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

Ukuhlaziya i-linagliptin ekhona nokhiye wayo omaphakathi 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1--[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) indlela yokuhlanganisa, thola umzila wokwenziwa ofanele ukukhiqizwa kwezimboni.Indlela: fingqa izindlela ezihlukene zokwenziwa.Imiphumela neziphetho: Umzila 2.2 unenqubo elula uma kuqhathaniswa nezindleko eziphansi, ofaneleka kakhulu ukukhiqizwa kwezimboni.

I-8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione iyisihluthulelo esimaphakathi ekuhlanganisweni komuthi we-hypoglycemic linagliptin.I-synthesis ye-1 isebenzisa i-methyl urea ne-cyanoacetic acid njengezinto zokuqala, futhi ibhekana nezinyathelo eziyisithupha zokusabela kwe-condensation, i-cyclization, i-nitrosation, ukunciphisa, i-cyclization, ne-bromine enesivuno esiphelele esingu-46.3%.Izakhiwo zabo bonke abaphakathi ziqinisekiswe yi-1HNMR.

Ukusungulwa kwamanje kuhlobene nendlela elula yokulungiselela i-high-purity linagliptin.I-Quinazoline, isihluthulelo esimaphakathi sokulungiswa kwebhodwe elilodwa le-linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, okuphakathi kuhlukaniswe filtration, bese isabela nge-(R)3 aminopiperidine dihydrochloride ukuthola isixazululo esiqukethe i-linagliptin.Ngemuva kokuthi ikhambi eliqukethe i-linagliptin selicutshungulwe futhi, umkhiqizo ohlanzekile weDeliraliptin.Ukulungiswa kwesihluthulelo esiphakathi kokusungulwa kwamanje kusebenzisa indlela yebhodwe elilodwa, elilula ukusebenza futhi lithuthukise isivuno.Ngemuva kokuhlukaniswa kokhiye ophakathi nendawo, kusabela nge-(R)3 aminopiperidine dihydrochloride, ngaleyo ndlela Ukuthola i-linagliptin ehlanzekile futhi ihlangabezana nezidingo zokukhiqiza nezimemezelo zezinkampani zemithi ngezinga elikhulu kakhulu.