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

Le suʻesuʻeina o le linagliptin o loʻo i ai nei ma lona 8-bromo-7-(2-butynyl) -3,7-dihydro-3-methyl-1- [(4-methyl -2-quinazolinyl) methyl) -1H-purine- 2,6-dione (11) auala faʻapipiʻi, saili se auala faʻapipiʻi talafeagai mo le gaosiga o fale gaosi oloa.Metotia: fai se aotelega o auala fa'apipi'i eseese.I'uga ma fa'ai'uga: Auala 2.2 o lo'o i ai se faiga faigofie ma maualalo le tau, lea e sili atu ona talafeagai mo le gaosiga o fale gaosi oloa.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione o se vaega autu i le tuʻufaʻatasia o le hypoglycemic drug linagliptin.O le faʻaogaina o le 1 faʻaaogaina le methyl urea ma le cyanoacetic acid e avea ma mea amata, ma faʻaalia ni laasaga e ono o le condensation, cyclization, nitrosation, faʻaitiitia, cyclization, ma le bromine ma le aofaʻi atoa o le 46.3%.O faʻatulagaga o fesoʻotaʻiga uma na faʻamaonia e le 1HNMR.

O le mea fou fou e fesoʻotaʻi ma se auala faigofie sauniuni o le linagliptin maualuga-mama.Quinazoline, o le mea autu autu mo le sauniuniga o 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, o le intermediate e vavaeeseina. filtration, ona tali atu lea i le (R)3 aminopiperidine dihydrochloride e maua ai se vaifofo e iai le linagliptin.A maeʻa ona toe gaosia le vaifofo o loʻo iai le linagliptin, Deliraliptin oloa mama.O le sauniuniga o le autu autu o le mea fou fou e faʻaaogaina ai se auala e tasi-pot, lea e faigofie ona faʻaogaina ma faʻaleleia le fua.A maeʻa ona tuʻueseese le vaega autu, e tali atu i le (R)3 aminopiperidine dihydrochloride, ma o le mauaina o le linagliptin mama maualuga e fetaui ma le gaosiga ma le taʻutinoga manaʻomia a kamupani vailaʻau i le tele.