Eli Lilly and Company

Milton J Zmijewski

Barbara S Briggs

David Lee Varie

Jeffrey Thomas Vicenzi

Benjamin Alan Anderson

Marvin M Hansen

Manuel Debono

Karl H Michel

Raymond C Yao

R Michael Molloy

Otis W Godfrey

Jeffrey T Fayerman

Gary G Marconi

Mary L Huber

Tom E Eaton

Michael D Jones

Jeffrey N Levy

Robert M Logan

Lynda M Ford

A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

Synthesis of (S)-.alpha.-methyl-1,3-benzodioxole-5-ethanol and

Stereoselective process for producing dihydro-2,3-benzodiazepine

Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides said phthalyl amidase, means for producing it by culturing the natural organism from which the activity was identified, and methods for using said phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides.

Enzyme from microbial source: phthalyl amidase

The present invention provides a biotransformation process for preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are hydrogen or a .beta.-glucuronide group of the formula ##STR2## provided at least one of R.sub.1 and R.sub.2 is a .beta.-glucuronide group.

Process for preparation of benzo[B]thiophene glucuronides

New glycopeptides prepared by biotransformation of a vancomycin-type antibiotic by an Acinomadura citrea culture (NRRL 18382), which are useful intermediates, and methods of preparing the biotransformed intermediates by adding a vancomycin-type glycopeptide to a growing culture of Actinomadura citrea NRRL 18382 and continuing fermentation under submerged aerobic conditions, are provided.

Biotransformation of glycopeptide antibiotics

Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides 2 phthalyl amidase, 2 method for producing it by culturing the natural organism from which the activity was identified, and methods for using the phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides. The ezyme is isolated from Xanthobacter agilis.

Phthalyl amidase-producing Xanthobacter agilis

Phthalyl amidase is an enzyme previously unknown in the art that catalyzes removal of the phthalyl moiety from phthalyl-containing amides. The current invention provides a phthalyl amidase, a method for producing it by culturing the natural organism from which the activity was identified, and methods for using the phthalyl amidase to remove the phthalyl moiety from phthalyl-containing amides. The enzyme is isolated from Xanthobacter agilis.

Removal of phthalyl groups from amides and esters using an amidase

An enantiomerically selective process for acylating racemic 3-amino azetidinone intermediates is provided using penicillin G amidase(acylase) as biocatalyst.

Enantiomerically selective biocatalyzed acylation

Improved fermentation process for producing the Gram-positive antibiotic A47934 which comprises cultivating a new strain of Streptomyces toyocaensis, NRRL 18112, and a biologically purified culture of this microorganism are provided.

Process for producing antibiotic A47934

Improved fermentation process for producing the gram-positive A-21978C antibiotics which comprises cultivating a new strain of Streptomyces roseosporus, NRRL 15998, and the biologically purified culture of this microorganism are provided.

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Carmel, IN, United States of America

Milton J Zmijewski