Enantioselective preparation of halophenyl alcohols and acylates

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United States of America Patent

PATENT NO 5986095
SERIAL NO

07817232

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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A process is described for preparing a compound of the formula or the S-enantiomer thereof, wherein: R is alkyl, aryl, cycloalkyl, aralkyl, or cycloalkylalkyl, R.sup.1 is halogen; R.sup.2 is halogen, alkyl, cycloalkyl, aryl or ##STR1## wherein the process comprises treating the associated racemic alcohol with an acylating agent ##STR2## (wherein L is a leaving group) and an enzyme or microorganism capable of enantioselective acylation. This process may also be used to isolate the unreacted R- or S-alcohol. The acylated product may be enantioselectively hydrolyzed with a lipase or lipase-supplying microorganism to the S- or R-alcohol. Compounds prepared by this invention are useful antipsychotic agents or useful intermediates therefor.

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Patent Owner(s)

  • E.R. SQUIBB & SONS, INC.

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Hanson, Ronald L Morris Plains, NJ 27 340
Patel, Ramesh N Bridgewater, NJ 69 651
Szarka, Laszlo J East Brunswick, NJ 33 159

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