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Imatinib synthesis by Lu

2015 
The present invention discloses a method for the synthesis of imatinib by Lu. The method of using Suzuki coupling reaction and a Kumada coupling, does not require isolation of intermediates, in one pot (one-pot) high yield intermediate (9), with a mixed anhydride instead of methacryloyl chloride; cheap price of the process of the present invention is the use of 4-halo Generation two anisole as a starting material, and a Kumada coupling by Suzuki coupling reaction, using a pot (one-pot) methods, the overall route is as follows: The present invention does not require intermediate separation and purification, to give high yields of intermediate (9) (chemical purity and optical purity of> = 99%), to avoid special reaction conditions, high temperature and pressure and microwave, with the last step of acrylic acid chloride and the resulting mixed acid anhydride chloride instead of acryloyl chloride, avoiding intermediate (10) occurs multilocus amidation, reduction by-product, in order to achieve a high yield and a high purity obtained by Lu imatinib, this process route a short, low cost, environmentally suitable for industrial production volume.
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