Production Method 1

1917354-49-4

6968-76-9

917389-29-8

32634-68-7

Reaction Conditions

1.1 Reagents: Phosphorus pentachloride Solvents: Toluene

Reference

Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer-Catalyzed Aza-Michael Reaction

Humphrey, Guy R.; et al, Organic Process Research & Development, 2016, 20(6), 1097-1103

Production Method 2

69-72-7

32634-68-7

1791412-04-8

917389-29-8

32634-68-7

Reaction Conditions

1.1 Reagents: Tripotassium phosphate Solvents: Toluene ,  Water ;  rt → 45 °C; 1 h, 45 °C
1.2 Reagents: Tripotassium phosphate Catalysts: Cinchonanium, 1-[[3,5-bis(trifluoromethyl)phenyl]methyl]-9-hydroxy-1′-[[3-(trifl… Solvents: Dimethylformamide ;  45 °C → 0 °C; 5 h, 0 °C
1.3 Reagents: Glycolic acid ;  0 °C → 50 °C; 2 h, 50 °C
1.4 Reagents: Ethyl acetate Solvents: Toluene ;  rt → 45 °C; 2 h, 45 °C

Reference

Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer-Catalyzed Aza-Michael Reaction

Humphrey, Guy R.; et al, Organic Process Research & Development, 2016, 20(6), 1097-1103

Production Method 3

917389-29-8

32634-68-7

917389-29-8

32634-68-7

Reaction Conditions

1.1 Solvents: Ethyl acetate ;  rt → 45 °C; 2 h, 45 °C
1.2 Reagents: Ethyl acetate ;  45 °C → rt; 3 h, rt

Reference

Asymmetric Synthesis of Letermovir Using a Novel Phase-Transfer-Catalyzed Aza-Michael Reaction

Humphrey, Guy R.; et al, Organic Process Research & Development, 2016, 20(6), 1097-1103

4-Quinazolineacetic acid, 8-fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-, methyl ester Raw materials

• Salicylic acid
• 4-Quinazolineacetic acid, 8-fluoro-1,2,3,4-tetrahydro-3-[2-methoxy-5-(trifluoromethyl)phenyl]-2-oxo-, methyl ester, (4S)-
• 4-Quinazolineacetic acid, 8-fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-, methyl ester
• (+)-O,O’-Di-p-toluoyl-D-tartaric Acid
• 1-(3-Methoxyphenyl)piperazine dihydrochloride
• methyl (E)-3-(3-fluoro-2-(((E)-((2-methoxy-5-(trifluoromethyl)phenyl)amino)(4-(3-methoxyphenyl)piperazin-1-yl)methylene)amino)phenyl)acrylate

4-Quinazolineacetic acid, 8-fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-, methyl ester Preparation Products

• 4-Quinazolineacetic acid, 8-fluoro-3,4-dihydro-2-[4-(3-methoxyphenyl)-1-piperazinyl]-3-[2-methoxy-5-(trifluoromethyl)phenyl]-, methyl ester (917389-29-8)
• (+)-O,O’-Di-p-toluoyl-D-tartaric Acid (32634-68-7)

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