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

Txhawm rau txheeb xyuas cov linagliptin uas twb muaj lawm thiab nws qhov tseem ceeb nruab nrab 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methyl -2-quinazolinyl)methyl)-1H-purine- 2,6-dione (11) synthesis txoj kev, nrhiav ib txoj kev hluavtaws haum rau kev tsim khoom.Txoj kev: summarize qhov sib txawv synthetic txoj kev.Cov txiaj ntsig thiab cov lus xaus: Txoj Kev 2.2 muaj cov txheej txheem yooj yim thiab tus nqi qis dua, uas tsim nyog rau kev tsim khoom lag luam.

8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione yog ib qho tseem ceeb nruab nrab ntawm cov synthesis ntawm cov tshuaj hypoglycemic linagliptin.Lub synthesis ntawm 1 siv methyl urea thiab cyanoacetic acid raws li cov ntaub ntawv pib, thiab dhau mus rau 6-kauj ruam kev tshwm sim ntawm condensation, cyclization, nitrosation, txo, cyclization, thiab bromine nrog tag nrho cov txiaj ntsig ntawm 46.3%.Cov qauv ntawm txhua tus neeg nruab nrab tau lees paub los ntawm 1HNMR.

Tam sim no invention muaj feem xyuam rau txoj kev npaj yooj yim ntawm high-purity linagliptin.Quinazoline, qhov nruab nrab tseem ceeb rau kev npaj ib lub lauj kaub ntawm linagliptin 8 bromo 7 (2 butyne 1 puag) 3,7 dihydro 3 methyl 1 [(4 methyl 2 quinazolinyl) methyl] 1H Purine 2,6 dione, qhov nruab nrab yog cais los ntawm filtration, thiab ces reacted nrog (R) 3 aminopiperidine dihydrochloride kom tau txais cov tshuaj uas muaj linagliptin.Tom qab cov tshuaj uas muaj linagliptin tau ua tiav dua, Deliraliptin cov khoom ntshiab.Kev npaj ntawm qhov tseem ceeb nruab nrab ntawm qhov kev tsim kho tam sim no siv txoj hauv kev ib lub lauj kaub, uas yooj yim rau kev khiav lag luam thiab txhim kho cov txiaj ntsig.Tom qab qhov tseem ceeb nruab nrab yog sib cais, nws yog reacted nrog (R) 3 aminopiperidine dihydrochloride, yog li tau txais high-purity linagliptin kuj ua tau raws li qhov yuav tsum tau ntawm zus tau tej cov thiab tshaj tawm cov kev cai ntawm cov tuam txhab tshuaj mus rau qhov loj tshaj plaws.