	2-8°C
solubility	DMSO (Slightly, Sonicated), Methanol (Slightly)
pka	2.44±0.50(Predicted)
color	White to Off-White
Water Solubility	Water : 25 mg/mL (50.66 mM; Need ultrasonic)
Stability	Hygroscopic
CAS DataBase Reference	63358-49-6
FDA UNII	0745KNO26J
ATC code	J01CA19

SAFETY

Risk and Safety Statements

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H315-H319-H335
Precautionary statements	P261-P305+P351+P338
Hazard Codes	Xi
Risk Statements	36/37/38
Safety Statements	26
WGK Germany	3
RTECS	MB7548000

Aspoxicillin price More Price(9)

Manufacturer	Product number	Product description	CAS number	Packaging	Price	Updated	Buy
TRC	A788675	Aspoxicillin(~80%)	63358-49-6	50mg	$210	2021-12-16	Buy
Biosynth Carbosynth	FA167401	Aspoxicillin	63358-49-6	5mg	$250	2021-12-16	Buy
Biosynth Carbosynth	FA167401	Aspoxicillin	63358-49-6	10mg	$300	2021-12-16	Buy
Biosynth Carbosynth	FA167401	Aspoxicillin	63358-49-6	25mg	$350	2021-12-16	Buy
AK Scientific	C991	Aspoxicillin	63358-49-6	5mg	$387	2021-12-16	Buy

Product number	Packaging	Price	Buy
A788675	50mg	$210	Buy
FA167401	5mg	$250	Buy
FA167401	10mg	$300	Buy
FA167401	25mg	$350	Buy
C991	5mg	$387	Buy

Aspoxicillin Chemical Properties,Uses,Production

Description

Aspoxicillin is an injectable, amino acid-type penicillin highly active against Gram-positive and Gram-negative bacteria, including the β-lactamase producing Bacillus frugilis. It is reportedly effective in the treatment of peritonitis, pneumonia and bronchitis.

Originator

Tanabe (Japan)

Uses

Aspoxicillin is a broad-spectrum antibiotic.

Definition

ChEBI: Aspoxicillin is a peptide.

Manufacturing Process

1). 3 g (23.6 millimoles) of D-2-amino-3-N-methylcarbamoyl-propionic acid hydrochloride (D-N'-methylasparagine HCl), 4.5 g of benzyloxycarbonyl chloride, 30 g of water, 30 ml of tetrahydrofuran and 12 g of potassium carbonate are mixed at 5° to 10°C. Then, the mixture is stirred at the same temperature for 2 hours. During the reaction, the mixture is kept at a slightly alkaline pH (pH 8) with potassium carbonate. 10 ml of water are added to the reaction mixture, and insoluble materials are filtered off. The filtrate is washed twice with ethyl acetate, acidified with citric acid and then extracted three times with 50 ml of ethyl acetate. The ethyl acetate extracts are washed with water, dried and evaporated to remove solvent. 5.1 g of D-2- benzyloxycarbonylamino-3-N-methylcarbamoyl-propionic acid are obtained. MP: 142°-143°C.
2). 2.8 g (10 millimoles) of D-2-benzyloxycarbonylamino-3-Nmethylcarbamoyl- propionic acid, 2.27 g of dicyclohexylcarbodiimide, 1.27 g of N-hydroxysuccinimide and 120 ml of tetrahydrofuran are mixed at 0° to 5°C, and the mixture is stirred at the same temperature for 16 hours. Insoluble materials are filtered off. Then, the filtrate is evaporated at 20°C under reduced pressure to remove the solvent, and the crystalline precipitates thus obtained are washed with a mixture of benzene-ether. 2.6 g of N-(D-2- benzyloxycarbonylamino-3-N-methylcarbamoyl-propionyloxy)succinimide are obtained. MP: 132°-134°C.
3). 3.75 g of N-(D-2-benzyloxycarbonylamino-3-Nmethylcarbamoylpropionyloxy) succinimide are dissolved in 50 ml of tetrahydrofuran. 12.5 ml of an aqueous 1 N-sodium hydroxide solution containing 2.3 g of p-hydroxy-D-phenylglycine are added to the solution. The mixture is stirred at room temperature for 24 hours. 20 ml of ethyl acetate and 20 ml of water are added to the reaction mixture, and said mixture is shaken. Then, the aqueous layer is separated, adjusted to pH 3 with citric acid and extracted with a mixture of 20 ml of tetrahydrofuran and 10 ml of ethyl acetate. The extract is washed with water, dried and evaporated to remove solvent. The residue thus obtained is washed with ether. 3.0 g of D-2-(D-2- benzyloxycarbonylamino-3-N-methylcarbamoylpropionamido)- 2-phydroxyphenylacetic acid are obtained as colorless crystalline powder. MP: 154°-156°C(decomp.).
4). 429 mg of D-2-(D-2-benzyloxycarbonylamino-3-Nmethylcarbamoylpropionamido)- 2-p-hydroxyphenylacetic acid and 382 mg of 6-aminopenicillanic acid triethylamine salt are dissolved in 10 ml of dimethylformamide. 303 mg of diphenylphosphoric azide [N3PO(OC6H5)2] and 110 mg of triethylamine are added to the solution at -5°C, and the mixture is stirred at -5°C for 15 hours. After the reaction, the mixture is adjusted to pH 3 with an aqueous 5% citric acid solution and extracted with a mixture of 15 ml of tetrahydrofuran and 10 ml of ethyl acetate. The extract is washed with water, dried and then evaporated at below 40°C to remove the solvent. Ether is added to the residue obtained, and precipitates are collected by filtration. 509 mg of 6-[D-2-(D-2-benzyloxycarbonylamino-3-Nmethylcarbamoylpropionamido)- 2-p-hydroxyphenylacetamido]penicillanic acid are obtained as a colorless powder.
5). 627 mg of 6-[D-2-(D-2-benzyloxycarbonylamino-3-N-methylcarbamoylpropionamido)- 2-p-hydroxyphenylacetamido]penicillanic acid and 400 mg of 30% palladium-BaCO3 are suspended in 10 ml of methanol. The suspension is shaken at room temperature for 30 minutes. Said shaking step is carried out in a hydrogen gas atmosphere under atmospheric pressure. After the reaction is completed, the catalysts are removed by filtration. The filtrate is evaporated at below 40°C to remove the solvent, and ether is added to the residue. Then, a colorless crystalline powder is collected by filtration and washed with tetrahydrofuran. 443 mg of 6-[D-2-(D-2-amino-3-N-methylcarbamoylpropionamido)- 2-p-hydroxyphenylacetamido]penicillanic acid are obtained. MP: 198°-201°C(decomp.).

brand name

Doyle

Therapeutic Function

Antibiotic

Antimicrobial activity

An acylaminopenicillin, synthesized from amoxicillin. It is more active than carbenicillin against Ps. aeruginosa and is less active than piperacillin against Staph. aureus, H. influenzae, the Enterobacteriaceae and Ps. aeruginosa. It is not absorbed when dosed orally; the plasma half-life is 87 min after intravenous infusion.
Aspoxicillin has been used in the treatment of respiratory, skin and soft tissue and urinary infections in adults and children, and, in combination with aminoglycosides, against gynecological infections and infections in patients with hematological disorders.

Aspoxicillin Preparation Products And Raw materials

Raw materials

N-Hydroxysuccinimide Amoxicillin 3-Nitrobenzenesulfonyl chloride Thioacetamide Activ Ester

Citric acid Dicyclohexylcarbodiimide 4-Hydroxy-D-(-)-2-phenylglycine Benzyl chloroformate Triethylamine

6-Aminopenicillanic acid PALLADIUM ON STRONTIUM CARBONATE, REDUCED

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Preparation Products

Aspoxicillin Suppliers

Global( 85)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
career henan chemical co	+86-0371-86658258	sales@coreychem.com	China	29914	58
Hubei xin bonus chemical co. LTD	86-13657291602	linda@hubeijusheng.com	CHINA	22968	58
BOC Sciences	+1-631-485-4226	inquiry@bocsci.com	United States	19553	58
Chongqing Chemdad Co., Ltd	+86-023-61398051 +8613650506873	sales@chemdad.com	China	39916	58
CONIER CHEM AND PHARMA LIMITED	+8618523575427	sales@conier.com	China	49390	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-81138252 +86-18789408387	1057@dideu.com	China	3537	58
SIMAGCHEM CORP	+86-13806087780	sale@simagchem.com	China	17367	58
TargetMol Chemicals Inc.	+1-781-999-5354 +1-00000000000	marketing@targetmol.com	United States	19892	58
Hefei TNJ Chemical Industry Co.,Ltd.	0551-65418671	sales@tnjchem.com	China	34572	58
Shaanxi Dideu Medichem Co. Ltd	+86-029-89586680 +86-18192503167	1026@dideu.com	China	9320	58

Supplier	Advantage
career henan chemical co	58
Hubei xin bonus chemical co. LTD	58
BOC Sciences	58
Chongqing Chemdad Co., Ltd	58
CONIER CHEM AND PHARMA LIMITED	58
Shaanxi Dideu Medichem Co. Ltd	58
SIMAGCHEM CORP	58
TargetMol Chemicals Inc.	58
Hefei TNJ Chemical Industry Co.,Ltd.	58
Shaanxi Dideu Medichem Co. Ltd	58

View Lastest Price from Aspoxicillin manufacturers

Image	Update time	Product	Price	Min. Order	Purity	Supply Ability	Manufacturer
	2020-05-12	Aspoxicillin 63358-49-6	US $1.00 / KG	1KG	99%	20T	Shaanxi Dideu Medichem Co. Ltd
	2019-08-08	Aspoxicillin 63358-49-6	US $3.00 / KG	1KG	99%	100kg	Career Henan Chemical Co

Aspoxicillin
63358-49-6
US $1.00 / KG
99%
Shaanxi Dideu Medichem Co. Ltd

Aspoxicillin
63358-49-6
US $3.00 / KG
99%
Career Henan Chemical Co

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TRIS(2-AMINOETHYL)AMINE D-ASPARTIC ACID ALPHA-AMIDE HYDROCHLORIDE 4-DIISOPROPYLAMINO-1-BUTANOL

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ASPOXICILLIN (2s,5r,6r)-6-[(2r)-2-[(2r)-2-amino-3-(n-methylcarbamoyl)-propionamido]-2-(p-hydroxyphenyl)acetamido]-3,3-dimehtyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid trihydrate glycinamide,n-methyl-d-asparaginyl-n-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-a n(sup4)-methyl-d-asparagininylamoxicillin zabicyclo(3.2.0)hept-6-yl)-d-2-(4-hydroxyphenyl)-,(2s-(2-alpha,5-alpha,6-beta) Aspoxicilin Doyle Glycinamide, N-methyl-D-asparaginyl-N-(2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl)-D-2-(4-hydroxyphenyl)-, [2S-(2a,5a,6b)]- Glycinamide, N-methyl-D-asparaginyl-N-[(2S,5R,6R)-2-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6-yl]-2-(4-hydroxyphenyl)-, (2R)- TA 058 ASPOXICILLIN 3-HYDRATE ASPC DOYE (2S，5R，6R)-6-[(2R)-2-[(2R)-2-Amino-3-(methylearbamoyl)propionamido]-2-(ρ-hydroxyphenyl)acetamido]-3，3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid (2S,5R,6R)-6α-[[(R)-[[(2R)-2-Amino-4-(methylamino)-1,4-dioxobutyl]amino](4-hydroxyphenyl)acetyl]amino]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2β-carboxylic acid 6α-[(R)-2-(4-Hydroxyphenyl)-2-[[(2R)-3-(methylcarbamoyl)-2-aminopropanoyl]amino]acetylamino]penicillanic acid N4-Methyl-D-Asn-4-hydroxy-D-phenyl Gly-N-[(2S,5β)-2β-carboxy-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]hept-6α-yl]-NH2 N4-Methyl-D-aspariginylamoxicillin Aspoxicillin USP/EP/BP Aspoxicillin (~80%) Benzenemethanamine,N-2-propen-6-yl- Aspoxicillin,inhibit,pleuropneumoniae,Inhibitor,penicillin,Actinobacillus,antimicrobial,Bacterial 63358-49-6 91878-06-9 C21H27N5O7S C21H27N5O7S3H2O AR to AZAntibiotics A Alphabetic Chemical Structure Chromatography OthersAnalytical Standards Pharmacology Standards