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

Hei tātari i te linagliptin o naianei me tona takawaenga matua 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) tikanga whakahiato, kimihia he ara waihanga e tika ana mo te hanga ahumahi.Tikanga: whakarāpopotohia ngā momo ara waihanga.Nga hua me nga whakatau: Ko te huarahi 2.2 he mahinga ngawari me te utu iti ake, he pai ake mo te hanga ahumahi.

Ko te 8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione he takawaenga matua mo te whakahiato o te linagliptin tarukino hypoglycemic.Ko te whakahiatotanga o te 1 e whakamahi ana i te methyl urea me te waikawa cyanoacetic hei rauemi timatanga, a ka uru ki nga tauhohenga e ono-taahiraa o te condensation, cyclization, nitrosation, reduction, cyclization, and bromine with the total yield of 46.3%.Ko nga hanganga o nga takawaenga katoa i whakapumautia e 1HNMR.

Ko te hangahanga o naianei e pa ana ki tetahi tikanga whakarite ngawari o te linagliptin tino parakore.Quinazoline, te takawaenga matua mo te whakarite-kohua o te linagliptin 8 bromo 7 (2 butyne 1 turanga) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, ka wehea te takawaenga e tātari, ka tauhohe ki te (R)3 aminopiperidine dihydrochloride kia whiwhi ai i tetahi otinga kei roto te linagliptin.I muri i te otinga o te linagliptin ka tukatuka ano, ko Deliraliptin te hua parakore.Ko te whakaritenga o te takawaenga matua o te tenenga o naianei ka tango i te tikanga kohua kotahi, he pai ki te whakahaere me te whakapai ake i te hua.I muri i te wehenga o te takawaenga matua, ka tauhohehia ki te (R)3 aminopiperidine dihydrochloride, na reira ko te whiwhi i te linagliptin parakore-nui ka tutuki hoki nga whakaritenga whakaputa me te whakapuakitanga o nga kamupene rongoa ki te whānuitanga nui.