Roche Colorado Corporation

Roche Palo Alto LLC

Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

David A Johnston

Lewis M Hodges

Yeun-Kwei Han

Mark A Schwindt

Michelangelo Scalone

Kurt Puentener

Michael P Fleming

Robert J Topping

Chris R Roberts

Roger P Micheli

Peter John Harrington

L Mark Hodges

Hiralal N Khatri

Goesta Rimmler

Richard A Gabel

Wolfgang Goehring

Martin R Guinn

Hendrick Moorlag

Michael D Groaning

Methods for the solid phase synthesis of T-1249 peptides and peptide intermediates, in particular methods involving synthesizing T-1249 peptide intermediates at low loading factors to produce products having excellent purity and yield.

Synthesis using peptide intermediate fragments

The present invention relates to technology for preparing derivatives of unsaturated, cyclic, organic acids and salts, thereof. Shikimic acid is an example of such an acid. More particularly, the present invention relates to preparing derivatives of these acids or salts thereof that are esterified, ketalized, functionalized with a leaving group, and/or provided with epoxide functionality. Preferred aspects may be used in the synthesis of Oseltamivir Phosphate starting from shikimic acid.

Derivatives of unsaturated, cyclic organic acids

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 provides a process for preparing a pyridine compound of the formula: wherein R, R, Rand a are those defined herein.

Process for preparation of pyridine derivatives of NK-1 receptor antagonist

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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Louisville, CO, United States of America

David A Johnston