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

No ka nānā ʻana i ka linagliptin e kū nei a me kāna kī waena 8-bromo-7-(2-butynyl) -3,7-dihydro-3-methyl-1-[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) hana synthesis, e ʻimi i kahi ala synthetic kūpono no ka hana ʻoihana.Hana: hōʻuluʻulu i nā ala synthetic like ʻole.Nā hualoaʻa a me nā hopena: Loaʻa i ke ala 2.2 kahi kaʻina hana maʻalahi a me ke kumukūʻai haʻahaʻa, ʻoi aku ka maikaʻi no ka hana ʻoihana.

ʻO 8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione kahi mea koʻikoʻi i ka synthesis o ka linagliptin lāʻau hypoglycemic.Hoʻohana ka synthesis o 1 i ka methyl urea a me ka cyanoacetic acid e like me ka hoʻomaka ʻana i nā mea hoʻomaka, a e hana i nā hopena ʻeono o ka condensation, cyclization, nitrosation, reduction, cyclization, a me bromine me ka huina o 46.3%.Ua hōʻoia ʻia nā hale o nā mea waena a pau e 1HNMR.

Pili ka mea hou i kēia manawa i kahi ʻano hoʻomākaukau maʻalahi o ka linagliptin maʻemaʻe kiʻekiʻe.ʻO Quinazoline, ke kī waena no ka hoʻomākaukau ʻana i hoʻokahi ipu o ka linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, ua hoʻokaʻawale ʻia ka waena e. kānana ʻana, a laila hana ʻia me (R)3 aminopiperidine dihydrochloride e loaʻa ai kahi hopena i loaʻa ka linagliptin.Ma hope o ka hoʻoponopono hou ʻia ʻana o ka linagliptin, ʻo Deliraliptin ka huahana maʻemaʻe.ʻO ka hoʻomākaukau ʻana o ke kī waena o ka mea i hana ʻia i kēia manawa e hoʻohana i kahi ʻano ipu hoʻokahi, kahi kūpono e hana a hoʻomaikaʻi i ka hua.Ma hope o ka hoʻokaʻawale ʻia ʻana o ke kī waena, ua hoʻopili ʻia me (R)3 aminopiperidine dihydrochloride, a laila e loaʻa ai ka linagliptin maʻemaʻe kiʻekiʻe e hoʻokō i nā koi a me ka hoʻolaha ʻana o nā ʻoihana lāʻau i ka nui loa.