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

Kusanthula linagliptin yomwe ilipo ndi fungulo lake lapakati 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1--[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) kaphatikizidwe njira, pezani njira yopangira yoyenera kupanga mafakitale.Njira: fotokozani mwachidule njira zosiyanasiyana zopangira.Zotsatira ndi zomaliza: Njira 2.2 ili ndi njira yosavuta komanso yotsika mtengo, yomwe ili yoyenera kupanga mafakitale.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione ndi gawo lapakati pakupanga kwa linagliptin mankhwala a hypoglycemic.Kaphatikizidwe ka 1 kamagwiritsa ntchito methyl urea ndi cyanoacetic acid ngati zida zoyambira, ndipo amakumana ndi magawo asanu ndi limodzi a condensation, cyclization, nitrosation, kuchepetsa, cyclization, ndi bromine ndi zokolola zonse za 46.3%.Zomangamanga zapakati zonse zidatsimikiziridwa ndi 1HNMR.

Zomwe zidapangidwa pano zikugwirizana ndi njira yosavuta yokonzekera ya linagliptin yoyera kwambiri.Quinazoline, chinsinsi chapakatikati pakukonza mphika umodzi wa linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, yapakatikati imasiyanitsidwa ndi kusefa, kenako anachita ndi (R) 3 aminopiperidine dihydrochloride kupeza yankho munali linagliptin.Mukatha kukonzedwanso yankho lomwe lili ndi linagliptin, Deliraliptin yoyera.Kukonzekera kwa kiyi wapakatikati pa zomwe zapezedwa pano kutengera njira ya mphika umodzi, yomwe ndi yabwino kugwira ntchito ndikuwongolera zokolola.Makiyi apakati akalekanitsidwa, amachitidwa ndi (R) 3 aminopiperidine dihydrochloride, potero Kupeza linagliptin yoyera kwambiri kumakwaniritsa zofunikira zopanga ndi kulengeza zamakampani opanga mankhwala kwambiri.