ChemicalBook > CAS DataBase List > (4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid

(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid

Product Name
(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid
CAS No.
203120-17-6
Chemical Name
(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid
Synonyms
Laninamivir;CS-746;R 125489;Lanimivir;Laninamivir-d3;Laninamivir (CS-8958);Laninamivir (Inavir, CS8958, R125489);R-125489,inhibit,Inhibitor,R125489,Influenza Virus,Laninamivir;(4S,5R,6R)-5-AcetaMido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-Methoxypropyl)-5,6-dihydro-4H-pyran-2-;(2R,3R,4S)-3-acetamido-2-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-4-guanidino-3,4-dihydro-2H-pyran-6-carboxylic acid
CBNumber
CB72485059
Molecular Formula
C13H22N4O7
Formula Weight
346.34
MOL File
203120-17-6.mol
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(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid Property

Melting point:
>300°C (dec.)
Density 
1.61
storage temp. 
-20°C Freezer
solubility 
Water (Slightly)
pka
3.81±0.70(Predicted)
form 
Solid
color 
White to Off-White
Water Solubility 
Water : 5 mg/mL (14.44 mM; Need ultrasonic)
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Usbiological
Product number
015457
Product name
Laninamivir
Packaging
500ug
Price
$496
Updated
2021/12/16
TRC
Product number
L174000
Product name
Laninamivir
Packaging
5mg
Price
$1695
Updated
2021/12/16
Usbiological
Product number
293873
Product name
Laninamivir
Packaging
5mg
Price
$2903
Updated
2021/12/16
AK Scientific
Product number
Y0284
Product name
Laninamivir
Packaging
2mg
Price
$1535
Updated
2021/12/16
Biosynth Carbosynth
Product number
ML58733
Product name
Laninamivir
Packaging
5mg
Price
$2100
Updated
2021/12/16
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(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid Chemical Properties,Usage,Production

Description

Laninamivir octanoate (CS-8958), an ester prodrug form of the neuraminidase (NA) inhibitor laninamivir (R-125489), was approved in Japan in 2010 for treatment of influenza virus infections. Laninamivir octanoate is given by intranasal administration at a 20 mg or 40 mg dose. It has a long half-life in humans such that efficacy can be achieved after only a single dose. In addition to vaccines for immunoprophylaxis, antiviral drugs play an essential role in the treatment of influenza virus infections. Two viral proteins have been targeted for therapeutic intervention: the M2 ion channel and NA.

Originator

Sankyo Co., Ltd. (Japan)

Uses

A new potent neuraminidase (NA) inhibitor, shows long-acting anti-influenza virus activity.

Uses

A new potent labelled neuraminidase

Definition

ChEBI: Laninamivir is a member of acetamides.

brand name

Inavir

Synthesis

Laninamivir octanoate is prepared starting from a neuraminic acid precursor. The route from 2,3-didehydroneuramic acid entails a multistep sequence to protect the acid and hydroxyl groups at the 4-, 20-, and 30-positions. Methylation of the remaining 10-hydroxyl by treatment with dimethylsulfate and NaH is followed by conversion of the 4-hydroxyl to an amine Cleavage of the 20,30-dihydroxy protecting group, conversion of the 4- NH2 to the guanidine, and acylation of the 30-OH group afford laninamivir octanoate. This three-step sequence can be reordered such that the guanidine is introduced first, followed by deprotection of the 20,30-diOH groups and acylation. An alternative sequence involves a Boc-protected guanidine intermediate, which is converted in a four-step sequence (deprotection of the acid and 20,30-hydroxyl groups, reprotection of the acid as its diphenylmethyl ether, acylation of the 30-OH and deprotection of the guanidine group) to laninamivir octanoate. Laninamivir can also be synthesized from the a-methyl glycoside of N-acetylneuramic acid methyl ester by an analogous route.

(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid Preparation Products And Raw materials

Raw materials

Preparation Products

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(4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid Suppliers

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203120-17-6, (4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acidRelated Search:


  • (4S,5R,6R)-5-Acetamido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-5,6-dihydro-4H-pyran-2-carboxylic acid
  • Laninamivir
  • (4S,5R,6R)-5-AcetaMido-4-guanidino-6-((1R,2R)-2,3-dihydroxy-1-Methoxypropyl)-5,6-dihydro-4H-pyran-2-
  • R 125489
  • Laninamivir (CS-8958)
  • (2R,3R,4S)-3-acetamido-2-((1R,2R)-2,3-dihydroxy-1-methoxypropyl)-4-guanidino-3,4-dihydro-2H-pyran-6-carboxylic acid
  • Laninamivir-d3
  • CS-746
  • Lanimivir
  • D-glycero-D-galacto-Non-2-enonic acid, 5-(acetylamino)-4-[(aminoiminomethyl)amino]-2,6-anhydro-3,4,5-trideoxy-7-O-methyl-
  • Laninamivir (Inavir, CS8958, R125489)
  • R-125489,inhibit,Inhibitor,R125489,Influenza Virus,Laninamivir
  • 203120-17-6
  • C1213CH22N215N2O7
  • C13H22N4O7
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  • Carbohydrates & Derivatives
  • Intermediates & Fine Chemicals
  • Isotope Labelled Compounds
  • Pharmaceuticals