Astrazeneca Ab

Astra Zeneca U.k. Limited

Michael Butters

Andrew Stocker

Paul Michael Murray

Colin Thomson

Evan William Snape

Jeffrey Norman Crabb

Bharti Patel

Philip Hopes

Matthew James Welham

Eric Merifield

Andrew James Watts

Paul Schofield

Debra Ainge

Parhalad Ray Sharma

Ravi Naidu Rayapati

Steven Robert Lenger

Ravi Ramakrishnan

Richard Wisedale

Colin Thompson

Eric c/o Astrazeneca Intellectual Property Merifield

Andrew Watts

The invention relates to compounds of formula (X), and salts thereof, and their use as intermediates in improved manufacturing processes for the synthesis of pharmaceutical compound (I):  X is &#x2550;O, &#x2550;N&#x2014;OH or &#x2550;N&#x2014;OC(O)Me; Y is hydrogen, PhS- or p-chlorophenylsulfanyl; Z is hydrogen or &#x2014;CHCOORwherein Ris selected from hydrogen, optionally substituted hydrocarbyl and optionally substituted heterocyclyl.

Pharmaceutical process and intermediates 714

A process for preparing pharmaceutically active compounds of formula (I) or a salt thereof wherein R, n, m, R, R, X, X, Xand Xare as defined in the specification, is described. Novel intermediates are also described and claimed.

Chemical process 632

A process for formation of a compound of formula (I) or a pharmaceutically acceptable salt thereof, (A chemical formula should be inserted here&#x2014;please see paper copy enclosed herewith) I via a Heck reaction is described. Intermediates useful in the process and processes for making said intermediates are also described. 

Chemical process

A method for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt or solvate thereof; from a compound of the formula: (IV); wherein L represents a leaving group. 

Process for the preparation of thiazolopyrimidines

Novel Process and Intermediates. A process for preparing a compound of formula (I) where Rand Rare as defined in the specification; and Ris hydrogen or a protecting group, which process comprises cyclisation of a compound of formula (II) where Rand Rand Rare as defined in relation to formula (I), and Ris nitrogen protecting group, and removing the group R, and thereafter if desired, removing any protecting group R. Novel intermediates and the use of these in the formation of pharmaceutical compounds is also described and claimed 

Process and intermediates for the preparation of thienopyrrole derivatives

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Bristol, United Kingdom

Michael Butters