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

Ho sekaseka linagliptin e teng le senotlolo sa eona sa mahareng 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1--[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) mokhoa oa ho kopanya, fumana tsela ea maiketsetso e loketseng tlhahiso ea indasteri.Mokhoa: akaretsa litsela tse fapaneng tsa maiketsetso.Liphetho le liqeto: Route 2.2 e na le ts'ebetso e batlang e le bonolo le litšenyehelo tse tlase, tse loketseng tlhahiso ea indasteri.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione ke karolo e ka sehloohong ea motsoako oa motsoako oa lithethefatsi tsa hypoglycemic linagliptin.The synthesis ea 1 e sebelisa methyl urea le cyanoacetic acid e le lisebelisoa tsa ho qala, 'me e kena mehatong e tšeletseng ea condensation, cyclization, nitrosation, fokotsa, cyclization, le bromine ka lihlahisoa tse feletseng tsa 46.3%.Mehaho ea li-intermediate tsohle e tiisitsoe ke 1HNMR.

Moqapi oa hona joale o amana le mokhoa o bonolo oa ho itokisa oa linagliptin.Quinazoline, senotlolo sa bohareng bakeng sa ho lokisa pitsa e le 'ngoe ea linagliptin 8 bromo 7 (2 butyne 1 base) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, e bohareng e arotsoe ke filtration, 'me ka mor'a moo a itšoara ka (R)3 aminopiperidine dihydrochloride ho fumana tharollo e nang le linagliptin.Kamora hore tharollo e nang le linagliptin e sebetsoe hape, sehlahisoa se hloekileng sa Deliraliptin.Ho lokisoa ha senotlolo sa bohareng ba boqapi ba hona joale ho nka mokhoa oa pitsa e le 'ngoe, e loketseng ho sebetsa le ho ntlafatsa chai.Ka mor'a hore senotlolo sa bohareng se arohane, se sebetsanoa le (R) 3 aminopiperidine dihydrochloride, ka tsela eo Ho fumana linagliptin e phahameng ka ho fetisisa e kopana le litlhoko tsa tlhahiso le phatlalatso ea lik'hamphani tsa meriana ka tekanyo e kholo ka ho fetisisa.