On October 30, 2008, Delisser, Vern; Hedberg, Martin; Jansson, Annette; Raadevik, Andreas; Ryberg, Per; Thiering, Swantje published a patent.Category: nitriles-buliding-blocks The title of the patent was Process for preparation of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indole-5-carbonitrile. And the patent contained the following:
The present invention pertains to a process for the preparation of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indole-5-carbonitrile as a free base and pharmaceutically acceptable salts thereof, particularly the citrate salt. For example, Et 2-[5-[(morpholin-4-yl)methyl]pyridin-2-yl]acetate was reacted with 3-fluoro-4-nitrobenzonitrile in THF at -20 °C in presence of lithium tert-butoxide to afford an intermediate, which was treated with Degussa heterogeneous catalyst (platinum and vanadium on active carbon) under hydrogen for selective reduction of nitro group to amino group. The reduction product obtained above was treated with citric acid monohydrate at 60-75 °C for 2 h in Bu acetate, DMF, and iso-propanol, cooled to 5 °C over 10 h, and held overnight at 5 °C to gave 75 % yield of 2-hydroxy-3-[5-(morpholin-4-ylmethyl)pyridin-2-yl]-1H-indole-5-carbonitrile citrate as an orange solid. Advantageously, the new process is suitable for large scale industrial manufacturing The experimental process involved the reaction of 3-Chloro-4-nitrobenzonitrile(cas: 34662-29-8).Category: nitriles-buliding-blocks
The Article related to preparation morpholin indole citrate, Heterocyclic Compounds (More Than One Hetero Atom): Other 6-Membered Rings, Two Hetero Atoms and other aspects.Category: nitriles-buliding-blocks
Referemce:
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts