Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Ulrich Zutter

Michelangelo Scalone

Martin Karpf

Peter Karl Matzinger

Beat Wirz

Rudolf Schmid

Patrizio Mattei

Hans Iding

Bjoern Bartels

Emil A Broger

Urs Schwitter

Stefan Hildbrand

Jean-Michel Adam

Bruno Lohri

Olaf Grassmann

Christophe Pfleger

Joseph Foricher

Roland Meier

Alec Fettes

Stefan Abrecht

Fritz Bliss

Gerard Moine

Philipp Cueni

The present invention provides processes to manufacture crystalline N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide. Also disclosed are compounds useful as intermediates in the methods of the invention.

Process to manufacture N-[(3S)-1-[4-[(3-fluorophenyl)methoxy]phenyl]-5-oxo-pyrrolidin-3-yl]acetamide

The present invention relates in part to a process for the preparation of a proline derivative of formula I wherein,  The proline derivatives of the formula I are preferential inhibitors of the cysteine protease Cathepsin S and are therefore useful to treat metabolic diseases like diabetes, atherosclerosis, abdominal aortic aneurysm, peripheral arterial disease and diabetic nephropathy.

Process for the preparation of proline derivatives

The present invention relates to a process of the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one of the formula by employing a dialkylmalonate of the formula wherein Ris lower alkyl, and the use of this process for the manufacture of DPP-IV inhibitors that are useful for the treatment and/or prophylaxis of diseases such as diabetes.

Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one

This invention relates to a process of the preparation of the novel intermediate (S)-4-fluoromethyl-dihydro-furan-2-one of the formula and with its use for the manufacture of pyrido[2,1-a]isoquinoline derivatives of the formula which are useful for the treatment and/or prophylaxis of diseases which are associated with DPP IV.

Process for the preparation of (S)-4-fluoromethyl-dihydro-furan-2-one useful in the preparation of the DPP-IV inhibitor (S)-1 ((2S,3S,11bS)-2-amino-9,10-dimethoxy-1,3,4,6,7, 11b-hexahydro-2H-pyrido[2,1-a] isoquinolin-3-yl)-4-fluoromethyl-pyrrolidin-2-one

Compounds of formula I and a process for the preparation of such compounds are disclosed.

Synthesis of &#x3b1;-amino-&#x3b2;-alkoxy-carboxylic acid esters

A novel process for the manufacture of compounds of the formulawherein Rand Rindependently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Asymmetric synthesis process

Stereo-specific synthesis of shimikic acid derivatives with improved efficiency

The present invention relates to a process for the preparation of compounds of formula I

Process for the preparation of chiral lactones

A novel process for the manufacture of compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 independently represent aroyl. The present invention also concerns novel intermediates used in the novel process for making compounds of formula I.

Asymmetric synthesis of azepines

Assymetric synthesis of azepines

A catalytic process for the manufacture of optically active compounds of the formula ##STR1## wherein R.sup.1 and R.sup.2 are alkyl, which is optionally interrupted by an O atom in a position other than the .alpha.-or .beta.-position, or optionally substituted benzyl,

Process for the preparation of optically active compounds

The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.

Production of oxetanones

The invention relates to a novel process for producing a compound having the formula ##STR1## wherein R.sup.1, R.sup.2 and X are described herein, via wherein R corresponding .beta.-keto- and .beta.-hydroxy-.delta.-lactones, as well as novel intermediates which occur in the process.

Growing community of inventors

Basel, Switzerland

Ulrich Zutter