Redx Pharma Limited

Avecia Pharmaceuticals, Ltd.

Bradford Pharma Limited

David John Moody

Jonathan William Wiffen

Jonathan Willian Wiffen

Jonathan William 62 Springhill Manor Wiffen

Provided are a compound of formula (5) and a process for its preparation wherein: Rrepresents an alkyl group; Rrepresents an aryl group; Rrepresents a protecting group or an alkyl group; Rrepresents a protecting group or a SORgroup where Ris an alkyl group; Rrepresents (PRR)Xor P(&#x2550;O)RRin which X is an anion and Rand Reach independently is an alkyl, aryl, alkoxy, or aryloxy group; Prepresents hydrogen or a protecting group; and W represents &#x2550;O or OP, in which Prepresents hydrogen or a protecting group.

Process and intermediate compounds useful in the preparation of statins, particularly rosuvastatin

There is provides a process for the preparation of a compound of formula (): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Rrepresents an alkyl group, such as a Calkyl group, and preferably an isopropyl group; Rrepresents an aryl group, preferably a 4-fluorophenyl group; Rrepresents hydrogen, a protecting group or an alkyl group, such as a Calkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SORgroup where Ris an alkyl group, such as a Calkyl group, and preferably a methyl group. 

Process and intermediate compounds useful in the preparation of statins

There is provided a process for the preparation of a compound of formula (7) wherein Rrepresents an alkyl group; Rrepresents an aryl group; Rrepresents hydrogen, a protecting group or an alkyl group; and Rrepresents hydrogen, a protecting group or a SORgroup where Ris an alkyl group, which comprises a) hydroxylating a compound of formula (1) wherein Y represents a halo group; Prepresents hydrogen or a protecting group, and W represents &#x2550;O or &#x2014;OP, in which Prepresents hydrogen or a protecting group, to give a compound of formula (2), b) oxidixing the compound of formula (2) to give a compound of formula (3), c) coupling the compound of formula (3) with a compound of formula (4), wherein Rrepresents a protecting group or an alkyl group; Rrepresents a protecting group or a SORgroup where Ris an alkyl group; and Rrepresents (PRR)+Xor P(&#x2550;O)RRin which X is an anion and Rand Reach independently is an alkyl, aryl. 

There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein Rrepresents a hydrogen or a hydrocarbyl group, Rrepresents a hydrogen or substituent group, Rrepresents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; Prepresents hydrogen or a protecting group, and W represents &#x2550;O or &#x2014;OP, in which Prepresents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents &#x2014;OP, deprotecting and then oxidizing the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents &#x2550;O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof. 

Process and intermediates useful in the preparation of statins, particularly atorvastatin

There is provides a process for the preparation of a compound of formula (7): wherein R is an optionally substituted hydrocarbyl group or an optionally substituted heterocyclic group; provides that R is not a compound of Formula (a): wherein Rrepresents an alkyl group, such as a Calkyl group, and preferably an isopropyl group; Rrepresents an aryl group, preferably a 4-fluorophenyl group; Rrepresents hydrogen, a protecting group or an alkyl group, such as a Calkyl group, and preferably a methyl group; and Rd represents hydrogen, a protecting group or a SORgroup where Ris an alkyl group, such as a Calkyl group, and preferably a methyl group. 

There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein Rrepresents a hydrogen or a hydrocarbyl group, Rrepresents a hydrogen or substituent group, Rrepresents a hydrogen or a hydrocarbyl group, and X represents a hydrogen or substituent group which comprises a) cyanating a compound of formula (1): wherein Y represents a halo group, preferably CI or Br; Prepresents hydrogen or a protecting group, and W represents =0 or &#x2014;OP, in which Prepresents hydrogen or a protecting group, to give a compound of formula (2): b) reducing the compound of formula (2) to give a compound of formula (3): coupling the compound of formula (3) with a compound of formula (4): to give a compound of formula (5): when W represents &#x2014;OP, deprotecting and then oxidising the compound of formula (5) to give a compound of formula (6): and e) subjecting the compound of formula (5) when W represents &#x2550;O, or compound of formula (6) to ring-opening, and removal of any remaining protecting groups, to give a compound of formula (7) or salts thereof 

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Fife, United Kingdom

David John Moody