Nitro-Aldol Approach for Commercial Manufacturing of Fenspiride Hydrochloride

An efficient, short manufacturing process for fenspiride hydrochloride is reported. Nitro-aldol condensation is the key reaction in the developed process. Improved routes to key building blocks are demonstrated by expedient multikilogram production. Hazardous reactions are avoided. API produced foll...

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Veröffentlicht in:Organic process research & development 2019-06, Vol.23 (6), p.1252-1256
Hauptverfasser: Pramanik, Chinmoy, Bapat, Kiran, Patil, Pradip, Kotharkar, Sandeep, More, Yogesh, Gotrane, Dinkar, Chaskar, Sudhir P, Mahajan, Ulhas, Tripathy, Narendra K
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Sprache:eng
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Zusammenfassung:An efficient, short manufacturing process for fenspiride hydrochloride is reported. Nitro-aldol condensation is the key reaction in the developed process. Improved routes to key building blocks are demonstrated by expedient multikilogram production. Hazardous reactions are avoided. API produced following this new route meets the quality requirement NLT 99.70% purity by HPLC with any individual impurity NMT 0.10% with very good yield.
ISSN:1083-6160
1520-586X
DOI:10.1021/acs.oprd.9b00022