8-Bromo-7-sed-2-ynyl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3

Ad resolvendum linagliptinum existentem eiusque clavem intermediam 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl -2-quinazolinyl)methyl)-1H-purine 2,6-dione (11) synthesis methodus, syntheticam viam invenio ad productionem industriae idoneam.Methodus: Summatim syntheticarum itinerum diversarum.Proventus et conclusiones: Iter 2.2 processus simplex relative habet et sumptus inferiores, qui ad productionem industrialem aptior est.

8-bromo-3,7-dihydro-3-methyl-1H-purinum-2,6-dione clavis media est in synthesi medicamentorum linagliptini hypoglycemici.Synthesis 1 utitur acido methyl ureae et cyanoacetico in materiis incipiens, ac sex gradus motus condensationis, cyclizationis, nitrosationis, reductionis, cyclizationis, et brominis cum toto cede 46,3% patitur.Structurae omnium intermediarum confirmata sunt 1HNMR.

Praesens inventio pertinet ad methodum praeparationis simplicem summus puritatis linagliptin.Quinazoline, clavis media ad praeparationem linagliptin 8 bromo 7 ollae unius (2 butyne 1 basis) 3,7 dihydro 3 methyl 1 [(4 yl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, medium separatur. filtration, tum portavit cum (R)3 aminopiperidine dihydrochloride ad solutionem linagliptin continentem obtinendam.Post solutionem linagliptin continens iterum processit, productum Deliraliptin purum.Praeparatio clavem intermedii praesentis inventionis unam ollam adhibet methodum, quae commoda operandi et melioris cedit.Post medium clavem separatum, cum aminopiperidine dihydrochloride 3 portatum est, eo quod linagliptin puritatem altam obtinens etiam productionem et declarationem postulationum societatum pharmaceuticae maxime occurrit.