Riociguat preparation method

Riociguat preparation method

  • CN 105,367,568 A
  • Filed: 11/18/2015
  • Published: 03/02/2016
  • Est. Priority Date: 11/18/2015
  • Status: Active Grant
First Claim
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1. prepare a method for the western croak of Leo, comprise the steps:

  • Step 1, prepare the intermediate N substituted benzyl-N-methyl-2-amino propane dinitrile shown in structural formula V, wherein substituent R is hydrogen or methoxyl group;

    Step 2,5-(N-methyl) (R replacement) benzyl amino-2-[1-(2-the luorobenzyl)-1H-pyrazolo [3 of preparation shown in formula II I, 4-b] pyridin-3-yl] pyrimidine-4,6-diamines, what limits in meaning and the step (1) of wherein R is identical;

    by 1-(2-the luorobenzyl)-1H-pyrazolo [3 shown in middle for step (1) the intermediate V for preparing and structural formula IV, 4-b] pyridine-3-carbonamidine carries out ring-closure reaction, obtains the pyrimidine ring intermediate III of benzyl protection;

    Step 3,5-methylamino--2-[1-(2-the luorobenzyl)-1H-pyrazolo [3 of preparation shown in formula II, 4-b] pyridin-3-yl] pyrimidine-4,6-diamines;

    the pyrimidine ring intermediate III that step (2) obtains is carried out reduction reaction, debenzylation is protected, and obtains intermediate II;

    Step 4, prepares the western croak of Leo shown in structural formula I;

    carry out urethane reaction by the intermediate II making step (3) obtain, obtains the western croak of Leo,Wherein step 2-4 is as follows;

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