Hoffmann-la Roche Inc.

Givaudan Corporation

David L Coffen

Milton Manowitz

Harold A Brandman

Rudolf Schmid

Mark J Sebastian

Perry Rosen

George W Holland

Frederick Wong

Panayiotis Kalaritis

W Harry Mandeville

Rodney I Fryer

John Joseph Partridge

Alan N Schwartz

Urs O Hengartner

Pradeep B Madan

John J Patridge

Enantiomerically pure (2R)-2-hydroxy arylalkanoic acid esters and (2S)-2-hydroxy arylalkanoic acids are prepared by the Pseudomonas lipase-catalyzed selective hydrolyxis of racemic (2RS)-2-hydroxy arylalkanoic acid esters in solution or suspension in an aqueous medium at a controlled pH of from about 5 to about 9.

Production of 2-hydroxy substituted arylalkanoic acids and esters by

Enantiomerically pure (2R)-hydroxy-substituted benzopyran-2-carboxylic acid esters and (2S)-hydroxy-substituted benzopyran-2-carboxylic acids, are prepared by the Pseudomonas lipase-catalyzed selective hydrolysis of racemic (2RS)-hydroxy-substituted benzopyran-2-carboxylic acid esters in solution or suspension in an aqueous or aqueous/organic medium, at a pH of from about 5 to about 10.

Production of benzopyran-2-carboxylic acids and esters by enzymatic

A process for the preparing a compound of the formula ##STR1## wherein R.sub.1 and R.sub.2 are each independently hydrogen, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, halogen, trifluoromethyl or nitro; or R.sub.1 and R.sub.2 taken together with the benzene ring to which they are attached are naphthalene, and Ar is p-lower alkoxy phenyl. which comprises reacting ##STR2## wherein R.sub.1 and R.sub.2 are as described above with the compound of the formula ##STR3## wherein Ar is as described above, in an aromatic organic compound. The intermediates formed by the process of the invention are useful in the production of thiazepin-4(5H)-ones which have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure and agents for treating ischemia.

Glycidic acid ester and process of preparation

A process for producing natural vitamin E and intermediates in this process.

Lower-alkyl or aryl-sulfonyl unsaturated tacopherols

Vitamin E intermediate

New optically active intermediates and processes thereto are provided for use in synthesizing therapeutically active prostaglandins of the formula: ##STR1## wherein R.sup.1 is hydrogen or lower alkyl; from a compound of the formula: ##STR2## wherein R.sup.1 is as above and R.sup.2 is hydrogen or a carboxy blocking group convertible to an acid by hydrolysis.

Prostaglandin intermediates

Vitamin E intermediates

6-Etherified hydroxy -2-(4',8',12'-trimethyl-5'-tridecenyl)-2,5,7,8-tetramethylchromans with an oxo or hydroxy substituent at the 2' position which may be substituted with an arylsulfonyl or a carboxyalkyl at the 3' position and containing a single or double bond at the 11 position, said chromans being intermediates for producing natural vitamin E.

2-(trimethyl-tridecenyl)-tetramethylchroman intermediates for vitamin E

Cyclopenta[b]furan-2-ones

The preparation of bicyclic diketones of the formula ##STR1## wherein R.sub.1 is lower alkyl or ar-lower alkyl from a compound of the formula ##STR2## wherein R.sub.1 is as previously described or a salt thereof, and a di-lower alkyl malonate is described. The reactants are combined in a reaction sequence consisting of Michael addition, cyclization, hydrolysis, and decarboxylation. The preparation of the compounds of formula II is also described.

Process for bicyclic diketones

The preparation of bicyclic diketones of the formula ##STR1## wherein R.sub.1 is lower alkyl or ar-lower alkyl, from compounds of the formula ##STR2## wherein R.sub.1 is as set forth above, is described.

Preparation of diketones

There is presented compounds of the formula ##STR1## wherein R.sub.1 is selected from the group consisting of aryl, substituted aryl, aralkyl, heteroaryl, cycloalkyl, lower alkyl, lower alkenyl, carboxy lower alkyl, carboalkoxy lower alkyl, aminoalkyl, substituted aminoalkyl, hydroxyalkyl, alkoxy alkyl, thioalkoxy alkyl and hydrogen. These compounds exhibit pharmacological activity as antihypertensive agents. Also presented are novel intermediates leading to the end products and a process to produce the end products.

Lasalocid derivatives

There is disclosed methods and compositions for inhibiting or preventing the growth of microorganisms in aqueous systems wherein the growth is inhibited or prevented by the presence of an effective amount of a 2-chloro-3-oxobutyramide derivative.

Preservation of aqueous systems with 2-chloro-3-oxobutyramide derivatives

Methods and compositions for inhibiting or preventing the growth of microorganisms in aqueous systems wherein the growth is inhibited or prevented by the presence of an effective amount of .alpha.-chloro-.beta.-aminocrotonamide.

Growing community of inventors

Glen Ridge, NJ, United States of America

David L Coffen