Roche Colorado Corporation

Hoffmann-la Roche Inc.

Roche Palo Alto LLC

Lewis M Hodges

David A Johnston

Michelangelo Scalone

Kurt Puentener

Mark A Schwindt

Yeun-Kwei Han

Michael P Fleming

Robert J Topping

Roger P Micheli

Chris R Roberts

Peter John Harrington

Goesta Rimmler

Wolfgang Goehring

Martin R Guinn

Hendrick Moorlag

The invention provides methods of synthesizing peptides, involving the steps of providing a composition including a peptide fragment, wherein the peptide fragment has at least one amino acid residue and includes a base-sensitive, N-terminal protecting group; removing the base-sensitive, N-terminal protecting group from the peptide fragment using a deprotection reagent that includes a base, whereby an N-terminal functionality on the peptide fragment is deprotected; removing the base from the composition to provide a residual base content of more than 100 ppm; causing a reactive peptide fragment having a reactive C-terminus and a base-sensitive N-terminal protecting group to react with the deprotected N-terminal functionality of the peptide fragment under conditions such that the reactive peptide fragment is added to the peptide fragment; and optionally repeating the deprotection and coupling steps until a desired peptide is obtained. Also provided are methods of synthesizing peptides, wherein base is removed from the composition to a point where the composition would provide a positive chloranil test. Also provided are methods of synthesizing peptides, wherein coupling is performed in basic reaction mixtures.

Process and systems for peptide synthesis

The present invention relates to a process for the manufacture of compounds of formula wherein the substituents are as described hereinwhich comprises the steps of with a compound of formula to form a compound of formula b) converting the OH/&#x2550;O function of compounds of formula XIV/XIVa into a leaving group P with a reagent containing a leaving group, selected from POCl, PBr, MeI and (FCSO)O to form a compound of formula wherein P is halogen or trifluoromethanesulfonate; and The compounds of formula I are valuable intermediates for the manufacture of therapeutically active compounds which have NK-1 antagonist activity.

Process for preparation of pyridine derivatives

The present invention relates to a novel process for producing a &#x3b4;-lactone of the formula:using an acyl halide of the formula:wherein R, RRand X are described herein, as well as novel intermediates. In particular, the present invention relates to a process for enantioselectively producing the (R)-&#x3b4;-lactone.

Synthesis of 3,6-dialkyl-5,6-dihydro-4-hydroxy-pyran-2-one

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Longmont, CO, United States of America

Lewis M Hodges