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A practical synthesis of cinacalcet (Sensipar ® , Mimpara ® ) is described. The synthesis starts from readily available starting materials and relies on safe and practical reaction conditions. The sequence comprises three synthetic steps and only one isolation point. The overall yield for the sequence is 85%.
A concise, scaleable synthesis of building block 10 for p38 kinase inhibitor B is described. The key step is the one-pot construction of 5-aryl-3-methyl-2-methylsulfanyl-6-pyridin-4-yl-3H-pyrimidin-4-one 4 from arylacetic acid ethyl ester 1. Subsequent hydrolysis of the thiomethyl group to the hydroxy group and chlorination provided the key intermediate, 2-chloro-3-methyl-6-pyridin-4-yl-5-aryl-3H-pyrimidin-4-one...
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