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

Kuongorora iripo linagliptin uye kiyi yayo yepakati 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1--[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) synthesis nzira, tsvaga nzira yekugadzira yakakodzera kugadzirwa kwemaindasitiri.Nzira: pfupikisa nzira dzakasiyana dzekugadzira.Migumisiro uye mhedziso: Nzira 2.2 ine maitiro akareruka uye mutengo wakaderera, uyo wakanyatsokodzera kugadzirwa kwemaindasitiri.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione ndiyo yakakosha yepakati mukugadzirwa kweiyo hypoglycemic drug linagliptin.Iyo synthesis ye1 inoshandisa methyl urea uye cyanoacetic acid sezvinhu zvekutanga, uye inosangana nenhanho-nhanho maitiro e condensation, cyclization, nitrosation, kuderedza, cyclization, uye bromine ine goho rakazara re46.3%.Izvo zvimiro zvevose vepakati zvakasimbiswa ne1HNMR.

Chigadzirwa chazvino chine chekuita neyakapusa nzira yekugadzirira yepamusoro-purity linagliptin.Quinazoline, kiyi yepakati pekugadzira poto ye linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, yepakati inoparadzaniswa ne kusefa, uyezve kuita ne (R) 3 aminopiperidine dihydrochloride kuwana mhinduro ine linagliptin.Mushure memhinduro ine linagliptin yagadziriswa zvakare, Deliraliptin yakachena chigadzirwa.Kugadzirira kwekiyi yepakati pechigadzirwa chiripo kunotora nzira yepoto imwe, iyo iri nyore kushanda uye inovandudza goho.Mushure mekunge kiyi yepakati yaparadzaniswa, inobatwa ne (R) 3 aminopiperidine dihydrochloride, nekudaro Kuwana yakakwirira-kuchena linagliptin inosanganawo nekugadzirwa uye kuziviswa zvinodiwa zvemakambani emishonga kusvika pamwero mukuru.