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1236409-72-5

1-(4-(1-cyanocyclobutyl)phenyl)-4-hydroxy-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonitrile synthesis

5synthesis methods
ethyl3-(2-cyano-N-(4-(1-cyanocyclobutyl)phenyl)acetamido)propanoate

1236410-58-4
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1-(4-(1-cyanocyclobutyl)phenyl)-4-hydroxy-2-oxo-1,2,5,6-tetrahydropyridine-3-carbonitrile

1236409-72-5
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Yield:1236409-72-5 5.8 kg

Reaction Conditions:

Stage #1: ethyl 3-(2-cyano-N-(4-(1-cyanocyclobutyl)phenyl)acetamido)propanoatewith 1,8-diazabicyclo[5.4.0]undec-7-ene in tetrahydrofuran at 60; for 1 h;Large scale;
Stage #2: with hydrogenchloride in water at 20 - 30; pH=1 - 2; for 20 h;Large scale;

References:

Shavnya, Andrei;Tao, Yong;Lilley, Susan C.;Bahnck, Kevin B.;Munchhof, Michael J.;Nematalla, Asaad;Waldo, Michael;Bill, David R. [Organic Process Research and Development,2013,vol. 17,# 12,p. 1510 - 1516]