Schering Corporation

William Brian Morgan

Aleksey Zaks

Michael J Homann

Viyyoor Moopil Girijavallabhan

Ashit K Ganguly

Anil K Saksena

Raymond G Lovey

Yi-Tsung Liu

Russell E Pike

Haiyan Wang

Jinchu Liu

Enantioselective enzymatic hydrolysis of 3-substituted esters of glutaric acid

The invention relates to a process for preparing a substituted (6,11-dihydro-5H-benzo[5,6]cyclohepta[1,2-b]pyridin-11-yl)piperidine compound of the formula (+)-I ##STR1## wherein: R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are independently selected from the group consisting of hydrogen, halo, C.sub.1 -C.sub.6 alkyl, amino, --OCH.sub.3, --OCF.sub.3 and CF.sub.3, and the dotted line represents an optional double bond; comprising:

Enzymatic kinetic resolution of an intermediate useful for preparing

A process for the microbiological or enzymatic hydrolytic resolution of racemic trans-2-(alkoxycarbonylethyl) lactams of the formula I: ##STR1## wherein R is C.sub.1 -C.sub.7 alkyl, 2,2,2-trifluoroethyl or methoxyethoxyethyl and R.sup.1 is hydrogen or a protecting group is disclosed, whereby an optically enriched compound of the formula Ib or IIa: ##STR2## is obtained.

Resolution of trans-2-(alkoxycarbonylethyl)-lactams useful in the

Disclosed is a process for preparing chiral compounds of the formula (I) ##STR1## wherein: X.sup.1 and X.sup.2 are independently F or Cl; and E is --SO.sub.2 R.sup.2, wherein R.sup.2 is C.sub.1 -C.sub.6 alkyl, --C.sub.6 H.sub.4 CH.sub.3 or --CF.sub.3 ; its enantiomer and racemates thereof, useful in the synthesis of tetrahydrofuran azole antifungals. Novel compounds of the formula ##STR2## wherein: X.sup.1 and X.sup.2 are independently F or Cl; B represents --C(O)Q* or --CH.sub.2 OR'; Q* represents a chiral auxiliary group; R' represents a hydroxy protecting group selected from --CH.sub.2 C.sub.6 H.sub.5, or --C(O)R.sup.1, wherein R.sup.1 is C.sub.1 -C.sub.6 alkyl; and A represents Cl, Br, I or triazolyl; are also disclosed.

Process for preparing intermediates for the synthesis of antifungal

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Chatham, NJ, United States of America

William Brian Morgan