Merck + Co., Inc.

Steven A King

Thomas R Verhoeven

Alan W Douglas

Lisa DiMichele

Andrew S Thompson

Michel M Chartrain

Joseph D Armstrong, Iii

David Alan Conlon

Brenda Pipik

Lorraine G Katz

Jennifer L Keller

.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50 N/mm.sup.2 of hydrogen in the presence of a strong acid.

Ruthenium-phosphine complex catalysts for asymmetric hydrogenations

The present invention provides a novel process for the preparation of 1,1-cyclopropanedimethanol cyclic sulfite which comprises: (a) contacting 1,1-cyclopropanedimethanol with dialkylsulfite in the presence of a base; and (b) removing from the reaction mixture the alcohol reaction by-product. This process is incorporated in the additional novel processes for preparing 1-(hydroxymethyl)cyclopropaneacetonitrile and 1-(thiomethyl)cyclopropaneacetic acid.

Process for the preparation of 1-(thiomethyl)-cyclopropaneacetic acid

.beta.- or .gamma.-Ketoesters and .beta.- or .gamma.-ketoamides are asymmetrically reduced with a Ru(II)-BINAP derived catalyst at about 40.degree. C. and about 50N/mm.sup.2 of hydrogen in the presence of a strong acid.

Asymmetric hydrogenation of beta- or gamma-ketoesters and beta- or

There is disclosed a novel microbial bioconversion process for the synthesis of a trans-hydroxy sulfone intermediate, which is the precursor to topical carbonic anhydrase inhibitors (TCAI's). TCAI's are effective in the treatment of glaucoma and ocular hypertension. The bioconversion process is carried out in the presence of the microorganism Rhodotorula rubra, or Rhodotorula piliminae and results in a trans-hydroxy sulfone which exhibits a diastereomeric excess of greater than 95%.

Bioconversion process for the synthesis of transhydroxy sulfone by

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Summit, NJ, United States of America

Steven A King