Improved process for the preparation of 6-chloro-5-(2-chloroethyl)oxindole
The current process for ziprasidone involves preparation and isolation of the key intermediate 6-chloro-5-(2-chloroethyl)oxindole. An improved process for the synthesis of this intermediate is reported here. The new process involves use of a novel Lewis acid-mediated selective deoxygenation of the precursor ketone with tetramethyldisiloxane. The new method affords the desired compound in a one-pot process obviating the need for isolation of the potentially hazardous precursor ketone. This process was successfully scaled up to multikilo scale.
Nadkarni, Durgesh V.,Hallissey, James F.
supporting information
p. 1142 - 1145
(2013/01/03)
Ziprasidone process
A process for preparing ziprasidone having low levels of keto ziprasidone and hydroxy ziprasidone impurities.
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Page/Page column 7
(2008/06/13)
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