Process and intermediates useful in the preparation of statins, particularly atorvastatin
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United States of America Patent
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Dec 24, 2013
Grant Date -
Mar 5, 2009
app pub date -
Aug 14, 2008
filing date -
Jul 25, 2003
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Abstract
There is provided a process for the preparation of a compound of formula (7) or salts thereof: wherein R1 represents a hydrogen or a hydrocarbyl group, R2 represents a hydrogen or substituent group, R3 represents 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; P1 represents hydrogen or a protecting group, and W represents ═O or —OP2, in which P2 represents 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 —OP2, 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 ═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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