On July 2, 2009, Nazare, Marc; Zech, Gernot; Goerlitzer, Jochen; Just, Melitta; Weiss, Tilo; Hessler, Gerhard; Czechtizky, Werngard; Ruf, Sven published a patent.Synthetic Route of 53838-27-0 The title of the patent was Preparation of pyrazole-carboxamide derivatives as P2Y12 antagonists for treating cardiovascular disorders. And the patent contained the following:
The present invention relates to compounds of the formula I (wherein D is 3-15-membered heterocyclyl, (C6-C14)-aryl, etc.; Q and Z are -(C0-C4)-alkylene-O-(C0-C4)-alkylene-; -(C0-C4)-alkylene-SO2-(C0-C4)-alkylene-, etc.; J is H, (C1-C6)-alkyl, etc.; A is a covalent bond, (C1-C8)-alkylene, etc.; B is a covalent bond, (C2-C10)alkenyl, etc.; V is (un)substituted monocyclic or bicyclic 3-15-membered heterocyclyl; G is a covalent bond, (C2-C10)-alkenyl, etc.; M is H, (C1-C8)-alkyl, etc.; R1 is H or (C1-C4)alkyl; R2 is H, (C1-C6)alkyl, etc.). The compounds of the formula I are valuable pharmacol. active compounds They exhibit a strong anti-aggregating effect on platelets and thus an anti-thrombotic effect and are suitable e.g. for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible antagonists of the platelet ADP receptor P2Y12, and can in general be applied in conditions in which an undesired activation of the platelet ADP receptor P2Y12 is present or for the cure or prevention of which an inhibition of the platelet ADP receptor P2Y12 is intended. The invention furthermore relates to processes for the preparation of compounds of the formula I, their use, in particular as active ingredients in pharmaceuticals, and pharmaceutical preparations comprising them. Example compound II was prepared in a multistep synthesis that culminated in the conversion of the 5-(1-ethoxycarbonyl-cyclobutoxy) intermediate to II. In a human P2Y12 recombinant cell membrane binding assay, II had an IC50 of 0.601 μM. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Synthetic Route of 53838-27-0
The Article related to pyrazole carboxamide derivative preparation p2y12 antagonist treatment cardiovascular disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazoles and other aspects.Synthetic Route of 53838-27-0
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