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Home > Products >  intermediate of Dolutegravir 1335210-34-8

intermediate of Dolutegravir 1335210-34-8 CAS NO.1335210-34-8

  • Min.Order: 1 Kilogram
  • Payment Terms: L/C,T/T,Other
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  • Product Details

Keywords

  • (4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid
  • Dolutegravir
  • 1335210-34-8

Quick Details

  • ProName: 4R,12aS-7-Methoxy-4-Methyl-6,8-dioxo-3...
  • CasNo: 1335210-34-8
  • Molecular Formula: C14H16N2O6
  • Appearance: White crystallization
  • Application: treating pulmonary embolism and preven...
  • DeliveryTime: in two weeks
  • PackAge: 25kg/drum
  • Port: SHANGHAI BEIJING
  • ProductionCapacity: 10 Metric Ton/Day
  • Purity: 99.9% by HPLC
  • Transportation: AIR SEA TRAIN
  • LimitNum: 1 Kilogram
  • Moisture Content: ≤0.5%

Superiority

We are very compeitive on Dolutegravir .Our mfr is Chinese GMP certified for this item with DMF document.

Product Name: (4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid
CAS: 1335210-34-8
MF: C14H16N2O6
MW: 308.29
EINECS:  
Product Categories:  
Mol File: 1335210-34-8.mol
(4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid Structure
 
(4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid Chemical Properties
Boiling point  560.8±50.0 °C(Predicted)
density  1.50±0.1 g/cm3(Predicted)
pka 5.52±0.40(Predicted)

Details

Synthesis 5-methoxy-6-(methoxycarbonyl)-4-oxo-1-(2-oxoethyl)-1,4-dihydropyridine-3-carboxylic acid (3.38 g, 107.24 mmol) was dissolved in 33 ml of acetonitrile. Add glacial acetic acid (3 ml) and methanesulfonic acid (0.21 ml, 3.24 mmol) in a 150 ml round bottom flask at room temperature. The reaction was heated to 60 ° C for 19 h. (R)-3-Amino-1-butanol (1.44 ml, 1.34 g, dissolved in 2.25 ml of CH3CN) was slowly added dropwise to the above reaction solution. The reaction was continued to stir at 60 ° C for 18 h to give a white suspension. The reaction solution was concentrated to dryness under reduced pressure to give a concentrate. Add 25 ml of CH2Cl2 and 1N HCl (25 ml). The organic layer was separated, and the aqueous layer was extracted with CH 2 Cl 2 (25 ml x 2). The organic layers were combined and concentrated to dryness under reduced pressure to give crude 6 2.2g. The crude product was recrystallized from 15 ml of MeOH/petroleum ether = 6/1 solvent. After filtration and drying, a pale yellow solid product of (4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid was obtained, 1.72 g.
(4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid
 
(4R,12aS)-7-Methoxy-4-Methyl-6,8-dioxo-3,4,6,8,12,12a-hexahydro-2H-[1,3]oxazino[3,2-d]pyrido[1,2-a]pyrazine-9-carboxylic acid Preparation Products And Raw materials
Raw materials 1-(2,2-diMethoxyethyl)-5-Methoxy-6-(Methoxycarbonyl)-4-oxo-1,4-dihydropyridine-3-carboxylic acid-->(R)-3-amino-1-butanol
Preparation Products O-Methyl Dolutegravir

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