Reaktion #159675

Reaktionsgleichung

5-chloro-2-(3-(3-(trifluoromethyl)phenoxy)azetidin-1-yl)nicotinic acid

methyl 4-(1-aminocyclopropyl)benzoate

methyl 4-(1-aminocyclopropyl)benzoate hydrochloride

→

title compound ( D149 )

Ausbeute 8.7%

methyl 4-(1-(5-chloro-2-(3-(3-(trifluoromethyl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate

Ausbeute 8.7%

Reaktionsbedingungen

Aufarbeitung

1. 1
   SonstigeThe title compound (D149) (20 mg) was prepared
2. 2
   SonstigeThe residue obtained from SPE-
3. 3
   SonstigeSi cartridge purification (38 mg)
4. 4
   workup.DISSOLUTIONdissolved in a mixture of chloroform/ethanol/n-hexane (70/15/15) (1 ml)
5. 5
   Sonstigewas separated by chiral HPLC [Phenomenex Lux1 column (250×20 mm, 5 μm particle size). Mobile phase: isocratic premixed mixture of (hexane 75%, ethanol 25%) containing 0.1% of diethylamine. Flow rate=10 ml/min. UV detection: 235 nm]
6. 6
   SonstigeCollected fractions, after solvent evaporation

Vorschrift

The title compound (D149) (20 mg) was prepared according to the experimental procedure described in Description 148 starting from 5-chloro-2-(3-(3-(trifluoromethyl)phenoxy)azetidin-1-yl)nicotinic acid (D105) (160 mg, 0.423 mmol) and methyl 4-(1-aminocyclopropyl)benzoate (D7) (115.45 mg, 0.507 mmol). The residue obtained from SPE-Si cartridge purification (38 mg) dissolved in a mixture of chloroform/ethanol/n-hexane (70/15/15) (1 ml) was separated by chiral HPLC [Phenomenex Lux1 column (250×20 mm, 5 μm particle size). Mobile phase: isocratic premixed mixture of (hexane 75%, ethanol 25%) containing 0.1% of diethylamine. Flow rate=10 ml/min. UV detection: 235 nm]. Collected fractions, after solvent evaporation afforded the title compound (D149) (20 mg)

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